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Abstract #10477 Published in IGR 6-1
Effects of 2-alkynyladenosine derivatives on intraocular pressure in rabbits
Konno T; Ohnuma SY; Uemoto K; Uchibori T; Nagai A; Kogi K; Endo K; Hosokawa T; Nakahata NEuropean Journal of Pharmacology 2004; 486: 307-316
The authors evaluated the activities of 2-alkynyladenosine derivatives, relatively selective adenosine A2 receptor agonists, in intraocular pressure (IOP) regulation in rabbits. An adenosine A2 receptor agonist 2-[p-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamidoadenosine (CGS-21680) decreased IOP, while another A2 receptor agonist 2-(phenylamino)adenosine transiently increased it. The first group of 2-alkynyladenosine derivatives (1-hexyn-1-yl derivatives) caused a transient increase followed by decrease in IOP, while the second group (1-octyn-1-yl and 6-cyano-1-hexyn-1-yl derivatives) only decreased it. The second group is also effective in the ocular hypertensive models induced by water-loading and α-chymotrypsin. The outflow facility was increased by a 1-octyn-1-yl derivative. Both increases and decreases in IOP induced by 2-alkynyladenosine derivatives were inhibited by an adenosine A2 receptor antagonist 3,7-dimethyl-1- propargylxanthine, but not by an adenosine A1 receptor antagonist 8-cyclopentyl-1,3-dipropyl xanthine. These findings suggest that 2-alkynyladenosine derivatives may affect IOP via adenosine A2 receptor, and 2-alkynyladenosine derivative-induced ocular hypotension is due to the increase of outflow facility.
Dr. T. Konno, Drug Research Section II, Fukushima Research Laboratories, TOA EIYO Ltd., 1 Tanaka, Yuno, Iizaka, Fukushima 960-0280, Japan
Classification:
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)
