Desfesoterodine

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

5-羟甲基托特罗定 (PNU 200577) 是一种新型毒蕈碱受体拮抗剂，Kb 为 0.84 nM。

5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

In vitro, Desfesoterodine preventes carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In radioligand binding studies carries out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, Desfesoterodine is not selective for any muscarinic receptor subtype.

Desfesoterodine (PNU-200577; 5-Hydroxymethyl Tolterodine; 0.1 and 1 mg/kg; IV) significantly increases bladder compliance after moderate and high doses. In vivo, Desfesoterodine is 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) . Animal Model:Female Sprague Dawley rats at ages 9 to 11 weeks weighing 180 to 250 gDosage:0.1 and 1 mg/kg Administration:IV; single imidafenacin administration Result:Significantly increased bladder compliance after moderate and high doses.

PNU-200577 | (R)-5-Hydroxymethyl Tolterodine

Metabolic Enzyme/Protease

Phosphatase

mAChR

Neurological Disease

——

207679-81-0

341.49

C22H31NO2

>98% (HPLC)

DMSO : ≥ 100 mg/mL; 292.83 mM

CC(C)N(CC[C@H](C1=CC=CC=C1)C1=C(O)C=CC(CO)=C1)C(C)C

——

(-20℃)

With Ice Pack

≥ 2 years