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Tolterodine tartrate(Kabi-2234 PNU-200583E)
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。
Tolterodine tartrate(Kabi-2234 PNU-200583E)图片
CAS NO:124937-52-6
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)475.57
FormulaC22H31NO.C4H6O6
CAS No.124937-52-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 95 mg/mL (199.8 mM)
Water: 17 mg/mL (35.7 mM)
Ethanol: 6 mg/mL (12.6 mM)
Other info

Chemical Name: (R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-methylphenol (2R,3R)-2,3-dihydroxysuccinate

InChi Key: TWHNMSJGYKMTRB-KXYUELECSA-N

InChi Code: InChI=1S/C22H31NO.C4H6O6/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24;5-1(3(7)8)2(6)4(9)10/h6-12,15-17,20,24H,13-14H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)/t20-;1-,2-/m11/s1

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

SynonymsPNU-200583 E; PNU200583E; Tolterodine tartrate; PNU-200583E; PNU 200583E; Detrol LA; Detrusitol.
实验参考方法
In Vitro

In vitro activity: Tolterodine has a high affinity and specificity for muscarinic receptors in vitro and it exhibits selectivity for the urinary bladder over salivary glands in vivo. Tolterodine is a new muscarinic receptor antagonist intended for the treatment of urinary urge incontinence and other symptoms related to an overactive bladder. Tolterodine effectively inhibits carbachol-induced contractions of isolated strips of urinary bladder from guinea pigs in a concentration-dependent, competitive manner. Tolterodine binds with high affinity to muscarinic receptors in urinary bladder (Ki 2.7 nM), heart (Ki 1.6 nM), cerebral cortex (Ki 0.75 nM) and parotid gland (Ki 4.8 nM) from guinea pigs and in urinary bladder from humans (Ki 3.3 nM).

In VivoTolterodine (1 mg/kg, i.v.) is significantly more potent in inhibiting acetylcholine-induced urinary bladder contraction than electrically-induced salivation in the anaesthetised cat. Tolterodine administered intravenously increases the mean micturition interval, bladder capacity and micturition volume in normal rats and resiniferatoxin treated rats. Tolterodine (2 nM/kg) significantly increases bladder capacity (BC) in saline vehicle- cerebral infarct rats without increasing residual volume but it has no effects on BC in resiniferatoxin- cerebral infarct rats. Tolterodine tartrate (0.1 and 1.0 mg/kg) significantly decreases the number and amplitude of non-voiding contractions by 38-74% and 29-44%, respectively, and increases bladder capacity by 19-51% in female rats with bladder outlet obstruction.
Animal modelCat
Formulation & Dosage1 mg/kg, i.v.
References

Eur J Pharmacol. 1997 May 30;327(2-3):195-207; J Urol. 2007 Jul;178(1):326-31.