MOR modulator-1

CAS: 2976336-81-7 F: C24H27N3O4S W: 453.55

MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits impr

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Bioactivity	MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with Ki of 0.25, 41.1, 1.30 nM, respectively[1]
Invitro	MOR modulator-1 在 MOR 处表现出亚纳摩尔结合亲和力，在 KOR (kappa 阿片受体) 处表现出单位纳摩尔结合亲和力，对 DOR (delta 阿片受体) 的结合亲和力要低得多，在 MOR处比 DOR 保持了合理的选择性[1]。MOR modulator-1 显示出最高的 δ/μ 选择性，比 NAT 高约 3 倍[1]。MOR modulator-1 与羧酰胺连接子 μ，δ，γ 连接，Ki 分别为 0.25, 41.1, 1.30 nM[1]。MOR modulator-1 与 MOR [35S]GTPγS 结合，EC50 为 2.16 nM [1]。MOR modulator-1 与 KOR [35S]GTPγS，KOR [35S]GTPγS 结合的 EC50 为 3.83 和23.6 nM [1]。MOR modulator-1 的效价从纳摩尔到亚纳摩尔不等，效价相当低，%Emax 值为 11.3 sup[1]/supMOR modulator-1 显著拮抗 DAMGO 诱导的 Gαqi5 转染的 mMORCHO 细胞内钙离子升高[1]。MOR modulator-1 在 Gαqi5 转染的 mMORCHO 细胞中抑制钙离子，IC50 为5.64 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> MOR modulator-1 相关抗体:
In Vivo	MOR modulator-1 (10 mg/kg, warm-water tail immersion, 20 min) 是这一系列 NAT 类似物中拮抗吗啡介导的镇痛作用的最有效药物[1]。MOR modulator-1 (10 mg/kg, warm-water tail immersion, 20 min) 的 AD50 值为 0.043 mg/kg，是 NAT 的 10 倍[1]。MOR modulator-1 (10 mg/kg, warm-water tail immersion, 20 min) 是所有 MOR 调节剂中最活跃的基于环氧吗啡喃的分子[1]。MOR modulator-1 (0.05-10 mg/kg, s.c., 20 min) 在所有测试剂量下均比 1 mg/kg naloxone (NLX) 表现出更少的湿狗抖动和爪子震颤，即使在最高剂量分别为 5 mg/kg 和 10mg/kg 时也是如此[1]。MOR modulator-1 (5 mg/kg, s.c., 20min) 在湿狗摇晃，跳跃和爪子震颤中的平均数值分别为 9.8，36.8 和 30.2[1]。MOR modulator-1 在给药后 5，10 和 30 min，脑内浓度分别为 0.187，0.235，和 0.264 μg/g，显示 MOR modulator-1 在皮下给药后迅速渗透到大脑中，并在大脑中停留了很长时间[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
CAS	2976336-81-7
Formula	C24H27N3O4S
Molar Mass	453.55
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]. Huang B, et al. Discovery of 6α-Thiazolylcarboxamidonaltrexamine Derivative (NTZ) as a Potent and Central Nervous System Penetrant Opioid Receptor Modulator with Drug-like Properties for Potential Treatment of Opioid Use Disorder. ACS Pharmacol Transl Sci. 2024 Dec 5;7(12):4165-4182.

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