Hellberg M R, Sallee V L, McLaughlin M A, Sharif N A, Desantis L, Dean T R, Zinke P W
Department of Medicinal Chemistry, Glaucoma Research, Alcon Research Ltd., Fort Worth, TX 76134, USA.
J Ocul Pharmacol Ther. 2001 Oct;17(5):421-32. doi: 10.1089/108076801753266802.
Travoprost is the isopropyl ester prodrug of a high affinity, selective FP prostaglandin full receptor agonist. In contrast to travoprost acid's high affinity and efficacy at the FP receptor, there is only sub-micromolar affinity for the DP, EP1, EP3, EP4, IP, and TP receptors. Travoprost produced a lower incidence of ocular irritation than PGF20 isopropyl ester at a dose of 1 microg in the New Zealand albino (NZA) rabbit. Topical ocular application of travoprost produced a marked miotic effect in cats following doses of 0.01, 0.03 and 0.1 microg. In the ocular hypertensive monkey, b.i.d. application of 0.1 and 0.3 microg of travoprost afforded peak reduction in intraocular pressure (IOP) of 22.7% and 28.6%, respectively. Topical application of travoprost was well tolerated in rabbits, cats and monkeys, causing no ocular irritation or discomfort at doses up to 1 microg. Travoprost is a promising ocular hypotensive prostaglandin FP derivative that has the ocular hypotensive efficacy of PGF2alpha isopropyl ester but with less severe ocular side effects.
曲伏前列素是一种高亲和力、选择性FP前列腺素全受体激动剂的异丙酯前药。与曲伏前列素酸对FP受体的高亲和力和效力不同，它对DP、EP1、EP3、EP4、IP和TP受体的亲和力仅为亚微摩尔级别。在新西兰白化兔中，曲伏前列素在1微克剂量下引起的眼部刺激发生率低于前列腺素F2α异丙酯。在猫中，局部眼部应用0.01、0.03和0.1微克剂量的曲伏前列素会产生明显的缩瞳作用。在高眼压猴子中，每日两次应用0.1和0.3微克曲伏前列素，眼内压（IOP）的峰值降低分别为22.7%和28.6%。曲伏前列素在兔、猫和猴子中的局部应用耐受性良好，在高达1微克的剂量下不会引起眼部刺激或不适。曲伏前列素是一种有前景的降眼压前列腺素FP衍生物，具有前列腺素F2α异丙酯的降眼压功效，但眼部副作用较轻。
