Tolterodine tartrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tolterodine Tartrate（PNU-200583E；Kabi-2234）是一种有效的毒蕈碱受体拮抗剂，在体内对膀胱的选择性优于对唾液腺的选择性。

Tolterodine Tartrate(PNU-200583E; Kabi-2234) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo.(In Vitro):Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors.(In Vivo):Tolterodine was extensively metabolized in vivo. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased.

Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM).The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors.

Tolterodine was extensively metabolized in vivo.In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased.

PNU-200583E | Kabi-2234

Endocrinology/Hormones

AChR

mAChR

Neurological Disease

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124937-52-6

475.58

C22H31NO·C4H6O6

>98% (HPLC)

Ethanol: 6 mg/mL (12.61 mM); Water: 17 mg/mL (35.74 mM); DMSO: 95 mg/mL (199.76 mM)

CC1=CC(=C(C=C1)O)[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O

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(-20℃)

With Ice Pack

≥ 2 years