An active metabolite of tolterodine and fesoterodine; inhibits M1-5 muscarinic receptors (Kis = 2.3

5-hydroxymethyl Tolterodine (formate) – 1 mg

Brand:
Cayman
CAS:
380636-49-7
Storage:
-20
UN-No:
Non-Hazardous - /

5-hydroxymethyl Tolterodine is an active metabolite of the muscarinic acetylcholine receptor antagonists tolterodine (Item No. 15027) and fesoterodine (Item No. 23777).{47319} It is formed from tolterodine by the cytochrome P450 (CYP) isoform CYP2D6 and from fesoterodine by plasma esterases.{47320,47319} 5-hydroxymethyl Tolterodine inhibits M1-5 muscarinic receptors with Ki values of 2.3, 2, 2.5, 2.8, and 2.9 nM, respectively, for the human receptors expressed in CHO cells.{47321} It selectively inhibits acetylcholine-induced bladder contraction over electrically induced salivation in anesthetized cats (ID50s = 15 and 40 nmol/kg, respectively).  

 

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SKU: 27833 - 1 mg Category:

Description

An active metabolite of tolterodine and fesoterodine; inhibits M1-5 muscarinic receptors (Kis = 2.3, 2, 2.5, 2.8, and 2.9 nM, respectively); selectively inhibits acetylcholine-induced bladder contraction over electrically induced salivation in anesthetized cats (ID50s = 15 and 40 nmol/kg, respectively)

Formal name: formic acid, compd. with 3-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxybenzenemethanol

Synonyms:  5-HMT|Desfesoterodine|PNU 200577

Molecular weight: 387.5

CAS: 380636-49-7

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Toxicology|Drug Metabolism|Cytochrome P450||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

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