Mu opioid receptor antagonist 7_product_DataBase

Bioactivity	Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC50 of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder[1].
In Vivo	Mu opioid receptor antagonist 7 (compound 24) (10 mg/kg) 对 µOR 激动剂诱导的镇痛作用具有强烈阻断作用，证明其具有拮抗 µOR 激动剂的能力[1]。Mu opioid receptor antagonist 7 (10 mg/kg，大鼠)可以恢复芬太尼(一种高效的 µOR 激动剂)引起的呼吸抑制[1]。Mu opioid receptor antagonist 7 (10 mg/kg，皮下，大鼠) 可实现 µOR 70% 的受体占据率，从而证明该化合物具有高 CNS 渗透性[1]。
Name	Mu opioid receptor antagonist 7
CAS	2378397-30-7
Formula	C22H27ClN2O2
Molar Mass	386.91
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Nerurkar A, et al. Novel series of tunable µOR modulators with enhanced brain penetration for the treatment of opioid use disorder, pain and neuropsychiatric indications. Bioorg Med Chem Lett. 2023 Aug 15;92:129405.

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