產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 10mg 100mg 1g
CAS	133099-07-7
別名
化學(xué)名	2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide;hydrobromide
分子式	C28H31BrN2O2
分子量	507.48
溶解度	≥ 20.2mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

DarifenacinHBr(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9 [1].

Themuscarinic acetylcholine receptor, also known as cholinergic/acetylcholine receptor M3, or themuscarinic 3, is amuscarinic acetylcholine receptorencoded by the human geneCHRM3. The M3muscarinic receptors are widely expressed in tissues such as smooth muscles, theendocrineglands, the exocrine glands, lungs and pancreas.M3 muscarinic receptor is involved in smooth muscle contraction and increases glandular secretions [2].

In vitro: In a model of the blood-brain barrier (BBB) and blood-ocular barrier (BOB), Darifenacin was a substrate for the P-gp drug efflux transporter. Darifenacin increased ATPase activity in a concentration-dependent manner in P-gp membranes with an ED50 value of 1.6 μM.Darifenacin treatment (100 nM) showed a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6 [3].

In vivo: Darifenacin dose-dependently inhibited the amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55%[1].In female Sprague-Dawley rats, administration of darifenacin (0.1 mg/kg i.v.) reduced bladder afferent activity in Aδ and C fibers. The decrease of afferent spikes in C fibers was more pronounced than that in Aδ fibers [3]. In patients with overactive bladder (OAB), darifenacin at a dose of 7.5 mg and 15 mg exihibited a rapid onset of effect, with significant improvement compared with placebo being seen for most parameters at the first clinic visit (week 2). Darifenacin administration (7.5 mg and 15 mg, daily) reduced the number of incontinence episodes per week from baseline by 67.7% and 72.8% respectively compared with 55.9% with placebo in patients with overactive bladder (OAB). Darifenacin (7.5 mg and 15 mg, daily) also showed significantly superior to placebo for improvements in micturition frequency, bladder capacity, frequency of urgency, number of incontinence episodes and severity of urgency leading to a change in clothing or pads in patients with overactive bladder (OAB) [4].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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