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Temanogrel

From Wikipedia, the free encyclopedia
Pharmaceutical compound
Temanogrel
Clinical data
Other namesAPD-791; APD791
Routes of
administration		Oral[1]
Drug classSerotonin 5-HT2A receptor antagonist
Identifiers
  • 3-methoxy-N-[3-(2-methylpyrazol-3-yl)-4-(2-morpholin-4-ylethoxy)phenyl]benzamide
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC24H28N4O4
Molar mass436.512 g·mol−1
3D model (JSmol)
  • CN1C(=CC=N1)C2=C(C=CC(=C2)NC(=O)C3=CC(=CC=C3)OC)OCCN4CCOCC4
  • InChI=1S/C24H28N4O4/c1-27-22(8-9-25-27)21-17-19(26-24(29)18-4-3-5-20(16-18)30-2)6-7-23(21)32-15-12-28-10-13-31-14-11-28/h3-9,16-17H,10-15H2,1-2H3,(H,26,29)
  • Key:ZEOQUKRCASTCFR-UHFFFAOYSA-N

Temanogrel (INNTooltip International Nonproprietary Name,USANTooltip United States Adopted Name; developmental code nameAPD791) is aserotonin5-HT2A receptorantagonist andinverse agonist which is under development for the treatment ofmyocardial ischemia andRaynaud's disease.[1][2] It was also being developed forarterial thrombosis andacute coronary syndromes, but development for the former use was suspended and development for the latter indication was discontinued.[1] The drug is takenorally.[1] Temanogrel is highlyselective for the serotonin 5-HT2A receptor, with more than 2,000-fold selectivity for this receptor over the serotonin5-HT2B and5-HT2C receptors and lack of activity at a variety of otherG protein-coupled receptors (GPCRs).[3][4] As of September 2022, it is inphase 2clinical trials for myocardial ischemia and Raynaud's disease.[1]

See also

[edit]

References

[edit]
  1. ^abcde"Temanogrel".AdisInsight. 20 September 2022. Retrieved16 January 2026.
  2. ^Alenazy FO, Thomas MR (January 2021). "Novel antiplatelet targets in the treatment of acute coronary syndromes".Platelets.32 (1):15–28.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. ^Adams JW, Ramirez J, Shi Y, Thomsen W, Frazer J, Morgan M, Edwards JE, Chen W, Teegarden BR, Xiong Y, Al-Shamma H, Behan DP, Connolly DT (October 2009). "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.doi:10.1124/jpet.109.153189.PMID 19628629.
  4. ^Xiong Y, Teegarden BR, Choi JS, Strah-Pleynet S, Decaire M, Jayakumar H, Dosa PI, Casper MD, Pham L, Feichtinger K, Ullman B, Adams J, Yuskin D, Frazer J, Morgan M, Sadeque A, Chen W, Webb RR, Connolly DT, Semple G, Al-Shamma H (June 2010). "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.doi:10.1021/jm100044a.PMID 20455563.
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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