LY3027788 是 LY3020371 的二酯类似物，是mGlu2/3 receptor的拮抗剂，是 LY3020371 的一种有效的口服活性前药。LY3027788 具有抗抑郁功效。
| 生物活性 | LY3027788, a diester analog of LY3020371 which is anmGlu2/3 receptorantagonist, is a potent and orally active prodrug of LY3020371. LY3027788 has antidepressant efficacy[1][2]. |
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体内研究
(In Vivo) | LY3027788 (4.8-27 mg/kg; a single p.o.) produces antidepressant-like decreases in immobility times in the forced-swim test in mice[1].
LY3027788 (4.8-16 mg/kg; a single p.o.) enhances the locomotor stimulant effects of quinpirole at the dose of 16 mg/kg in the locomotor activity assay in mice[1].
LY3027788 (10-30 mg/kg; a single p.o.) dose dependently increases the wake time of rats without engendering rebound hypersomnolence[1].
LY3027788 (a single p.o.) leads to the rapid and dose-proportionate appearance of the pharmacologically active species LY3020371 in plasma of both mouse (4.8-27 mg/kg) and rat (3-30 mg/kg)[1].
| Animal Model: | Male Sprague-Dawley mice (20-25 g)[1] | | Dosage: | 4.8, 16, 27 mg/kg | | Administration: | A single p.o. (60 minutes prior to testing) | | Result: | Potent and efficacious with a minimal effective dose of 16 mg/kg in the mouse forced-swim assay.
The ED60was 8.2 mg/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
