Chemistry:Temanogrel

From HandWiki

Temanogrel (INN, USAN; developmental code name APD791) is a serotonin 5-HT2A receptor antagonist and inverse agonist which is under development for the treatment of myocardial ischemia and Raynaud's disease.[1][2] It was also being developed for arterial thrombosis and acute coronary syndromes, but development for the former use was suspended and development for the latter indication was discontinued.[1] The drug is taken orally.[1] Temanogrel is highly selective for the serotonin 5-HT2A receptor, with more than 2,000-fold selectivity for this receptor over the serotonin 5-HT2B and 5-HT2C receptors and lack of activity at a variety of other G protein-coupled receptors (GPCRs).[3][4] As of September 2022, it is in phase 2 clinical trials for myocardial ischemia and Raynaud's disease.[1]

See also

  • Serotonin 5-HT2A receptor antagonist

References

  1. ↑ 1.0 1.1 1.2 1.3 "Temanogrel". 20 September 2022. https://adisinsight.springer.com/drugs/800026642. 
  2. ↑ "Novel antiplatelet targets in the treatment of acute coronary syndromes". Platelets 32 (1): 15–28. January 2021. doi:10.1080/09537104.2020.1763731. PMID 32529932. "APD791 is a high-affinity, selective 5-HT2A antagonist that improves coronary patency during recurrent thrombosis in preclinical models [83,84]. A phase I study for APD791 was initiated to assess its pharmacokinetics, pharmacodynamics and safety upon co-administration with aspirin and clopidogrel in healthy subjects planned in South Korea. However, the Clinicaltrials.gov record indicated that the trial was terminated on the basis of the sponsor’s decision (Clinicaltrials.gov identifier NCT02419820) in 2019 [85].". 
  3. ↑ "APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology". J Pharmacol Exp Ther 331 (1): 96–103. October 2009. doi:10.1124/jpet.109.153189. PMID 19628629. 
  4. ↑ "Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis". J Med Chem 53 (11): 4412–4421. June 2010. doi:10.1021/jm100044a. PMID 20455563. 



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