Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T23547
|
||||
Former ID |
TTDS00125
|
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Target Name |
Opioid receptor
|
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Target Type |
Successful
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Disease | Alcohol dependence [ICD10: F10] | ||||
Analgesia [ICD9: 338; ICD10: R52, G89] | |||||
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42] | |||||
Alcohol use disorders [ICD9: 303; ICD10: F10.2] | |||||
Constipation [ICD9: 564; ICD10: K59.0] | |||||
Cancer pain [ICD9: 140-229, 338,780; ICD10: R52, G89] | |||||
Dry cough; Drug withdrawal syndrome; Ppioid type drug dependence [ICD10: R05] | |||||
Hepatitis virus infection [ICD9: 573.3; ICD10: K75.9] | |||||
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26] | |||||
Influenza A infection [ICD10: J10, J11] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Moderate to severe pain [ICD10: R52, G89] | |||||
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0] | |||||
Opioid induced adverse effect [ICD9: 304; ICD10: F11] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Opioid addication [ICD10: F11] | |||||
Parkinson's disease [ICD9: 332; ICD10: G20] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29] | |||||
BioChemical Class |
GPCR rhodopsin
|
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Target Validation |
T23547
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Drugs and Mode of Action | |||||
Drug(s) | Dextropropoxyphene | Drug Info | Approved | Pain | [536942], [542582] |
Ketobemidone | Drug Info | Approved | Pain | [551871] | |
Levorphanol | Drug Info | Approved | Moderate to severe pain | [551871] | |
Methadone | Drug Info | Approved | Dry cough; Drug withdrawal syndrome; Ppioid type drug dependence | [551871] | |
Nalmefene | Drug Info | Approved | Opioid addication | [551871] | |
Naltrexone | Drug Info | Approved | Alcohol dependence | [551871] | |
Oxymorphone | Drug Info | Approved | Moderate to severe pain | [551871] | |
Pentazocine | Drug Info | Approved | Moderate to severe pain | [551871] | |
Sufentanil | Drug Info | Approved | Analgesia | [551871] | |
Tilidine | Drug Info | Approved | Pain | [551871] | |
Dihydrocodeine | Drug Info | Phase 4 | Cancer pain | [522148], [542583] | |
Naltrexone | Drug Info | Phase 4 | Human immunodeficiency virus infection | [525241], [539012] | |
Oxymorphone | Drug Info | Phase 4 | Pain | [522753], [542100] | |
ALO-02 Oxycodone- naltrexone core | Drug Info | Phase 3 | Pain | [551491] | |
Bupropion+naltrexone | Drug Info | Phase 3 | Obesity | [532233] | |
Oravescent fentanyl | Drug Info | Phase 3 | Neuropathic pain | [536374] | |
AeroLEF | Drug Info | Phase 2 | Pain | [522487] | |
AZD-7268 | Drug Info | Phase 2 | Anxiety disorder | [522867], [542769] | |
CNSB-001 | Drug Info | Phase 2 | Neuropathic pain | [548808] | |
JKB-122 | Drug Info | Phase 2 | Hepatitis virus infection | [525323] | |
NP-2 | Drug Info | Phase 2 | Influenza A infection | [548787] | |
OCFENTANIL | Drug Info | Phase 2 | Pain | [531161] | |
Odelepran | Drug Info | Phase 2 | Alcohol use disorders | [522511] | |
Oxytrex | Drug Info | Phase 2 | Pain | [522403] | |
S-297995 | Drug Info | Phase 2 | Opioid induced adverse effect | [551683] | |
PTI-202 | Drug Info | Phase 1 | Pain | [548354] | |
SYN-1001 | Drug Info | Phase 1 | Pain | [547773] | |
CB-01-16 | Drug Info | Preclinical | Constipation | [548954] | |
Propiram fumarate | Drug Info | Discontinued in Phase 3 | Cancer pain | [545491] | |
CereCRIB | Drug Info | Discontinued in Phase 2 | Pain | [546394] | |
OxycoDex | Drug Info | Discontinued in Phase 2 | Pain | [547593] | |
PTI-701 | Drug Info | Discontinued in Phase 2 | Pain | [547276] | |
Ultramorph | Drug Info | Discontinued in Phase 2 | Pain | [547177] | |
BL-1827 | Drug Info | Discontinued in Phase 1 | Cancer pain | [547169] | |
APF-580 | Drug Info | Terminated | Pain | [548583] | |
EK-399 | Drug Info | Terminated | Inflammatory disease | [545666] | |
Org-30035 | Drug Info | Terminated | Psychotic disorders | [545339] | |
OX-23 | Drug Info | Terminated | Pain | [548624] | |
Agonist | AeroLEF | Drug Info | [544239] | ||
BL-1827 | Drug Info | [547170] | |||
CNSB-001 | Drug Info | [544320] | |||
Dextropropoxyphene | Drug Info | [536942] | |||
Levorphanol | Drug Info | [535895] | |||
Methadone | Drug Info | [537460], [537485] | |||
Oravescent fentanyl | Drug Info | [536374] | |||
SYN-1001 | Drug Info | [527377] | |||
Ultramorph | Drug Info | [525691] | |||
Modulator | ALO-02 Oxycodone- naltrexone core | Drug Info | [527586] | ||
APF-580 | Drug Info | [550145] | |||
AZD-7268 | Drug Info | [550881] | |||
BRIFENTANIL | Drug Info | [531532], [551871] | |||
CereCRIB | Drug Info | [550829] | |||
Dihydrocodeine | Drug Info | [526452] | |||
EK-399 | Drug Info | [528069] | |||
JKB-122 | Drug Info | [550158], [551871] | |||
Ketobemidone | Drug Info | [534254], [551871] | |||
OCFENTANIL | Drug Info | [530205], [551871] | |||
Org-30035 | Drug Info | [550146] | |||
OxycoDex | Drug Info | [531999] | |||
Oxymorphone | Drug Info | [542100] | |||
Oxytrex | Drug Info | [528981] | |||
Propiram fumarate | Drug Info | [533551] | |||
PTI-202 | Drug Info | [551481] | |||
PTI-701 | Drug Info | [551480] | |||
Tilidine | Drug Info | [527358], [551871] | |||
Antagonist | Bupropion+naltrexone | Drug Info | [536710] | ||
CB-01-16 | Drug Info | [550566] | |||
Cyprodine | Drug Info | [536285] | |||
Nalmefene | Drug Info | [536742], [536928] | |||
Naltrexone | Drug Info | [529288], [551871] | |||
NP-2 | Drug Info | [526015] | |||
Odelepran | Drug Info | [532470] | |||
Pentazocine | Drug Info | [534923], [537855] | |||
S-297995 | Drug Info | [551683] | |||
Sufentanil | Drug Info | [537460] | |||
References | |||||
Ref 522148 | ClinicalTrials.gov (NCT00547885) Randomized Controlled Double Blind Trial of Short vs Long Acting Dihydrocodeine in Chronic Non-malignant Pain. U.S. National Institutes of Health. | ||||
Ref 522403 | ClinicalTrials.gov (NCT00734461) Study to Evaluate the Subjective Effects of PTI-801 in Non-Physically Dependent Subjects With a History of Drug Abuse. U.S. National Institutes of Health. | ||||
Ref 522487 | ClinicalTrials.gov (NCT00791804) Phase II Study of Inhaled AeroLEF for Analgesia After ACL Knee Surgery. U.S. National Institutes of Health. | ||||
Ref 522511 | ClinicalTrials.gov (NCT00804570) A Study for the Treatment of Alcohol Dependence.. U.S. National Institutes of Health. | ||||
Ref 522753 | ClinicalTrials.gov (NCT00955110) Study to Compare Oxymorphone Extended-Release (Opana ER) Versus Oxycodone Controlled-Release (Oxycontin). U.S. National Institutes of Health. | ||||
Ref 522867 | ClinicalTrials.gov (NCT01020799) AZD7268 Safety and Tolerability Study. U.S. National Institutes of Health. | ||||
Ref 531161 | A phase II clinical study of once-a-day fentanyl citrate patch in patients with cancer pain--switching from once-every-three-days fentanyl patch to once-a-day fentanyl citrate patch. Gan To Kagaku Ryoho. 2010 Sep;37(9):1747-52. | ||||
Ref 532233 | A randomized, phase 3 trial of naltrexone SR/bupropion SR on weight and obesity-related risk factors (COR-II). Obesity (Silver Spring). 2013 May;21(5):935-43. | ||||
Ref 536942 | Retrospective diagnosis of an adverse drug reaction in a breastfed neonate: liquid chromatography-tandem mass spectrometry quantification of dextropropoxyphene and norpropoxyphene in newborn and maternal hair. J Anal Toxicol. 2008 Nov-Dec;39(9):787-9. | ||||
Ref 539012 | (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: 1639). | ||||
Ref 542100 | (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: 7094). | ||||
Ref 542582 | (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: 7593). | ||||
Ref 542583 | (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: 7594). | ||||
Ref 542769 | (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: 7824). | ||||
Ref 545339 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002901) | ||||
Ref 545491 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003460) | ||||
Ref 545666 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004080) | ||||
Ref 546394 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007886) | ||||
Ref 547169 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013581) | ||||
Ref 547177 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013632) | ||||
Ref 547276 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014737) | ||||
Ref 547593 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017613) | ||||
Ref 547773 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019167) | ||||
Ref 548354 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024906) | ||||
Ref 548583 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026787) | ||||
Ref 548624 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027164) | ||||
Ref 548787 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028817) | ||||
Ref 548808 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029018) | ||||
Ref 525691 | Antagonists of excitatory opioid receptor functions enhance morphine's analgesic potency and attenuate opioid tolerance/dependence liability. Pain. 2000 Feb;84(2-3):121-31. | ||||
Ref 526015 | Vascular endothelial growth factor receptor-1 and neuropilin-2 form complexes. J Biol Chem. 2001 Jun 1;276(22):18688-94. Epub 2001 Mar 14. | ||||
Ref 526452 | Affinities of dihydrocodeine and its metabolites to opioid receptors. Pharmacol Toxicol. 2002 Aug;91(2):57-63. | ||||
Ref 527358 | Actions of tilidine and nortilidine on cloned opioid receptors. Eur J Pharmacol. 2005 Jan 4;506(3):205-8. Epub 2004 Dec 15. | ||||
Ref 527377 | Improved brain uptake and pharmacological activity profile of morphine-6-glucuronide using a peptide vector-mediated strategy. J Pharmacol Exp Ther. 2005 May;313(2):712-9. Epub 2005 Jan 12. | ||||
Ref 527586 | Adding ultralow-dose naltrexone to oxycodone enhances and prolongs analgesia: a randomized, controlled trial of Oxytrex. J Pain. 2005 Jun;6(6):392-9. | ||||
Ref 528069 | Evaluation of the discriminative stimulus effect of an enkephalin analog, EK-399, in the rat. Nihon Yakurigaku Zasshi. 1991 Jun;97(6):361-9. | ||||
Ref 528981 | Oxytrex: an oxycodone and ultra-low-dose naltrexone formulation. Expert Opin Investig Drugs. 2007 Aug;16(8):1277-83. | ||||
Ref 529288 | An evaluation of mu-opioid receptor (OPRM1) as a predictor of naltrexone response in the treatment of alcohol dependence: results from the Combined Pharmacotherapies and Behavioral Interventions for Alcohol Dependence (COMBINE) study. Arch Gen Psychiatry. 2008 Feb;65(2):135-44. | ||||
Ref 530205 | Comparison of ocfentanil and fentanyl as supplements to general anesthesia. Anesth Analg. 1991 Nov;73(5):622-6. | ||||
Ref 531532 | Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics. J Med Chem. 1990 Oct;33(10):2876-82. | ||||
Ref 531999 | Differential activation of the ?-opioid receptor by oxycodone and morphine in pain-related brain regions in a bone cancer pain model. Br J Pharmacol. 2013 Jan;168(2):375-88. | ||||
Ref 532470 | A phase 2, placebo-controlled study of the opioid receptor antagonist LY2196044 for the treatment of alcohol dependence. Alcohol Clin Exp Res. 2014 Feb;38(2):511-20. | ||||
Ref 533551 | The relative analgesic efficacy of propiram fumarate, codeine, aspirin, and placebo in post-impaction dental pain. J Clin Pharmacol. 1984 Jan;24(1):35-42. | ||||
Ref 534254 | The mu1 and mu2 opioid receptor binding of ketobemidone, norketobemidone and 3-dimethylamino-1,1-diphenylbutene. Pharmacol Toxicol. 1996 Aug;79(2):103-4. | ||||
Ref 534923 | Functional characterization of a sigma receptor and its gene expression by haloperidol. Nippon Yakurigaku Zasshi. 1999 Jul;114(1):61-8. | ||||
Ref 535895 | Comparison of the effects of dextromethorphan, dextrorphan, and levorphanol on the hypothalamo-pituitary-adrenal axis. J Pharmacol Exp Ther. 2004 May;309(2):515-22. Epub 2004 Jan 23. | ||||
Ref 536285 | Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54. | ||||
Ref 536742 | Effects of opioid receptor gene variation on targeted nalmefene treatment in heavy drinkers. Alcohol Clin Exp Res. 2008 Jul;32(7):1159-66. | ||||
Ref 536928 | Unconditioned behavioral effects of the powerful kappa-opioid hallucinogen salvinorin A in nonhuman primates: fast onset and entry into cerebrospinal fluid. J Pharmacol Exp Ther. 2009 Feb;328(2):588-97. Epub 2008 Nov 10. | ||||
Ref 536942 | Retrospective diagnosis of an adverse drug reaction in a breastfed neonate: liquid chromatography-tandem mass spectrometry quantification of dextropropoxyphene and norpropoxyphene in newborn and maternal hair. J Anal Toxicol. 2008 Nov-Dec;39(9):787-9. | ||||
Ref 537460 | mu-Opioid receptor-stimulated synthesis of reactive oxygen species is mediated via phospholipase D2. J Neurochem. 2009 Jun 10. | ||||
Ref 537855 | Propiram. A review of its pharmacodynamic and pharmacokinetic properties, and clinical use as an analgesic. Drugs. 1993 Sep;46(3):428-45. | ||||
Ref 542100 | (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: 7094). | ||||
Ref 544239 | Current Research on Opioid Receptor Function. Curr Drug Targets. 2012 February; 13(2): 230-246. | ||||
Ref 544320 | Molecular Mechanisms of Opioid Receptor-Dependent Signaling and Behavior. Anesthesiology. 2011 December; 115(6): 1363-1381. | ||||
Ref 547170 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013581) | ||||
Ref 550145 | WO patent application no. 2010,0094,51, Long-acting injectable analgesic formulations for animals. | ||||
Ref 550158 | WO patent application no. 2011,1401,90, Tetrazolones as inhibitors of fatty acid synthase. | ||||
Ref 550829 | US patent application no. 5,874,099, Methods for making immunoisolatary implantable vehicles with a biocompatible jacket and a biocompatible matrix core. |
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