Spiroxatrine

Spiroxatrine is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 3 nM) and alpha2-adrenergic receptors (alpha2-ARs, Kis = 28, 1. and 1. nM for alpha2A, alpha2B, and alpha2C, respectively). It is selective for these receptors over 5-HT1D (Ki = 2 µM) and 5-HT1B at 10 µM. Spiroxatrine also induces calcium mobilization in CHO cells expressing the human nociception opioid peptide (NOP) receptor (EC50 = 323 nM). It inhibits decreases in mean arterial pressure induced by urapidil in anesthetized normotensive cats when administered at doses of 3 or 10 nmol/kg. Spiroxatrine (2. and 5 mg/kg) induces catalepsy and catatonia in rats. It enhances reductions in ethanol intake induced by fluoxetine in alcohol-preferring rats. InChI: InChI=1S/C22H25N3O3/c26-21-22(25(16-23-21)17-6-2-1-3-7-17)10-12-24(13-11-22)14-18-15-27-19-8-4-5-9-20(19)28-18/h1-9,18H,10-16H2,(H,23,26) InChIKey: JVGBTTIJPBFLTE-UHFFFAOYSA-N SMILES: O=C(NCN1C2=CC=CC=C2)C31CCN(CC4OC5=C(OC4)C=CC=C5)CC3