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Desfesoterodine Sale

(Synonyms: (R)-5-羟甲基托特罗定; PNU-200577; 5-Hydroxymethyl Tolterodine) 目录号 : GC35842

5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM,Desfesoterodine) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

Desfesoterodine Chemical Structure

Cas No.:207679-81-0

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10mM (in 1mL DMSO)
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Sample solution is provided at 25 µL, 10mM.

Description

5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM,Desfesoterodine) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

5-hydroxymethyl tolterodine is a major pharmacologically active metabolite of tolterodine. 5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips. 5-hydroxymethyl tolterodine antagotizes muscarinic receptors with a pA2 of 9.1. 5-hydroxymethyl tolterodine causes a concentration-dependent inhibition of (-)3 H-QNB binding in homogenates of guinea-pig urinary bladder, parotid gland, heart and cerebral cortex. [1] 5-hydroxymethyl tolterodine has a similar pharmacological profile with tolterodine. [2] Intravenous infusion of 5-hydroxymethyl tolterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure. [3]

5-hydroxymethyl tolterodine is significantly more potent at inhibiting acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50 15 and 40 nmol/kg, respectively. 5-hydroxymethyl tolterodine is three times more potent at the urinary bladder compared to the salivary gland. [1]

[1] Nilvebrant L, et al. Pharmacol Toxicol, 1997, 81(4), 169-172. [2] Nilvebrant L, et al. Life Sci, 1997, 60(13-14), 1129-1136. [3] Modiri AR, et al. Urology, 2002, 59(6), 963-968.

化学性质

Cas No. 207679-81-0 SDF
别名 (R)-5-羟甲基托特罗定; PNU-200577; 5-Hydroxymethyl Tolterodine
Canonical SMILES OC1=C(C=C(CO)C=C1)[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C
分子式 C22H31NO2 分子量 341.49
溶解度 DMSO: ≥ 100 mg/mL (292.83 mM) 储存条件 Store at -20°C
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1 mM 2.9283 mL 14.6417 mL 29.2834 mL
5 mM 0.5857 mL 2.9283 mL 5.8567 mL
10 mM 0.2928 mL 1.4642 mL 2.9283 mL
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