RS 127445 is an orally bioavailable and potent antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.32 nM).{36203} It is selective for 5-HT2B over other 5-HT receptor subtypes (Ki = >3 μM for 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, 5-HT3, 5-HT5, a
库存:
1 mg, 10 mg, 5 mg
供应商:
Cayman
CAS号:
199864-86-3
A 5-HT2B receptor antagonist (Ki = 0.32 nM); selective for 5-HT2B over other 5-HT receptor subtypes (Ki = >3 μM for 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, 5-HT3, 5-HT5, and 5-HT6); reduces contraction of rat isolated stomach fundus (pA2 = 9.5) and 5-HT-induced increases in intracellular calcium (IC50 = 0.04 nM); blocks (±)-α-methyl-5-HT-induced relaxation of isolated rat jugular veins (pA2 = 9.95); reduces peristaltic frequency and fecal output in mice in a dose-dependent manner; reduces basal, but not cocaine-induced, dopamine outflow in the nucleus accumbens of rats; decreases cocaine- or quinpirole-induced hyperlocomotion in rats