产品名称

英文名称：5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)

同义词

Desfesoterodine、NCGC00346585-01、(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol、AMY14591、Benzenemethanol, 3-((1R)-3-(bis(1-methylethyl)amino)-1-phenylpropyl)-4-hydroxy-、HY-76569、(R)-2-[3-(Diisopropylamino)-1-phenylpropyl]-4-(hydroxymet、地非索罗定

产品性质

CAS编号：207679-81-0

分子式：C22H31NO2

分子量：341.49

PubChem编号：9819382

别名：地非索罗定

英文别名：Desfesoterodine|NCGC00346585-01|(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol|AMY14591|Benzenemethanol, 3-((1R)-3-(bis(1-methylethyl)amino)-1-phenylpropyl)-4-hydroxy-|HY-76569|(R)-2-[3-(Diisopropylamino)-1-phenylpropyl]-4-(hydroxymet

规格或纯度：≥99%

英文名称：5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)

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.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍5-hydroxymethyl Tolterodine是一种蕈毒碱受体竞争性拮抗剂

IUPAC Name：2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenol

INCHI：InChI=1S/C22H31NO2/c1-16(2)23(17(3)4)13-12-20(19-8-6-5-7-9-19)21-14-18(15-24)10-11-22(21)25/h5-11,14,16-17,20,24-25H,12-13,15H2,1-4H3/t20-/m1/s1

InChi Key：DUXZAXCGJSBGDW-HXUWFJFHSA-N

Canonical SMILES：CC(C)N(CCC(C1=CC=CC=C1)C2=C(C=CC(=C2)CO)O)C(C)C

Isomeric SMILES：CC(C)N(CC[C@H](C1=CC=CC=C1)C2=C(C=CC(=C2)CO)O)C(C)C

PubChem CID：9819382

溶解性：68 mg/mL in DMSO or Ethanol，不溶于水

象形图：

信号词：Danger

危险声明：H319 Causes serious eye irritationH301 Toxic if swallowedH302 Harmful if swallowedH317 May cause an allergic skin reaction

预防措施声明：P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P270,P272,P333+P313,P362+P364,P330,P264+P265,P301+P316,P301+P317,P337+P317

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