A first generation histamine H1 receptor antagonist (Ki = 2.6 nM) that also inhibits muscarinic acetylcholine receptors (Ki = 22 nM); penetrates the CNS

Promethazine (hydrochloride) – 50 g

Brand:
Cayman
CAS:
58-33-3
Storage:
-20
UN-No:
Limited Quantity - 3077 / 9

Promethazine is a first generation histamine H1 receptor antagonist (Ki = 2.6 nM) whose antihistamine activity has been reported in guinea pigs and mice at ED50 values of 0.43 and 5.9 mg/kg, respectively.{23214,25628} Promethazine can penetrate the CNS, depressing central H1 receptor activity, which may relate to its sedative properties, and can also inhibit muscarinic acetylcholine receptors (Ki = 22 nM).{23214,25628} Furthermore, 32 mg/kg promethazine demonstrates antiemetic effects in ferret models of motion sickness or chemotherapy-induced nausea.{26898}  

 

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Description

A first generation histamine H1 receptor antagonist (Ki = 2.6 nM) that also inhibits muscarinic acetylcholine receptors (Ki = 22 nM); penetrates the CNS, depressing central H1 receptor activity, which may relate to its sedative properties

Formal name: N,N,α-trimethyl-10H-phenothiazine-10-ethanamine, monohydrochloride

Synonyms:  Diprazin|Fellozine|Lergigan|Phenergan|Romergan

Molecular weight: 320.9

CAS: 58-33-3

Purity: ≥95%

Formulation: A crystalline solid

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

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