Drug intelligence / Profile preview

lomerizine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Lomerizine is a diphenylmethylpiperazine calcium channel blocker with relatively selective central nervous system effects. It is primarily used for the prophylactic treatment of migraines and is also being investigated for eye-related diseases associated with local circulatory disturbances, such as normal-tension glaucoma. Lomerizine acts mainly by blocking voltage-dependent calcium channels (specifically L-type and T-type), leading to vasodilation in cerebral blood vessels and increased blood flow in the brain and retina. Additionally, it antagonizes the 5-hydroxytryptamine receptor 2A, inhibiting serotonin-induced contraction of cerebral arteries—a mechanism believed to contribute to its antimigraine effect. The drug also demonstrates neuroprotective properties in retinal injury models[1][2][3][5][7].

Brand names
Lomerizine
Other names
lomerizina1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazineLomerazine
02

Targets

HTR2A (Serotonin receptor 5-HT2A)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)CaV3 (Caveolin-3)

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