Key result
Diphenylpyraline analogs inhibit Ca2+-dependent contractions in isolated mouse mesenteric arteries and display binding interactions with the CaV1.1 channel.
Diphenylpyraline analogs demonstrate potential calcium channel blocker activity, inhibiting vascular contractions in preclinical models.
May support novel CaV1.1 modulators distinct from dihydropyridines; leaves open clinical translation.
Molecular interactions of 4-diphenylmethoxy-1-methylpiperidine derivatives with the calcium channel CaV1.1 (pdb:6JP5) are described. All the compounds tested, previously shown to inhibit adrenergic vascular contractions, display similar binding energetics and interactions with the trans-membrane domain of 6JP5 on the opposite side relative to the channel pore, where nifedipine, a known dihydropyridine Ca2+ channel blocker binds. Additionally, the compounds tested inhibit Ca2+-dependent contractions in isolated mouse mesenteric arteries. Thus, diphenylpyraline analogs may exert their anticontractile effects, at least partially, by blocking vascular Ca2+ channels.
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Pulgar et al. (2023) studied this question. 4-diphenylmethoxy-1-methylpiperidine derivatives was evaluated on Ca2+-dependent contractions and binding energetics. Diphenylpyraline analogs inhibit Ca2+-dependent contractions in isolated mouse mesenteric arteries and display binding interactions with the CaV1.1 channel.
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