BAY38-7271

简介生物活性靶点体外研究体内研究 BAY38-7271 试剂级价格

BAY38-7271

CAS号:212188-60-8
英文名:(R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate
中文名:BAY38-7271
CBNumber:CB22502634
分子式:C20H21F3O5S
分子量:430.4379496
MOL File:212188-60-8.mol

BAY38-7271化学性质

沸点 :527.2±50.0 °C(Predicted)
密度 :1.350±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
酸度系数(pKa) :14.81±0.10(Predicted)

BAY38-7271性质、用途与生产工艺

简介 bay38 -7271 (KN 38-7271)是由化学家Wayne E. Kenney最初合成的一种药物，是拜耳公司开发的一种大麻素受体激动剂。它具有镇痛和神经保护作用，并被用于科学研究，建议用于治疗创伤性脑损伤。在动物实验中，它是一种完全的激动剂，与CP 55,940的效力差不多，并且对CB1和CB2受体都有相当高的亲和力，在CB1处的Ki值为2.91nM，在CB2处为4.24nM。它已经被授权给KeyNeurotek制药公司进行临床开发，并在2008年进入II期临床试验，但它的开发似乎已经停止。
生物活性 BAY 38-7271 是一个选择性、高效的大麻素受体 CB1/CB2 激动剂，对人重组 CB1 和 CB2 作用的 Ki 值分别为 1.85 nM 和 5.96 nM。BAY 38-7271 具有很强的神经保护特性。
靶点

CB1

1.85 nM (Ki)

CB2

5.96 nM (Ki)
体外研究

BAY 38-7271 shows only minor interactions at the micromolar range with other binding sites such as adenosine A ₃ receptor (IC ₅₀ = 7.5 μM), peripheral GABA _A benzodiazepine receptor (IC ₅₀ = 971 nM), melatonin ML ₁ receptor (IC ₅₀ = 3.3 μM), and at the monoamine transporter (IC ₅₀ = 1.7 μM).

体内研究

BAY 38-7271 (Ed ₅₀ = 0.02 mg/kg; i.v. and 0.5 mg/kg; i.p.) induces a potent and dose-de-pendent reduction in core body temperature.
BAY 38-7271 has low physical dependence liability and is not essentially different from that of other cannabinoid CB ₁ receptor agonists.
BAY 38-7271 (1-1000 ng/kg/h; i.v. infusion; for 4 hours) shows neuroprotective efficacy in the rat SDH model.
BAY 38-7271 also has neuroprotective efficacy in models of transient and permanent occlusion of the middle cerebral artery and brain edema models.

Animal Model:	Wistar rat ,TBI rat models (acute subdural hematoma, SDH)
Dosage:	1 ng/kg/h, 10 ng/kg/h, 100 ng/kg/h, 1000 ng/kg/h
Administration:	Intravenous infusion, for 4 hours
Result:	Reduced the mean infarct volume.