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Pharmacological and pharmacokinetic study of olmesartan medoxomil in animal diabetic retinopathy models.

Abstract：

:A close relationship between the renin-angiotensin system and the pathophysiology of diabetic retinopathy has been suggested, several angiotensin II type 1 receptor (angiotensin AT1 receptor) antagonists being effective in animal models. Therefore, we examined the efficacy of an angiotensin AT1 receptor antagonist, olmesartan medoxomil (CS-866), in animal retinopathy models. In diabetic stroke-prone spontaneously hypertensive (SHRSP) rats, 4-week treatment with CS-866 prevented the elongation of oscillatory potential peaks dose-dependently which almost normalized at 3 mg/kg/day. Next, in oxygen-induced retinopathy mice, CS-866 at 1 mg/kg significantly prevented the retinal neovascularization. In these animal models, plasma concentrations of CS-866 were comparable to the in vitro IC50 value of the angiotensin AT1 receptor. In summary, our data demonstrated that CS-866 was effective in early and late stage retinopathy models through the inhibition of the angiotensin AT1 receptor. These findings suggest the possibility of CS-866 as a therapeutic agent for diabetic retinopathy.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Nakamura H,Inoue T,Arakawa N,Shimizu Y,Yoshigae Y,Fujimori I,Shimakawa E,Toyoshi T,Yokoyama T

doi

10.1016/j.ejphar.2005.02.047

keywords:

subject

Has Abstract

pub_date

2005-04-11 00:00:00

pages

239-46

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(05)00242-6

journal_volume

512

pub_type

杂志文章

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