Target Information

Target General Infomation
Target ID
T86704
Target Name
Phosphodiesterase (PDE) 3
Target Type
Successful
Disease Allergy [ICD9: 995.3; ICD10: T78.4]
Arteriosclerosis [ICD9: 440; ICD10: I70]
Asthma [ICD10: J45]
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4]
Cough [ICD9: 786.2; ICD10: R05]
Congestive heart failure [ICD9: 428; ICD10: I50]
Cardiotonic [ICD10: I50]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Cardiovascular disorder [ICD10: I00-I99]
Heart failure [ICD9: 428; ICD10: I50]
Intermittent claudication [ICD9: 440.21; ICD10: I73.9]
Septic shock [ICD9: 785.52; ICD10: A41.9]
BioChemical Class
Hydrolases (EC:3)
EC Number
EC 3.1.4.17
Drugs and Mode of Action
Drug(s) Cilostazol Drug Info Approved Intermittent claudication [536186], [542155]
Enoximone Drug Info Approved Congestive heart failure [536361]
Inamrinone Lactate Drug Info Approved Cardiotonic [551871]
Milrinone Drug Info Approved Congestive heart failure [468278], [536361]
Oxtriphylline Drug Info Approved Cough [538364]
K-134 Drug Info Phase 2 Arteriosclerosis [522473]
Org-30029 Drug Info Phase 2 Heart failure [534035]
RPL-554 Drug Info Phase 2 Allergic rhinitis [525173]
Tipelukast Drug Info Phase 2 Asthma [525273]
349U85.HCL Drug Info Phase 1 Cardiovascular disorder [526644], [533980]
SDZ-MKS-492 Drug Info Phase 1 Asthma [533607], [533957]
NSP-805 Drug Info Discontinued in Phase 2 Heart failure [545097]
OPC-8490 Drug Info Discontinued in Phase 2 Cardiovascular disorder [544607]
Org-9731 Drug Info Discontinued in Phase 2 Heart failure [545949]
Pumafentrine Drug Info Discontinued in Phase 2 Asthma [547102]
Tolafentrine Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [545580]
NIP-520 Drug Info Discontinued in Phase 1 Asthma [547049]
R 80122 Drug Info Discontinued in Phase 1 Cardiovascular disorder [544843]
Benafentrine dimaleate Drug Info Terminated Septic shock [544550]
Org-9935 Drug Info Terminated Asthma [546889]
SDZ-ISQ-844 Drug Info Terminated Asthma [545901]
Siguazodan Drug Info Terminated Allergy [544635]
UD-CG-212 Drug Info Terminated Heart failure [526768]
ZARDAVERINE Drug Info Terminated Chronic obstructive pulmonary disease [544526]
Modulator 349U85.HCL Drug Info [533980]
Benafentrine dimaleate Drug Info [533628]
Cilostazol Drug Info [556264]
Enoximone Drug Info
Inamrinone Lactate Drug Info
K-134 Drug Info [531714], [544269]
Milrinone Drug Info [556264]
NIP-520 Drug Info [1572591]
NSP-805 Drug Info
OPC-8490 Drug Info
Org-30029 Drug Info [534035]
Org-9731 Drug Info [533708]
Org-9935 Drug Info
Oxtriphylline Drug Info [556264]
Pumafentrine Drug Info
R 80122 Drug Info [535804]
RPL-554 Drug Info
SDZ-ISQ-844 Drug Info [533858]
SDZ-MKS-492 Drug Info [533607], [533957]
Siguazodan Drug Info
Tipelukast Drug Info
Tolafentrine Drug Info
UD-CG-212 Drug Info
ZARDAVERINE Drug Info
References
Ref 468278(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: 5225).
Ref 522473ClinicalTrials.gov (NCT00783081) Safety and Efficacy of K-134 for the Treatment of Intermittent Claudication. U.S. National Institutes of Health.
Ref 525173ClinicalTrials.gov (NCT02427165) Comparison of RPL554 With Placebo and Salbutamol in Asthmatic Patients. U.S. National Institutes of Health.
Ref 525273ClinicalTrials.gov (NCT02503657) Safety and Tolerability Study in Subjects With Idiopathic Pulmonary Fibrosis (IPF).
Ref 526644Cardiovascular pharmacology of the vasodilator-cardiotonic agent, 349U85. J Cardiovasc Pharmacol. 1992 Oct;20(4):579-89.
Ref 526768Electrophysiological actions of the pimobendan metabolite, UD-CG 212 Cl, in guinea pig myocardium. J Pharmacol Exp Ther. 1992 Jan;260(1):58-63.
Ref 533607Effects of MKS-492 on antigen-induced bronchoconstriction and allergic reaction in guinea pigs and rats. Jpn J Pharmacol. 1993 Dec;63(4):405-13.
Ref 533957Effects of a cyclic nucleotide phosphodiesterase isoenzyme type III inhibitor, SDZ MKS 492 on airway responsiveness in beagles. Arerugi. 1993 Aug;42(8):920-5.
Ref 533980Pharmacokinetics and pharmacodynamics of a new cardiotonic vasodilator agent, 349U85, in normal subjects. Clin Pharmacol Ther. 1994 Jan;55(1):55-63.
Ref 534035Effects of the positive inotropic agent Org 30029 on developed force and aequorin light transients in intact canine ventricular myocardium. Circ Res. 1993 Mar;72(3):597-606.
Ref 536186Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 538364FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 086742.
Ref 542155(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: 7148).
Ref 544526Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000057)
Ref 544550Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000110)
Ref 544607Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000283)
Ref 544635Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000375)
Ref 544843Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001304)
Ref 545097Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002110)
Ref 545580Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003767)
Ref 545901Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005292)
Ref 545949Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005468)
Ref 546889Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010891)
Ref 547049Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012535)
Ref 547102Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013080)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 531714A phase II dose-ranging study of the phosphodiesterase inhibitor K-134 in patients with peripheral artery disease and claudication. J Vasc Surg. 2012 Feb;55(2):381-389.e1.
Ref 533607Effects of MKS-492 on antigen-induced bronchoconstriction and allergic reaction in guinea pigs and rats. Jpn J Pharmacol. 1993 Dec;63(4):405-13.
Ref 533628Studies on anti-allergic action of AH 21-132, a novel isozyme-selective phosphodiesterase inhibitor in airways. Jpn J Pharmacol. 1995 Feb;67(2):149-56.
Ref 533708The effects of various drugs on the myocardial inotropic response. Gen Pharmacol. 1995 Jan;26(1):1-31.
Ref 533858Effects of inhaled SDZ ISQ 844, a cyclic nucleotide phosphodiesterase isoenzyme type III/IV inhibitor, on airway responsiveness in beagles. Arerugi. 1994 Apr;43(4):551-6.
Ref 533957Effects of a cyclic nucleotide phosphodiesterase isoenzyme type III inhibitor, SDZ MKS 492 on airway responsiveness in beagles. Arerugi. 1993 Aug;42(8):920-5.
Ref 533980Pharmacokinetics and pharmacodynamics of a new cardiotonic vasodilator agent, 349U85, in normal subjects. Clin Pharmacol Ther. 1994 Jan;55(1):55-63.
Ref 534035Effects of the positive inotropic agent Org 30029 on developed force and aequorin light transients in intact canine ventricular myocardium. Circ Res. 1993 Mar;72(3):597-606.
Ref 535804Inhibition of human cardiac cyclic AMP-phosphodiesterases by R 80122, a new selective cyclic AMP-phosphodiesterase III inhibitor: a comparison with other cardiotonic compounds. J Pharmacol Exp Ther. 1992 Oct;263(1):6-14.
Ref 544269K-134, a Phosphodiesterase 3 Inhibitor, Prevents Brain Damage by Inhibiting Thrombus Formation in a Rat Cerebral Infarction Model. PLoS One. 2012; 7(10): e46432.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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