advertisement
Adenosine is thought to participate in the regulation of intraocular pressure since adenosine and several adenosine derivatives increase and/or decrease intraocular pressure. This article reviews the involvement of adenosine receptors in the regulation of intraocular pressure and the possible application of relatively selective adenosine A2-receptor agonists, 2-alkynyladenosine derivatives (2-AAs), as novel drugs for treatment of glaucoma. We found that some 2-AAs decreased intraocular pressure in normotensive rabbits. Moreover, these 2-AAs are also effective in the ocular hypertensive models induced by water-loading and α-chymotrypsin. In addition, the ocular hypotension induced by 2-(1-octyn-1-yl) derivative was 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. Moreover, the outflow facility was increased by the 2-(1-octyn-1-yl) derivative. These findings suggest that 2-AAs may affect intraocular pressure via adenosine A 2-receptor, and 2-AAs-induced ocular hypotension is due to the increase in outflow facility. Some 2-AAs may be novel drugs against ocular hypertension and/or glaucoma, although additional studies are required to characterize the effects of 2-AAs on regulation of intraocular pressure in detail. LA: Japanese
T. Konno, Drug Research Section II, Fukushima Research Laboratories, Toa Eiyo Ltd., Iizaka, Fukushima 960-0280
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)