依普西隆
| 中文名称 | 依普西隆 |
|---|---|
| 中文同义词 | 2-[4-[4-(2-嘧啶基)-1-哌嗪基]丁基]-1,2-苯并异噻唑-3(2H)-酮-1,1-二氧化物;依普西隆;化合物 T22871;IPSAPIRONE,5-HT1激动剂 |
| 英文名称 | Ipsapirone |
| 英文同义词 | IPSAPIRONE;2-[4-[4-(2-PYRIMIDINYL)-1-PIPERAZINYL]BUTYL]-1,2-BENZISOTHIAZOL-3(2H)-ONE-1,1-DIOXIDE;1,2-benzisothiazol-3(2h)-one,2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-,1,;Isapirone;2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)benzo[d]isothiazol-3(2H)-one 1,1-dioxide;Benzeneethanamine,5-chloro-α-methyl-;1,2-Benzisothiazol-3(2H)-one, 2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-, 1,1-dioxide |
| CAS号 | 95847-70-4 |
| 分子式 | C19H23N5O3S |
| 分子量 | 401.48 |
| EINECS号 | |
| 相关类别 | Serotonin receptor |
| Mol文件 | 95847-70-4.mol |
| 结构式 |  |
依普西隆 性质
| 熔点 | 137-138° |
|---|---|
| 沸点 | 629.8±65.0 °C(Predicted) |
| 密度 | 1.345±0.06 g/cm3(Predicted) |
| 储存条件 | Store at RT |
| 溶解度 | 在 DMSO 中溶解度为 10 mM |
| 形态 | 粉末 |
| 酸度系数(pKa) | 7.69±0.10(Predicted) |
Ipsapirone (TVX Q 7821)，是具有抗焦虑活性的化合物，是 5-HT1A 受体的部分激动剂，也表现出 5-HT1A 受体的拮抗作用，并且只在高剂量时，对 5-HT2 和α1 肾上腺素能表现出抑制作用。
|
5-HT 1A Receptor
|
Ipsapirone inhibits induced by 8-OH-DPAT and 5-methoxydimethyltryptamine (agonists of 5-HT1A receptors) behavioural effects (flat body posture and forepaw treading) in normal and reserpinized rats.
Ipsapirone (2.5-80 mg/kg), given alone to rats induces a slight flattening of body posture (~ 1 point at the highest dose) and a mild hind limb abduction observed at doses 2.5-80 mg/kg. Ipsapirone given alone at low doses (2.5-10 mg/kg i.p.) does not significantly change the body temperature in rats and mice, but decreased it in both those species at high doses (35 mg/kg i.p.) by ca. 2-2.5℃.
| Animal Model: |
Male Albino-Swiss mice (18-24 g) and male Wistar rats (160-200 g).
|
| Dosage: | 5 and 10 mg/kg. |
| Administration: | IP 30 min before 8-OH-DPAT and 5-MeODMT injections. |
| Result: | Behavioural responses (flat body posture, forepaw treading) to 8-OH-DPAT (5 mg/kg s.c.) in rats were antagonized by Ipsapirone (5 and 10 mg/kg i.p.). |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-19686 | 依普西隆 Ipsapirone | 95847-70-4 | 5mg | 800元 |
| 2024/01/25 | HY-19686 | Ipsapirone | 10 mg | 1200元 |