1299470-39-5
| 中文名稱 | 1299470-39-5 |
|---|---|
| 中文同義詞 | 鹽酸伊潘立酮;化合物 T22858 |
| 英文名稱 | Iloperidone (hydrochloride) |
| 英文同義詞 | Iloperidone (hydrochloride);Iloperidone hydrochloride (HP-873 hydrochloride);Iloperidone D3 Hydrochloride |
| CAS號 | 1299470-39-5 |
| 分子式 | C24H28ClFN2O4 |
| 分子量 | 462.95 |
| EINECS號 | |
| 相關(guān)類別 | |
| Mol文件 | 1299470-39-5.mol |
| 結(jié)構(gòu)式 |  |
1299470-39-5 性質(zhì)
| 儲存條件 | Store at -20°C |
|---|---|
| 溶解度 | 溶于二甲基亞砜 |
| 形態(tài) | 粉末 |
|
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.