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

RS 127445 – 1 mg

Brand:
Cayman
CAS:
199864-87-4
Storage:
-20
UN-No:
Non-Hazardous - /

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, and 5-HT6). RS 127445 reduces contraction of rat isolated stomach fundus (pA2 = 9.5) and lowers intracellular increases in calcium (IC50 = 0.04 nM) induced by 5-HT (Item No. 14332). It also blocks (±)-α-methyl-5-HT-induced relaxation of isolated rat jugular veins (pA2 = 9.95). RS 127445 (1-30 mg/kg) reduces peristaltic frequency and fecal output in mice in a dose-dependent manner.{36204} Systemic administration of RS 127445 (0.16 mg/kg) reduces basal, but not cocaine-induced, dopamine outflow in the nucleus accumbens of rats and decreases hyperlocomotion induced by cocaine (Item Nos. ISO60176 | 16186 | 22165) or quinpirole.{36202}  

 

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Description

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

Formal name: 4-(4-fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine

Synonyms: 

Molecular weight: 281.3

CAS: 199864-87-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

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