Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T01777
|
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Former ID |
TTDR01180
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Target Name |
Alpha-2C adrenergic receptor
|
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Gene Name |
ADRA2C
|
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Synonyms |
Alpha-2C adrenoceptor; Alpha-2C adrenoreceptor; Subtype C4; ADRA2C
|
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Target Type |
Successful
|
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Disease | Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | ||||
Alcohol use disorders [ICD9: 303; ICD10: F10.2] | |||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Asthma [ICD10: J45] | |||||
Contusion [ICD10: S36.220S] | |||||
Depression [ICD9: 311; ICD10: F30-F39] | |||||
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | |||||
Dementia; Obesity [ICD9:290-294, 278; ICD10: F01-F07, E66] | |||||
Diabetic nephropathy; Fibromyalgia [ICD9:250.4, 729.1; ICD10: E11.21, M79.7] | |||||
Erythema [ICD9: 695; ICD10: L51-L54] | |||||
Fibromyalgia [ICD9: 729.1; ICD10: M79.7] | |||||
Glaucoma [ICD9: 365; ICD10: H40-H42] | |||||
Hypertension [ICD9: 401; ICD10: I10-I16] | |||||
Hypotension [ICD9: 458, 796.3; ICD10: I95] | |||||
Heart arrhythmia [ICD10: I47-I49] | |||||
Heart failure [ICD9: 428; ICD10: I50] | |||||
Male sexual disorders [ICD10: F52] | |||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Ocular disease [ICD10: H00-H59] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Ocular hypertension [ICD9: 365.04; ICD10: H40.0] | |||||
Prostate disease [ICD10: N42.9] | |||||
Poison intoxication [ICD10: T36-T50] | |||||
Peptic ulcer [ICD9: 531-534; ICD10: K25-K27] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Sexual dysfunction [ICD9: 302.7; ICD10: F52] | |||||
Function |
Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins.
|
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BioChemical Class |
GPCR rhodopsin
|
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Target Validation |
T01777
|
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UniProt ID | |||||
Sequence |
MASPALAAALAVAAAAGPNASGAGERGSGGVANASGASWGPPRGQYSAGAVAGLAAVVGF
LIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFG QVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISA VISFPPLVSLYRQPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLR TRTLSEKRAPVGPDGASPTTENGLGAAAGAGENGHCAPPPADVEPDESSAAAERRRRRGA LRRGGRRRAGAEGGAGGADGQGAGPGAAESGALTASRSPGPGGRLSRASSRSVEFFLSRR RRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQVPGPLFK FFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ |
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Structure |
1HLL; 1HO9; 1HOD; 1HOF
|
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Drugs and Mode of Action | |||||
Drug(s) | Amezinium | Drug Info | Approved | Hypotension | [551871] |
Amosulalol | Drug Info | Approved | Hypertension | [533886] | |
Brimonidine | Drug Info | Approved | Ocular hypertension | [468255], [522318] | |
Dihydroergocristine | Drug Info | Approved | Alcohol use disorders | [533548], [539825] | |
MOXONIDINE | Drug Info | Approved | Alcohol use disorders | [526626] | |
Propylhexedrine | Drug Info | Approved | Obesity | [551871] | |
Rilmenidine | Drug Info | Approved | Hypertension | [551871] | |
Tetrahydrozoline | Drug Info | Approved | Ocular disease | [529302] | |
Xylometazoline | Drug Info | Phase 4 | Allergic rhinitis | [468231], [522245] | |
IDAZOXAN HYDROCHLORIDE | Drug Info | Phase 3 | Neurological disease | [521807] | |
TNX-102 | Drug Info | Phase 3 | Fibromyalgia | [547624] | |
AGN-XX/YY | Drug Info | Phase 2 | Diabetic nephropathy; Fibromyalgia | [549889] | |
MEDETOMIDINE | Drug Info | Phase 2 | Pain | [529347] | |
ORM-12741 | Drug Info | Phase 2 | Alzheimer disease | [525230] | |
V-101 | Drug Info | Phase 2 | Erythema | [523141] | |
INDORAMIN | Drug Info | Withdrawn from market | Hypertension | [468125], [551871] | |
Ecabapide | Drug Info | Discontinued in Preregistration | Peptic ulcer | [544686] | |
Delequamine hydrochloride | Drug Info | Discontinued in Phase 3 | Male sexual disorders | [546534] | |
FLUPAROXAN | Drug Info | Discontinued in Phase 3 | Depression | [540696], [544705] | |
NOLOMIROLE HYDROCHLORIDE | Drug Info | Discontinued in Phase 3 | Heart failure | [545464] | |
Deriglidole | Drug Info | Discontinued in Phase 2 | Diabetes | [544511] | |
Fadolmidine | Drug Info | Discontinued in Phase 2 | Pain | [547121] | |
GYKI-16084 | Drug Info | Discontinued in Phase 2 | Prostate disease | [546866] | |
JTH-601 | Drug Info | Discontinued in Phase 2 | Prostate disease | [546856] | |
MAZAPERTINE | Drug Info | Discontinued in Phase 2 | Discovery agent | [545274] | |
MK-912 | Drug Info | Discontinued in Phase 2 | Discovery agent | [544718] | |
NMI-870 | Drug Info | Discontinued in Phase 2 | Sexual dysfunction | [547220] | |
SGB-1534 | Drug Info | Discontinued in Phase 2 | Hypotension | [544565] | |
GYKI-12743 | Drug Info | Discontinued in Phase 1 | Hypertension | [545079] | |
A-75169 | Drug Info | Terminated | Glaucoma | [545494] | |
A-80426 | Drug Info | Terminated | Discovery agent | [546043] | |
ARC239 | Drug Info | Terminated | Discovery agent | [540708], [544602] | |
F-14413 | Drug Info | Terminated | Alzheimer disease | [547865] | |
Midaglizole | Drug Info | Terminated | Asthma | [544537] | |
SK&F-104078 | Drug Info | Terminated | Discovery agent | [544626] | |
SNAP-5089 | Drug Info | Terminated | Heart arrhythmia | [468115], [546179] | |
WB-4101 | Drug Info | Terminated | Discovery agent | [468117], [545656] | |
Inhibitor | (+/-)-nantenine | Drug Info | [530558] | ||
(1,2,3,4-Tetrahydro-isoquinolin-3-yl)-methanol | Drug Info | [525507] | |||
(1H-Benzoimidazol-5-yl)-(1H-imidazol-2-yl)-amine | Drug Info | [534315] | |||
(1H-Imidazol-2-yl)-quinoxalin-6-yl-amine | Drug Info | [534315] | |||
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine | Drug Info | [534315] | |||
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine | Drug Info | [534315] | |||
(2-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine | Drug Info | [534087] | |||
(3-Ethyl-indol-1-yl)-propyl-pyridin-4-yl-amine | Drug Info | [534087] | |||
(3-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine | Drug Info | [534087] | |||
(R)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [534195] | |||
(S)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [534195] | |||
1,2,3,4,4a,5,10,10a-Octahydro-benzo[g]quinoline | Drug Info | [534719] | |||
1,2,3,4,5,6-Hexahydro-benzo[c]azocine | Drug Info | [534195] | |||
1,2,3,4-Tetrahydro-benzo[h]isoquinolin-8-ol | Drug Info | [534531] | |||
1,2,3,4-Tetrahydro-isoquinolin-7-ol | Drug Info | [534531] | |||
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole | Drug Info | [526994] | |||
1,2,3,4-tetrahydroisoquinoline | Drug Info | [528403] | |||
1-((S)-2-aminopropyl)-1H-indazol-6-ol | Drug Info | [527952] | |||
2,3,4,5-Tetrahydro-1H-benzo[c]azepine | Drug Info | [534195] | |||
2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine | Drug Info | [534195] | |||
2,3,4,5-Tetrahydro-benzo[f][1,4]oxazepine | Drug Info | [534195] | |||
2,3-Dihydro-1H-isoindole | Drug Info | [534195] | |||
2-BFi | Drug Info | [525733] | |||
3-Fluoromethyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [527365] | |||
3-Methoxymethyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [525507] | |||
3-Methyl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [534195] | |||
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole | Drug Info | [533805] | |||
4-(4-Methyl-indan-1-yl)-1H-imidazole | Drug Info | [534467] | |||
5-Aminomethyl-naphthalen-2-ol | Drug Info | [534531] | |||
6,7,8,9-Tetrahydro-5-thia-8-aza-benzocycloheptene | Drug Info | [534195] | |||
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | [526918] | |||
8-Methoxy-1,2,3,4-tetrahydro-benzo[h]isoquinoline | Drug Info | [534531] | |||
A-80426 | Drug Info | [527481] | |||
Butyl-indol-1-yl-pyridin-4-yl-amine | Drug Info | [534087] | |||
C-(6-Methoxy-naphthalen-1-yl)-methylamine | Drug Info | [534531] | |||
C-Naphthalen-1-yl-methylamine | Drug Info | [534531] | |||
CONESSINE | Drug Info | [529632] | |||
Ethyl-indol-1-yl-pyridin-4-yl-amine | Drug Info | [534087] | |||
GNF-PF-2857 | Drug Info | [528472] | |||
GNF-PF-3427 | Drug Info | [528472] | |||
GNF-PF-3878 | Drug Info | [528472] | |||
Indol-1-yl-methyl-pyridin-4-yl-amine | Drug Info | [534087] | |||
Indol-1-yl-prop-2-ynyl-pyridin-4-yl-amine | Drug Info | [534087] | |||
Indol-1-yl-propyl-pyridin-4-yl-amine | Drug Info | [534087] | |||
Indol-1-yl-pyridin-4-yl-amine | Drug Info | [534087] | |||
INDORAMIN | Drug Info | [533682] | |||
MAZAPERTINE | Drug Info | [533800] | |||
MEDETOMIDINE | Drug Info | [533805] | |||
METHYLNORADRENALINE | Drug Info | [533545] | |||
MEZILAMINE | Drug Info | [533406] | |||
MOXONIDINE | Drug Info | [534128] | |||
PIPEROXAN | Drug Info | [533545] | |||
R-226161 | Drug Info | [528772] | |||
RX-821002 | Drug Info | [533375] | |||
S-34324 | Drug Info | [527481] | |||
SK&F-104078 | Drug Info | [533682] | |||
SK&F-64139 | Drug Info | [528403] | |||
SNAP-5089 | Drug Info | [525611] | |||
SNAP-5150 | Drug Info | [525611] | |||
TRACIZOLINE | Drug Info | [526918] | |||
TRAMAZOLINE | Drug Info | [533545] | |||
TRYPTOLINE | Drug Info | [526918] | |||
WB-4101 | Drug Info | [533545] | |||
Modulator (allosteric modulator) | 5-(N,N-hexamethylene)-amiloride | Drug Info | [534623] | ||
Antagonist | 5-methylurapidil | Drug Info | [526042] | ||
all-trans-4-oxo-retinoic acid | Drug Info | [527472] | |||
ARC239 | Drug Info | [535225] | |||
Ciproxifan | Drug Info | [536039] | |||
F-14413 | Drug Info | [527640] | |||
GYKI-16084 | Drug Info | [528199] | |||
JP1302 | Drug Info | [528615] | |||
JTH-601 | Drug Info | [525752] | |||
MK-912 | Drug Info | [534977] | |||
ORM-12741 | Drug Info | [532654] | |||
piribedil | Drug Info | [526443] | |||
spiroxatrine | Drug Info | [526102] | |||
TNX-102 | Drug Info | [551739] | |||
[125I]BE-2254 | Drug Info | [533751] | |||
[3H]MK-912 | Drug Info | [533843] | |||
[3H]rauwolscine | Drug Info | [526770] | |||
[3H]RX821002 | Drug Info | [533799] | |||
Agonist | 6-fluoro-noradrenaline | Drug Info | [533826] | ||
A61603 | Drug Info | [533660] | |||
AGN-XX/YY | Drug Info | [550943] | |||
amidephrine | Drug Info | [533826] | |||
Chloroethylclonidine | Drug Info | [537921] | |||
cirazoline | Drug Info | [533826] | |||
Fadolmidine | Drug Info | [527103] | |||
indanidine | Drug Info | [533826] | |||
SKF 89748 | Drug Info | [533826] | |||
V-101 | Drug Info | [532145] | |||
xylazine | Drug Info | [534634] | |||
[125I]HEAT | Drug Info | [533679] | |||
Modulator | A-75169 | Drug Info | [550028] | ||
Amezinium | Drug Info | [533574], [551871] | |||
Amosulalol | Drug Info | [533886], [551871] | |||
Brimonidine | Drug Info | [468255] | |||
Delequamine hydrochloride | Drug Info | [534174] | |||
Deriglidole | Drug Info | [534576] | |||
Dihydroergocristine | Drug Info | [533548], [551871] | |||
Ecabapide | Drug Info | [534260] | |||
ETHOXY-IDAZOXAN | Drug Info | [531785] | |||
FLUPAROXAN | Drug Info | [528251] | |||
GYKI-12743 | Drug Info | [528315] | |||
IDAZOXAN HYDROCHLORIDE | Drug Info | [526773] | |||
Midaglizole | Drug Info | [533463] | |||
NMI-870 | Drug Info | [544155] | |||
NOLOMIROLE HYDROCHLORIDE | Drug Info | [526875] | |||
Propylhexedrine | Drug Info | [533622], [551871] | |||
Rilmenidine | Drug Info | [534272], [551871] | |||
SGB-1534 | Drug Info | [533371] | |||
Tetrahydrozoline | Drug Info | [529302], [551871] | |||
V-103 | Drug Info | [543685] | |||
Xylometazoline | Drug Info | [530593], [551871] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | cGMP-PKG signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
PANTHER Pathway | Alpha adrenergic receptor signaling pathway | ||||
Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
Reactome | Adrenoceptors | ||||
Adrenaline signalling through Alpha-2 adrenergic receptor | |||||
Adrenaline,noradrenaline inhibits insulin secretion | |||||
G alpha (i) signalling events | |||||
G alpha (z) signalling events | |||||
Surfactant metabolism | |||||
WikiPathways | Monoamine GPCRs | ||||
GPCRs, Class A Rhodopsin-like | |||||
Platelet Aggregation (Plug Formation) | |||||
Integration of energy metabolism | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 468115 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 498). | ||||
Ref 468117 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 499). | ||||
Ref 468125 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 501). | ||||
Ref 468231 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 517). | ||||
Ref 468255 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 520). | ||||
Ref 521807 | ClinicalTrials.gov (NCT00294944) The Effectiveness of Idazoxan in Treating TRD. U.S. National Institutes of Health. | ||||
Ref 522245 | ClinicalTrials.gov (NCT00630474) Nasal Decongestion and Obstructive Sleep Apnea. U.S. National Institutes of Health. | ||||
Ref 522318 | ClinicalTrials.gov (NCT00675207) Comparison of Brimonidine Purite, Dorzolamide, and Brinzolamide as Adjunctive Therapy to Prostaglandin Analogs. U.S. National Institutes of Health. | ||||
Ref 523141 | ClinicalTrials.gov (NCT01186068) Dose Response Study of Patients With Erythematous Rosacea. U.S. National Institutes of Health. | ||||
Ref 525230 | ClinicalTrials.gov (NCT02471196) Efficacy of ORM-12741 on Agitation/Aggression Symptoms in Alzheimer's Disease. | ||||
Ref 526626 | The role of I(1)-imidazoline and alpha(2)-adrenergic receptors in the modulation of glucose metabolism in the spontaneously hypertensive obese rat model of metabolic syndrome X. J Pharmacol Exp Ther.2003 Aug;306(2):646-57. Epub 2003 May 19. | ||||
Ref 529302 | Prolonged cardiovascular effects after unintentional ingestion of tetrahydrozoline. Clin Toxicol (Phila). 2008 Feb;46(2):171-2. | ||||
Ref 529347 | Sedative and cardiopulmonary effects of medetomidine hydrochloride and xylazine hydrochloride and their reversal with atipamezole hydrochloride in calves. Am J Vet Res. 2008 Mar;69(3):319-29. | ||||
Ref 533548 | Effect of dihydroergocristine on blood pressure and activity at peripheral alpha-adrenoceptors in pithed rats. Eur J Pharmacol. 1984 Jan 13;97(1-2):21-7. | ||||
Ref 533886 | Effects of amosulalol, a combined alpha 1- and beta-adrenoceptor-blocking agent, on ischemic myocardial energy metabolism in dogs. J Pharm Sci. 1993 Mar;82(3):291-5. | ||||
Ref 539825 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 278). | ||||
Ref 540696 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 41). | ||||
Ref 540708 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 524). | ||||
Ref 544511 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000010) | ||||
Ref 544537 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000085) | ||||
Ref 544565 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000148) | ||||
Ref 544602 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000266) | ||||
Ref 544626 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000354) | ||||
Ref 544686 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000582) | ||||
Ref 544705 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000678) | ||||
Ref 544718 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000716) | ||||
Ref 545079 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002059) | ||||
Ref 545274 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662) | ||||
Ref 545464 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003364) | ||||
Ref 545494 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003469) | ||||
Ref 545656 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004048) | ||||
Ref 546043 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006017) | ||||
Ref 546179 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006771) | ||||
Ref 546534 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008832) | ||||
Ref 546856 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010685) | ||||
Ref 546866 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010746) | ||||
Ref 547121 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013220) | ||||
Ref 547220 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014166) | ||||
Ref 547624 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017946) | ||||
Ref 468255 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 520). | ||||
Ref 525507 | J Med Chem. 1999 Jun 3;42(11):1982-90.3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor. | ||||
Ref 525611 | Bioorg Med Chem Lett. 1999 Oct 4;9(19):2843-8.Design and synthesis of novel dihydropyridine alpha-1a antagonists. | ||||
Ref 525733 | Bioorg Med Chem Lett. 2000 Mar 20;10(6):605-7.Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand. | ||||
Ref 525752 | Effect of JTH-601, a novel alpha(1)-adrenoceptor antagonist, on prostate function in dogs. Eur J Pharmacol. 2000 Apr 7;394(1):123-30. | ||||
Ref 526042 | Phe-308 and Phe-312 in transmembrane domain 7 are major sites of alpha 1-adrenergic receptor antagonist binding. Imidazoline agonists bind like antagonists. J Biol Chem. 2001 Jul 6;276(27):25366-71. Epub 2001 Apr 30. | ||||
Ref 526102 | Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes. Jpn J Pharmacol. 2001 Jun;86(2):189-95. | ||||
Ref 526443 | Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. | ||||
Ref 526770 | Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. Mol Pharmacol. 1992 Jul;42(1):1-5. | ||||
Ref 526773 | Different sites of action for alpha 2-adrenoceptor antagonists in the modulation of noradrenaline release and contraction response in the vas deferens of the rat. J Pharm Pharmacol. 1992 Mar;44(3):231-4. | ||||
Ref 526875 | Effect of nolomirole on monocrotaline-induced heart failure. Pharmacol Res. 2004 Jan;49(1):1-5. | ||||
Ref 526918 | Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors. | ||||
Ref 526994 | Bioorg Med Chem Lett. 2004 Feb 23;14(4):1003-5.Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands. | ||||
Ref 527103 | Antinociceptive properties of fadolmidine (MPV-2426), a novel alpha2-adrenoceptor agonist. CNS Drug Rev. 2004 Summer;10(2):117-26. | ||||
Ref 527365 | J Med Chem. 2005 Jan 13;48(1):134-40.3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity. | ||||
Ref 527472 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. J Med Chem. 2005 Mar 24;48(6):1709-12. | ||||
Ref 527481 | J Med Chem. 2005 Mar 24;48(6):2054-71.Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity. | ||||
Ref 527640 | Activation of noradrenergic transmission by alpha2-adrenoceptor antagonists counteracts deafferentation-induced neuronal death and cell proliferation in the adult mouse olfactory bulb. Exp Neurol. 2005 Aug;194(2):444-56. | ||||
Ref 527952 | J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. | ||||
Ref 528199 | A novel approach to the treatment of benign prostatic hyperplasia. BJU Int. 2006 Jun;97(6):1252-5. | ||||
Ref 528251 | The pharmacology of fluparoxan: a selective alpha 2-adrenoceptor antagonist. Br J Pharmacol. 1991 Apr;102(4):887-95. | ||||
Ref 528315 | GYKI-12743 a new postsynaptic vascular alpha-adrenoceptor antagonist. Acta Physiol Hung. 1991;77(3-4):257-67. | ||||
Ref 528403 | J Med Chem. 2006 Sep 7;49(18):5424-33.Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamineN-methyltransferase. | ||||
Ref 528472 | J Med Chem. 2006 Oct 19;49(21):6351-63.Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists. | ||||
Ref 528615 | Pharmacological characterization and CNS effects of a novel highly selective alpha2C-adrenoceptor antagonist JP-1302. Br J Pharmacol. 2007 Feb;150(4):391-402. Epub 2007 Jan 15. | ||||
Ref 528772 | Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism. | ||||
Ref 529302 | Prolonged cardiovascular effects after unintentional ingestion of tetrahydrozoline. Clin Toxicol (Phila). 2008 Feb;46(2):171-2. | ||||
Ref 529632 | J Med Chem. 2008 Sep 11;51(17):5423-30. Epub 2008 Aug 7.The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. | ||||
Ref 530558 | Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. | ||||
Ref 530593 | Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. | ||||
Ref 531785 | Discriminative stimulus properties of ethoxy idazoxan. J Psychopharmacol. 1995 Jan;9(3):228-33. | ||||
Ref 532145 | Rosacea: update on management and emerging therapies. Skin Therapy Lett. 2012 Dec;17(10):1-4. | ||||
Ref 532654 | A double-blind, randomized, placebo-controlled crossover trial of the alpha2C-adrenoceptor antagonist ORM-12741 for prevention of cold-induced vasospasm in patients with systemic sclerosis. Rheumatology (Oxford). 2014 May;53(5):948-52. | ||||
Ref 533371 | Potent alpha-adrenoceptor blocking action of SGB-1534, a new quinazoline antihypertensive agent in vitro experiments. Gen Pharmacol. 1986;17(2):143-9. | ||||
Ref 533375 | J Med Chem. 1986 Oct;29(10):2000-3.Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists. | ||||
Ref 533406 | J Med Chem. 1986 Aug;29(8):1394-8.4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors. | ||||
Ref 533463 | Studies of midaglizole (DG-5128). A new type of oral hypoglycemic drug in healthy subjects. Diabetes. 1987 Feb;36(2):216-20. | ||||
Ref 533545 | J Med Chem. 1982 Dec;25(12):1389-401.alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs. | ||||
Ref 533548 | Effect of dihydroergocristine on blood pressure and activity at peripheral alpha-adrenoceptors in pithed rats. Eur J Pharmacol. 1984 Jan 13;97(1-2):21-7. | ||||
Ref 533574 | Pharmacology of amezinium, a novel antihypotensive drug. III. Studies on the mechanism of action. Arzneimittelforschung. 1981;31(9a):1558-65. | ||||
Ref 533622 | Airway compromise and delayed death following attempted central vein injection of propylhexedrine. J Emerg Med. 1994 Nov-Dec;12(6):795-7. | ||||
Ref 533660 | A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype. J Pharmacol Exp Ther. 1995 Jul;274(1):97-103. | ||||
Ref 533679 | KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues. Mol Pharmacol. 1995 Aug;48(2):250-8. | ||||
Ref 533682 | J Med Chem. 1995 Sep 1;38(18):3415-44.Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. | ||||
Ref 533751 | Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. J Pharmacol Exp Ther. 1995 Jan;272(1):134-42. | ||||
Ref 533799 | Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs. Eur J Pharmacol. 1994 Jan 24;252(1):43-9. | ||||
Ref 533800 | J Med Chem. 1994 Apr 15;37(8):1060-2.A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. | ||||
Ref 533805 | J Med Chem. 1994 Jul 22;37(15):2328-33.A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors. | ||||
Ref 533826 | Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes. Mol Pharmacol. 1994 Nov;46(5):929-36. | ||||
Ref 533843 | The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors. J Pharmacol Exp Ther. 1994 Dec;271(3):1558-65. | ||||
Ref 533886 | Effects of amosulalol, a combined alpha 1- and beta-adrenoceptor-blocking agent, on ischemic myocardial energy metabolism in dogs. J Pharm Sci. 1993 Mar;82(3):291-5. | ||||
Ref 534087 | J Med Chem. 1996 Jan 19;39(2):570-81.Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. | ||||
Ref 534128 | J Med Chem. 1996 Mar 15;39(6):1193-5.Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. | ||||
Ref 534174 | Modulation of sexual behaviour in the rat by a potent and selective alpha 2-adrenoceptor antagonist, delequamine (RS-15385-197). Br J Pharmacol. 1996 May;118(1):63-72. | ||||
Ref 534195 | J Med Chem. 1996 Aug 30;39(18):3539-46.Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase. | ||||
Ref 534260 | Identification of major biliary and urinary metabolites of ecabapide in rats. Xenobiotica. 1996 Sep;26(9):983-94. | ||||
Ref 534272 | Rilmenidine-induced ocular hypotension: role of imidazoline1 and alpha 2 receptors. Curr Eye Res. 1996 Sep;15(9):943-50. | ||||
Ref 534315 | J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists. | ||||
Ref 534467 | J Med Chem. 1997 Sep 12;40(19):3014-24.Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket". | ||||
Ref 534531 | J Med Chem. 1997 Dec 5;40(25):3997-4005.Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. | ||||
Ref 534576 | Mechanisms of the hypoglycemic effects of the alpha2-adrenoceptor antagonists SL84.0418 and deriglidole. Life Sci. 1998;62(9):839-52. | ||||
Ref 534623 | Characterization of the allosteric interactions between antagonists and amiloride analogues at the human alpha2A-adrenergic receptor. Mol Pharmacol. 1998 May;53(5):916-25. | ||||
Ref 534634 | Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding. Biochem Pharmacol. 1998 Apr 1;55(7):1035-43. | ||||
Ref 534719 | J Med Chem. 1998 Oct 8;41(21):4165-70.N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies. | ||||
Ref 534977 | Silent alpha(2C)-adrenergic receptors enable cold-induced vasoconstriction in cutaneous arteries. Am J Physiol Heart Circ Physiol. 2000 Apr;278(4):H1075-83. | ||||
Ref 535225 | Potent alpha(2A)-adrenoceptor-mediated vasoconstriction by brimonidine in porcine ciliary arteries. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2049-55. | ||||
Ref 536039 | The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20. | ||||
Ref 537921 | Selective irreversible binding of chloroethylclonidine at alpha 1- and alpha 2-adrenoceptor subtypes. Mol Pharmacol. 1993 Dec;44(6):1165-70. | ||||
Ref 543685 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 27). | ||||
Ref 544155 | Female Sexual Dysfunction: Therapeutic Options and Experimental Challenges. Cardiovasc Hematol Agents Med Chem. 2009 October; 7(4): 260-269. |
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