1299470-39-5
1299470-39-5 用途与合成方法
|
Rat D 2 Receptor 54 nM (Ki) |
Rat 5-HT 2 Receptor 3.1 nM (Ki) |
Rat D 1 Receptor 546 nM (Ki) |
Rat 5-HT 1A Receptor 168 nM (Ki) |
Rat 5-HT 6 Receptor 42.7 nM (Ki) |
Rat 5-HT 7 Receptor 21.6 nM (Ki) |
Human D 1 Receptor 216 nM (Ki) |
Human D 3 Receptor 7.1 nM (Ki) |
Human D 4 Receptor 25 nM (Ki) |
Human D 5 Receptor 319 nM (Ki) |
Human 5-HT 2A Receptor 5.6 nM (Ki) |
Human 5-HT 2C Receptor 42.8 nM (Ki) |
Iloperidone hydrochloride displays higher affinity for the dopamine D
3
receptor (K
i
=7.1 nM) than for the dopamine D
4
receptor (K
i
=25 nM). Iloperidone displays high affinity for the 5-HT
6
and 5-HT
7
receptors (K
i
=42.7 and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT
2A
(Ki=5.6 nM) than for the 5-HT
2C
receptor (K
i
=42.8 nM).
Iloperidone hydrochloride is eliminated slowly, with a mean t
1/2
of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, t
max
, or C
max
. These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events.
