95847-70-4
中文名称
依普西隆
英文名称
Ipsapirone
CAS
95847-70-4
分子式
C19H23N5O3S
分子量
401.48
MOL 文件
95847-70-4.mol
更新日期
2024/09/27 11:48:58
95847-70-4 结构式
基本信息
中文别名
依普西隆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
英文别名
IsapironeIPSAPIRONE
1,2-benzisothiazol-3(2h)-one,2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-,1,
2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)benzo[d]isothiazol-3(2H)-one 1,1-dioxide
2-[4-[4-(2-PYRIMIDINYL)-1-PIPERAZINYL]BUTYL]-1,2-BENZISOTHIAZOL-3(2H)-ONE-1,1-DIOXIDE
物理化学性质
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Soluble to 10 mM in DMSO
酸度系数(pKa)7.69±0.10(Predicted)
形态粉末
颜色White to off-white
常见问题列表
生物活性
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。靶点
|
5-HT 1A Receptor
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体内研究
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.). |