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5-hydroxymethyl tolterodine(PNU 200577)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
5-hydroxymethyl tolterodine(PNU 200577)图片
CAS NO:207679-81-0
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)341.49
FormulaC22H31NO2
CAS No.207679-81-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 68 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: 68 mg/mL (199.1 mM)
Other info

Chemical Name: (R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol

InChi Key: DUXZAXCGJSBGDW-HXUWFJFHSA-N

InChi Code: 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

SMILES Code: OC1=CC=C(CO)C=C1[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C

SynonymsDesfesoterodine, PNU-200577; 5-HMT, 5-HM; PNU200577; PNU 200577
实验参考方法
In Vitro

In vitro activity: 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. 5-hydroxymethyl tolterodine has a similar pharmacological profile with tolterodine. Intravenous infusion of 5-hydroxymethyl tolterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure.

In Vivo5-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.
Animal modelMale guinea-pigs
Formulation & DosageDissolved in saline; 2 nmol/kg -203 nmol/kg; i.v. injection
References

Pharmacol Toxicol. 1997 Oct;81(4):169-72.