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
2024/10/28 11:14:33
95847-70-4 結(jié)構(gòu)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
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
物理化學(xué)性質(zhì)
熔點(diǎn)137-138°
沸點(diǎn)629.8±65.0 °C(Predicted)
密度1.345±0.06 g/cm3(Predicted)
儲(chǔ)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(jiàn)問(wèn)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(dòng)劑，也表現(xiàn)出 5-HT1A 受體的拮抗作用，并且只在高劑量時(shí)，對(duì) 5-HT2 和α1 腎上腺素能表現(xiàn)出抑制作用。靶點(diǎn)
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5-HT 1A Receptor
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體內(nèi)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).
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| 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.). |