tcsc2694 Alverine (citrate)

Alverine citrate is a 5-HT_1A receptor antagonist, with an IC₅₀ of 101 nM.

IC50 & Target: IC50: 101 nM (5-HT_1A)^[1].

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^[1]. 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 Ca^2+[2].