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Amitifadine hydrochloride

CAS No. : 410074-74-7

MCE 站：Amitifadine hydrochloride

产品活性：Amitifadine hydrochloride 是5-羟色胺-去甲肾上腺素-多巴胺的再摄取抑制剂 (SNDRI)，其在 HEK 293 细胞中测得的 IC₅₀ 值分别为 12， 23， 96 nM。

研究领域：Neuronal Signaling

作用靶点：Serotonin Transporter  |  Dopamine Transporter

In Vitro: Amitifadine (DOV 21,947) is an antidepressant drug. K_i values for SERT, NET, and DAT are 99 nM, 262 nM, and 213 nM. The IC₅₀ values for serotonin, norepinephrine and dopamine uptake are 12, 23 and 96 nM, respectively.

In Vivo: The 30 mg/kg Amitifadine dose significantly reduces nicotine self-administration. The 5 and 10 mg/kg doses reduce nicotine self-administration during the first 15 min. of the session when the greatest amount of nicotine is self-administered. The 30 mg/kg Amitifadine dose, but not the lower doses cause a significant reduction in locomotor activity averaged over the 1-hour session and reduce food motivated responding. The 10 mg/kg dose causes hypoactivity at the beginning of the session, but 5 mg/kg does not cause any hypoactivity. The effect of chronic Amitifadine treatment (10 mg/kg) over the course of 15 sessions is also determined. Amitifadine causes a significant reduction in nicotine self-administration, which is not seen to diminish over two consecutive weeks of treatment and a week after enforced abstinence. Amitifadine significantly reduces nicotine self-administration. This prompts further research to determine if Amitifadine might be an effective treatment for smoking cessation.

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