A-317920


CAS No. : 360551-59-3

360551-59-3
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Cat. No. : HY-122171
M.Wt: 453.53
Formula: C25H31N3O5
Purity: >98 %
Solubility:
Introduction of 360551-59-3 :

A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade[1]. In Vitro:A-317920 is a potent antagonist at rat H3R in reversing R-α-methylhistamine [(R)-α-MeHA] inhibition of Forskolin-stimulated cAMP formation (pKb value of 9.1) but a weak antagonist at human H3R in cyclase (pKb value of 6.3) and calcium mobilization (pKb value of 7.3) assays in cells co-expressing Galphaqi5-protein[1].
A-317920 potently antagonizes native H3Rs by blocking histamine inhibition of potassium-evoked [3H]histamine release from rat brain cortical synaptosomes (pKb value of 9.3) and (R)-α-MeHA reversal of electric field-stimulated guinea pig ileum contractions (pA2 value of 8.3)[1].
In Vivo:A-317920 (3-10 mg/kg; s.c; 30 min prior to training; for a total of five trials) significantly improves in the avoidance test in spontaneously hypertensive rat (SHR) pups[1].

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