Ispronicline |
رقم الكتالوجGC63548 |
أظهر Ispronicline (TC-1734) ، وهو ناهض جزئي لمستقبلات النيكوتين α4β2 النيكوتين الانتقائي للدماغ (nAChR) ، خصائص تعزز الذاكرة في القوارض وملف تعريف التحمل الجيد
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Cas No.: 252870-53-4
Sample solution is provided at 25 µL, 10mM.
Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR[1][2].
Ispronicline (10-20 mg/kg; s.c.) induces c-Fos expression in selective regions of the rat forebrain[1]. Ispronicline pharmacokinetics (half-life of 2 h in rats) contrasts with the long-lasting improvement of working memory (18 h to 2 d)[2].
[1]. Julie Jacobsen, et al. The α4β2 nicotine acetylcholine receptor agonist ispronicline induces c-Fos expression in selective regions of the rat forebrain. Neurosci Lett. 2012 Apr 25;515(1):7-11.
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