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Alverine citrate

CAS No. : 5560-59-8

MCE 站：Alverine citrate

产品活性：Alverine citrate 是 5-HT_1A 受体的一个拮抗剂，其 IC₅₀ 值为101 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: Alverine is a drug used for functional gastrointestinal disorders. Alverine acts directly on the muscle in the gut, causing it to relax. Alverine Citrate (20 mg/kg) suppresses the effect of 5-HTP, but not that of 8-OH-DPAT. However, when injected intracerebroventricularly (75 μg/rat) alverine citrate reduces 8-OH-DPAT-induced enhancement of rectal distension-induced abdominal contractions. In-vitro binding studies reveal that Alverine citrate has a high affinity for 5-HT_1A receptors and a weak affinity for 5-HT3 and 5-HT4 subtypes. Alverine may increase Ca influx during action potentials due to inhibition of the inactivation of L-type Ca channels, but may also suppress evoked activity by inhibiting the sensitivity of contractile proteins to Ca²⁺.

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