83812-65-1
Chemical Structure
ICI 147798
- CAS No.: 83812-65-1
- Formula:C24H30ClN7O4
- Molecular Weight:515.99
InChIKey: GUMKBOVHSJWJQS-UHFFFAOYSA-N
SMILES: O=C(C1=NC(Cl)=C(N)N=C1N)NC(C)(C)C(NCCNCC(COC2=CC=CC3=C2C=CC=C3)O)=O
Biological Activity: ICI 147798 is an orally effective β-adrenoceptor antagonist with a pKB of 9.1 (in guinea pig right atrium) and 8.8 (in guinea pig trachea). ICI 147798 acts as a diuretic and intraocular pressure-lowering agent. ICI 147798 blocks β-adrenoceptors, inhibits isoproterenol-induced tachycardia and vasodepressor responses, exhibits slowly dissociating, insurmountable antagonism against β1-adrenoceptors, and shows surmountable competitive antagonism against β2-adrenoceptors. ICI 147798 induces natriuresis and kaliuresis, inhibits sodium transport, and reduces intraocular pressure[1][2][3].
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ICI 147798 | ICI 147798 is an orally effective β-adrenoceptor antagonist with a pKB of 9.1 (in guinea pig right atrium) and 8.8 (in guinea pig trachea). ICI 147798 acts as a diuretic and intraocular pressure-lowering agent. ICI 147798 blocks β-adrenoceptors, inhibits isoproterenol-induced tachycardia and vasodepressor responses, exhibits slowly dissociating, insurmountable antagonism against β1-adrenoceptors, and shows surmountable competitive antagonism against β2-adrenoceptors. ICI 147798 induces natriuresis and kaliuresis, inhibits sodium transport, and reduces intraocular pressure. | |||||||||||||||||||||
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- [1]. Kau ST, et al. ICI 147,798: a novel diuretic agent with beta adrenoceptor blocking activity. J Pharmacol Exp Ther. 1987;242(3):818-826. [Content Brief]
- [2]. Kau ST, et al. On the topically effective ocular hypotensive properties of ICI 147,798, a natriuretic beta-adrenoceptor antagonist, in rabbits. Pharmacol Toxicol. 1989;64(1):132-136. [Content Brief]
- [3]. Keith RA, et al. ICI 147,798: a slowly dissociable beta adrenoceptor antagonist that causes insurmountable beta-1 and surmountable beta-2 adrenoceptor antagonism in isolated tissues. J Pharmacol Exp Ther. 1989;248(1):240-248. [Content Brief]
Keywords
