Bifeprunox 是有效的多巴胺D2和5-HT1A受体部分激动剂，对皮质 5-HT1A 和纹状体 D2 的pKi分别为 7.19 和 8.83，对海马 5-HT1A 的pEC50为 6.37。Bifeprunox 作为一种抗精神病剂，可用于精神分裂症的研究。
| 生物活性 | Bifeprunox is a potentdopamine D2-like and5-HT1A receptorpartial agonist withpKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and apEC50of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia[1][2]. |
| IC50& Target[2] | 5-HT1AReceptor 7.19 (pKi, cortex) | D2Receptor 8.83 (pKi, striatum) | 5-HT1AReceptor 6.37 (pEC50, hippocampus) |
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体外研究
(In Vitro) | Bifeprunox has a pKiof 8 at h5-HT1A receptors, with an Emaxof 70%[1].
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体内研究
(In Vivo) | Bifeprunox (0.001-2.5 mg/kg) reduces marble burying in mice[2].
Bifeprunox (4-250 μg/kg) influences nicotine-seeking behaviour in response to drug-associated stimuli in rats[3].
| Animal Model: | Male NMRI mice (weighing 20-22 g)[2] | | Dosage: | 0.001, 0.0025, 0.01, 0.04, 0.16, 0.63, and 2.5 mg/kg | | Administration: | I.p. | | Result: | Reduced marble burying. Potently active from 0.0025 mg/kg. |
| Animal Model: | Naive male Wistar rats (weighing 250-275 g)[3] | | Dosage: | 4, 16, 64 and 250 μg/kg | | Administration: | Injected s.c. 30 minutes before testing | | Result: | 4-16 μg/kg dose-dependently attenuated the responsereinstating effects of nicotine-associated cues. Higher doses (64-250 μg/kg, s.c.) reduced spontaneous locomotor activity and suppressed operant responding induced by sucrose-associated cues and by the primary reinforcing properties of nicotine or sucrose. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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