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Desfesoterodine

CAS No. : 207679-81-0

MCE 站：Desfesoterodine

产品活性：Desfesoterodine (PNU-200577) 是一种有效的，选择性毒蕈碱受体 (mAChR) 拮抗剂，K_B 和 pA₂ 分别为 0.84 nM 和 9.14。Desfesoterodine 是 Tolterodine (PNU-200583; HY-A0024) 和 Fesoterodine (HY-70053) 的主要药理活性代谢产物。Desfesoterodine 改善大鼠脑梗死诱导膀胱过度活动。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mAChR

In Vitro: 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.

In Vivo: 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) .

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