2173037-97-1
2173037-97-1 結(jié)構(gòu)式
基本信息
Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-4-[(3-methoxybenzoyl)amino]-, (1S,2S,4S,5R,6S)-
物理化學(xué)性質(zhì)
常見問題列表
|
mGluR3 0.47 nM (EC 50 ) |
mGluR3 0.927 nM (Ki) |
mGluR2 47.5 (EC 50 ) |
mGluR2 412 (Ki) |
LY2794193 exhihits inhibition of spontaneous Ca
2+
oscillations in cultured rat cortical neurons with an EC
50
of 43.6 nM.
In the rat cortical neuron Ca
2+
oscillation assay, LY2794193 exhibits a biphasic inhibition of spontaneous Ca
2+
transients (high affinity EC
50
=0.44 nM; 48% of the total agonist response; low affinity EC
50
=43.6 nM; 52% of the total agonist response) with combined maximal agonist efficacy (E
max
) of 66%.
LY2794193 (1-30 mg/kg, s.c.), given 30 min prior to PCP (5 mg/kg, s.c.) leads a dose-related reduction in ambulations.
LY2794193 (1 mg/kg; i.v.) exhibits moderate clearance (18.3 mL/min per kg) and volume of distribution (1.17 L/kg) with a calculated plasma half-life (T
1/2
) of 3.1 h in Male Sprague-Dawley rats.
LY2794193 (3 mg/kg; s.c.) leads to the rapid appearance in the plasma (AUC=9.9 μM; C
max
=6.78 μM; T
max
=0.44 h) and a calculated bioavailability of 121% in male Sprague-Dawley rats.
| Animal Model: | Male Sprague-Dawley rats |
| Dosage: | 1, 3, 10, or 30 mg/kg |
| Administration: | Administrated s.c.; given 30 min prior to PCP (5 mg/kg, s.c.) |
| Result: | A dose-related reduction in ambulations was observed, with the 10 and 30 mg/kg dose groups found to be statistically significant. |