A potent 5-HT2A receptor antagonist (Ki = 6.06 nM for the human receptor); selective for the human 5-HT2A receptor over human 5-HT2B and 5-HT2C and rat 5-HT2B receptors (Kis = 3

MDL 11939 – 5 mg

Brand:
Cayman
CAS:
107703-78-6
Storage:
-20
UN-No:
Non-Hazardous - /

MDL 11939 is a potent, orally bioavailable, and selective antagonist of the serotonin (5-HT) receptor subtype 5-HT2A (Ki = 6.06 nM for the human receptor).{41330} It is selective for the human 5-HT2A receptor over human 5-HT2B and 5-HT2C and rat 5-HT2B receptors (Kis = 3,020, 1,020, and 4,700 nM, respectively), as well as 5-HT1, 5-HT1A, α1- and α2-adrenergic, dopamine D2, muscarinic acetylcholine, histamine, and opiate receptors.{41330,41333} MDL 11939 administered to rats prior to or following learned helplessness-induced stress prevents increases in acoustic startle response.{41331} MDL 11939 (10 mg/kg, i.v.) also has anti-arrhythmic activity in anesthetized dogs following myocardial infarction.{41332}  

 

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Description

A potent 5-HT2A receptor antagonist (Ki = 6.06 nM for the human receptor); selective for the human 5-HT2A receptor over human 5-HT2B and 5-HT2C and rat 5-HT2B receptors (Kis = 3,020, 1,020, and 4,700 nM, respectively); selective for 5-HT2A receptor over 5-HT1, 5-HT1A, α1- and α2-adrenergic, dopamine D2, muscarinic acetylcholine, histamine, and opiate receptors; prevents increases in acoustic startle response when administered prior to or following a stress protocol

Formal name: α-phenyl-1-(2-phenylethyl)-4-piperidinemethanol

Synonyms: 

Molecular weight: 295.4

CAS: 107703-78-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Neuroscience|Behavioral Neuroscience

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