Tiotidine
Names
Biological Activity
[Description]:
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[1][2].
[Related Catalog]:
[Target]
H2 Receptor:7.3-7.8 (pA2)
H1 receptor:<4.5 (pA2)
H3 Receptor:4.8 (pA2)
[In Vitro]
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[2]. Tiotidine actually behaves as an inverse agonist in U-937 cells, diminishing basal cAMP levels[3].
[References]
Chemical & Physical Properties
[ Density]:
1.5g/cm3
[ Boiling Point ]:
543.6ºC at 760 mmHg
[ Molecular Formula ]:
C10H16N8S2
[ Molecular Weight ]:
312.41800
[ Flash Point ]:
282.5ºC
[ Exact Mass ]:
312.09400
[ PSA ]:
188.54000
[ LogP ]:
1.98258
[ Index of Refraction ]:
1.728