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IC50: 0.03 μM

Fluspirilene is a potent and non-competitive antagonist of agonist-activated L-type calcium channels.

Voltage-gated calcium channels are critical for coupling membrane depolarization to the influx of calcium. The calcium that flows into excitable cells via voltage-gated calcium channels generates both electrical and chemical signals.

In vitro: Fluspirilene was found to be weakly active as an antagonist of Ca2(+)-induced contractions in K(+)-depolarized taenia. In addition, fluspirilene at 10-1000 nM was a potent non-competitive antagonist of the effects of Bay K 8644 on Ca2(+)-induced contractions and could selectively antagonise the effects of Bay K 8644, without affecting the calcium antagonist effects of nitrendipine [1].

In vivo: In a previous animal study, adult male Wistar rats were intramuscularly injected with a 8 mg/kg dose of fluspirilene. Results showed that the excretion was slow but constant during the first 12 days. The identified metabolites of the urine and faeces showed oxidative N-dealkylation as the major metabolic pathway [2].

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