Sigma-1 receptor antagonist 1 |
| رقم الكتالوجGC38038 |
مضاد مستقبل سيجما ‑ 1 (المركب 137) هو مضاد لمستقبلات سيجما -1 (σ1R) قوي وانتقائي ، مع تقارب ارتباط عالٍ بمستقبل σ1R (Ki = 1.06 نانومتر)
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Cas No.: 1639220-19-1
Sample solution is provided at 25 µL, 10mM.
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Sigma?1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma?1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain[1].
Sigma?1 receptor antagonist 1 exhibits a high binding affinity to σ1R receptor (Ki = 1.06 nM) and good σ-1/2 selectivity (1344-fold)[1].
Sigma?1 receptor antagonist 1 exerts dose-dependent antinociceptive effects in mice formalin model and rats CCI models of neuropathic pain[1].
[1]. Lan Y, et al. Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain. J Med Chem. 2014 Dec 26;57(24):10404-23.
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