Temanogrel

Temanogrel (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code name APD791) is a serotonin 5-HT_2A 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-HT_2A receptor, with more than 2,000-fold selectivity for this receptor over the serotonin 5-HT_2B and 5-HT_2C 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]

Other namesAPD-791; APD791

Routes of
administrationOral^[1]

Drug classSerotonin 5-HT_2A receptor antagonist

CAS Number

• 887936-68-7

Quick facts Clinical data, Other names ...

Temanogrel

Clinical data
Other names	APD-791; APD791
Routes of administration	Oral[1]
Drug class	Serotonin 5-HT2A receptor antagonist
Identifiers
IUPAC name 3-methoxy-N-[3-(2-methylpyrazol-3-yl)-4-(2-morpholin-4-ylethoxy)phenyl]benzamide
CAS Number	887936-68-7
PubChem CID	11604525
ChemSpider	9779281
UNII	F42Z27575A
KEGG	D09976
ChEBI	CHEBI:177604
ChEMBL	ChEMBL1084617
CompTox Dashboard (EPA)	DTXSID70237321
Chemical and physical data
Formula	C24H28N4O4
Molar mass	436.512 g·mol−1
3D model (JSmol)	Interactive image
SMILES CN1C(=CC=N1)C2=C(C=CC(=C2)NC(=O)C3=CC(=CC=C3)OC)OCCN4CCOCC4
InChI 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

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