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(R)-5-羟甲基托特罗定

5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) （订货以英文为准）

编号：H129983
CAS号：207679-81-0
分子式：C22H31NO2
分子量：341.49
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H129983-1mg 阿拉丁 1mg ¥204.90
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H129983-10mg 阿拉丁 10mg ¥865.90
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H129983-50mg 阿拉丁 50mg ¥3007.90
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H129983-5mg 阿拉丁 5mg ¥617.90
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H129983-250mg 阿拉丁 250mg ¥7364.90
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H129983-100mg 阿拉丁 100mg ¥4212.90
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H129983-500mg 阿拉丁 500mg ¥10299.90
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产品名称 5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)
中文名称 (R)-5-羟甲基托特罗定
CAS号 207679-81-0
分子式（M.F.） C22H31NO2
分子量（M.W.） 341.49
储存条件 -20°C储存
溶解性DMSO 68 mg/mL Water <1 mg/mL Ethanol 68 mg/mL
存贮条件储存温度-20°C
备注5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.
生化机理(R)-5-Hydroxymethyl Tolterodine is a potent and selective muscarinic receptor antagonist with a Kb and a pA2 of 0.84 nM and 9.14, respectively. (R)-5-Hydroxymethyl Tolterodine is a major pharmacologically active metabolite of tolterodine. In vitro, (R)-5-Hydroxymethyl Tolterodine prevented carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In vivo, (R)-5-Hydroxymethyl Tolterodine was significantly more potent at suppressing acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50=15 and 40 nmol/kg, respectively). In radioligand binding studies carried out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, (R)-5-Hydroxymethyl Tolterodine was not selective for any muscarinic receptor subtype. Thus, (R)-5-Hydroxymethyl Tolterodine is similar to tolterodine in terms of antimuscarinic potency, functional selectivity for the urinary bladder in vivo and absence of selectivity for muscarinic receptor subtypes in vitro. The results of this study clearly indicate that (R)-5-Hydroxymethyl Tolterodine contributes to the therapeutic action of tolterodine, in view of its high antimuscarinic potency, similar serum concentration and lower degree of protein binding.
别名(R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol;(R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol
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