151227-08-6性质、用途与生产工艺
AP521 是一个人 5-HT1A 受体激动剂,其 IC50 值为 94 nM。
5-HT
1A
Receptor
94 nM (IC
50
, in human)
|
5-HT
1A
Receptor
135 nM (IC
50
, in rat)
|
5-HT
1B
Receptor
254 nM (IC
50
, in rat)
|
5-HT
1B
Receptor
5530 nM (IC
50
, in human)
|
5-HT
1D
Receptor
418 nM (IC
50
, in human)
|
5-HT
5A
Receptor
422 nM (IC
50
, in human)
|
5-HT
7
Receptor
198 nM (IC
50
, in rat)
|
AP521 is an agonist of human 5-HT
1A
receptor with IC
50
s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT
1A
(rat), 5-HT
1A
(human), 5-HT
1B
(rat), 5-HT
1B
(human), 5-HT
1D
(human), 5-HT
5a
(human) and 5-HT
7
(rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM.
AP521 significantly increases the number of shock acceptances [F(5,105)=4.46, P<0.01] at doses between 0.5 to 10 mg/kg. Oral administration of AP521 at 3 and 10 mg/kg significantly decreases freezing time [F(3,60)=2.89, P<0.05]. AP521 significantly increases the time spent on the open arms by approximately 2-fold as compare to the vehicle treated group [F(3, 36)=4.21, P<0.05 for AP521]. The anxiolytic-like effect of AP521 appears to be dose-related. AP521 significantly increases the extracellular 5-HT level of the medial prefrontal cortex (mPFC) at 10 mg/kg from 0.5 to 1 h after administration. AP521 at 3 mg/kg tends to increase the extracellular 5-HT level, however, this increase is not significant.
151227-08-6
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