17-phenyl trinor PGF N-ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost. The N-ethyl amide prostaglandin prodrugs are converted to the active free acid more slowly than the analogous prostaglandin ester prodrugs such as latanoprost. This product is the isopropyl ester of the free acid prostaglandin which corresponds to Bimatoprost. The free acid, 17-phenyl trinor PGF, is a potent FP receptor agonist. In human and animal models of glaucoma, FP receptor agonist activity corresponds very closely with intraocular hypotensive activity. The 17-phenyl trinor PGF isopropyl ester derivative was examined for IOP-lowering activity during the development of latanoprost. At the dose of 3 μg/eye in the monkey, 17-phenyl trinor PGF isopropyl ester was the most potent analog tested in reducing IOP, lowering the IOP 1.3 mm Hg below the level achieved by latanoprost. However, this derivative was also significantly more irritating to the eye than latanoprost.
17-Phenyl trinor PGF2α isopropyl ester is a FP receptor agonist and intraocular pressure-lowering agent. 17-Phenyl trinor PGF2α isopropyl ester induces iris sphincter contraction, reduces intraocular pressure and pupil diameter, causes no ocular irritation, and only leads to mild conjunctival hyperemia. 17-Phenyl trinor PGF2α isopropyl ester is applicable to relevant research on glaucoma.
体内研究
17 Phenyl trinor PGF2 α isopropyl ester (3 μg; single ocular local administration) can induce a statistically significant maximum 2.9 mmHg IOP reduction in cynomolgus monkeys with normal blood pressure [1].
17-Phenyl trinor PGF2 α isopropyl ester (3 μg; ocular surface administration; A single dose can cause mild eye irritation in domestic female cats.
17-Phenyl trinor PGF2α isopropyl ester (0.03-3 μg; Single ocular administration can induce dose-dependent mild conjunctival congestion in New Zealand albino white rabbits [1].
Animal Model:
Cynomolgus monkeys
Dosage:
3 μg
Administration:
o.a.; single dose
Result:
Produced a maximum reduction in IOP of 2.9 mmHg.
Animal Model:
Domestic female cats (2-3 kg)
Dosage:
3 μg
Administration:
o.a.; single dose
Result:
Caused a maximum irritation score of 0.2 arbitrary units, which was significantly lower than the irritation induced by PGF2α isopropyl ester (1b).
Animal Model:
New Zealand White albino rabbits (2-3 kg)
Dosage:
0.03 μg, 0.1 μg, 0.3 μg, 1 μg, 3 μg
Administration:
o.a.; single dose
Result:
Induced mild conjunctival hyperemia, with maximum difference scores (experimental eye vs. control eye) of approximately 0.8, 1.0, 1.4, 1.5, and 1.7 arbitrary units at doses of 0.03 μg, 0.1 μg, 0.3 μg, 1 μg, and 3 μg, respectively; this hyperemia was significantly less pronounced than that induced by PGF2α isopropyl ester (1b).
分子式
C26H38O5
分子量
430.6
CAS号
130209-76-6
中文名称
比马前列素异丙酯
运输条件
Room temperature in continental US; may vary elsewhere.