Timolol Maleate (Synonyms: MK-950, (S)-Timolol (maleate), WP934) |
カタログ番号GC12468 |
チモロール マレイン酸 (L-714,465 マレイン酸) は、心選択的でない親水性 β-アドレナリン受容体遮断薬です。
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Cas No.: 26921-17-5
Sample solution is provided at 25 µL, 10mM.
(S)-Timolol Maleate (L-714,465 Maleate;MK 950), is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively).
(S)-Timolol Maleate (L-714,465 Maleate;MK 950), 50% bioavailability following oral administration. Does not cross the blood brain barrier. Timolol maleate does appear to have some local anesthetic properties in human cornea after chronic use by susceptible individuals.
References:
[1]. Deepika Aggarwal, Indu P. Kaur. Improved pharmacodynamics of timolol maleate from a mucoadhesive niosomal ophthalmic drug delivery system. International Journal of Pharmaceutics. 2005, 290(1-2): 155-159.
[2]. Mandagere AK, Thompson TN, Hwang KK. Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. J Med Chem. 2002;45(2):304-11.
[3]. A.H El-Kamel. In vitro and in vivo evaluation of Pluronic F127-based ocular delivery system for timolol maleate. International Journal of Pharmaceutics. 2002, 241, (1) :47-55.
[4]. Konstas AG, Maltezos AC, Gandi S, et al. Comparison of 24-hour intraocular pressure reduction with two dosing regimens of latanoprost and timolol maleate in patients with primary open-angle glaucoma. American Journal of Ophthalmology .1999, 128(1):15-20.
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