Temanogrel

SKU: orb1307683

Description

Temanogrel (APD791) is a potent and selective 5-HT2A receptor antagonist with a Ki of 4.9 nM. This small molecule is a valuable research tool for investigating serotonin signaling in cardiovascular and neurological studies, applicable in both in vitro and in vivo experimental models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 887936-68-7
• MW: 436.5
• Purity: 99.24% (May vary between batches)
• Formula: C₂₄H₂₈N₄O₄
• SMILES: COc1cccc(c1)C(=O)Nc1ccc(OCCN2CCOCC2)c(c1)-c1ccnn1C
• Target: 5-HT Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.45 mM);DMSO:125 mg/mL (286.37 mM)

Bioactivity

• Target IC50:
  5-HT2A:4.9 nM (ki)
• In Vivo:
  Plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6, and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h, and 2.25 h after the start of treatment in dogs assigned to receive Temanogrel. There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment .
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• In Vitro:
  Temanogrel inhibits inositol phosphate accumulation (IC50: 5.2 nM). Temanogrel shows effective inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively). Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis (IC50: 13±7 nM) .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

APD 791, APD791, APD-791, 5-HT Receptor, 5-HT2A, 5-HT2A Receptor, 5-hydroxytryptamine Receptor, 5HTReceptor, 5HT Receptor, Inhibitor, inhibit, Serotonin Receptor, Temanogrel

Compound Identifiers

PubChem CID

11604525