Balovaptan (RG7314) (Synonyms: RG7314) |
رقم الكتالوجGC31295 |
بالوفابتان (RG7314) هو مضاد لمستقبل الڤاسوپريسين 1a (hV1a) المختار والذي يمكن تناوله عن طريق الفم، وهو قادر على اختراق الدماغ بشكل انتقائي. يعد بالوفابتان خافضًا للحصيلة التأثيرية لمستقبل hV1a في الإنسان والفئران، حيث تبلغ قدراته التثبُّطية Kis 1 نانومول/لتر و39 نانومول/لتر على التوالي. كما يستخدَم هذا المضاد في أغراض الأبحاث المعنية بِالْإِصَابَةِ بِطُیورِ الزَّینَة.
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Cas No.: 1228088-30-9
Sample solution is provided at 25 µL, 10mM.
Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for hV1a and mhV1a, and is used for the research of autism. Balovaptan shows >30000-fold selectivity for hV1a over hV2 receptors, 9891-fold selectivity over hOTR (human oxytocin receptor)[1].
[1]. Ratni H, et al. Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. J Med Chem. 2015 Mar 12;58(5):2275-89.
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