产品
编 号:F427577
分子式:C10H16N8S2
分子量:312.42
产品类型
结构图
CAS No: 69014-14-8
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产品详情
生物活性:
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
体外研究:
Tiotidine competitively antagonizes the positive chronotropic action of histamine with an apparent dissociation constant of 30 μM (23-38 μM). Tiotidine abolishes H2-mediated increases in contractile force leaving H2-mediated negative inotropic responses unopposed. The actions of histamine at the A-V node, manifested by lengthening of the P-R interval and A-V block, are attenuated by 2.5 x 10(-7) M Tiotidine.Tiotidine actually behaves as an inverse agonist in U-937 cells, diminishing basal cAMP levels.