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。
| 生物活性 | Ipsapirone (TVX Q 7821) is an anxiolytic compound and a5-HT1Areceptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits5-HT1Areceptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2and the α1-adrenergic function[1][2]. |
| IC50& Target[1][2] | |
体内研究
(In Vivo) | 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[1].
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℃[1].
| Animal Model: | Male Albino-Swiss mice (18-24 g) and male Wistar rats (160-200 g)[1].
| | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(62.27 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.4908 mL | 12.4539 mL | 24.9078 mL | | 5 mM | 0.4982 mL | 2.4908 mL | 4.9816 mL | | 10 mM | 0.2491 mL | 1.2454 mL | 2.4908 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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