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95847-70-4

中文名稱 依普西隆
英文名稱 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 2024/12/12 09:51:21
95847-70-4 結構式 95847-70-4 結構式

基本信息

中文別名
依普西隆
2-[4-[4-(2-嘧啶基)-1-哌嗪基]丁基]-1,2-苯并異噻唑-3(2H)-酮-1,1-二氧化物
英文別名
Isapirone
IPSAPIRONE
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

物理化學性質

熔點137-138°
沸點629.8±65.0 °C(Predicted)
密度1.345±0.06 g/cm3(Predicted)
儲存條件Store at RT
溶解度Soluble to 10 mM in DMSO
酸度系數(shù)(pKa)7.69±0.10(Predicted)
形態(tài)粉末
顏色White to off-white

常見問題列表

生物活性
Ipsapirone (TVX Q 7821),是具有抗焦慮活性的化合物,是 5-HT1A 受體的部分激動劑,也表現(xiàn)出 5-HT1A 受體的拮抗作用,并且只在高劑量時,對 5-HT2 和α1 腎上腺素能表現(xiàn)出抑制作用。
靶點

5-HT 1A Receptor

體內研究

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.).
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