Lomerizine dihydrochloride

Non Antibodies

L-type Ca2+ channels

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

541, 5

A Blocker of L-Type Voltage-Gated Ca2+ Channels

DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

41116134

Lomerizine dihydrochloride inhibited CaV currents in PC12 cells with IC50 of 1.9 µM1. It inhibits L-type Ca2+ channels2.

Yes

Voltage-dependent L-type Ca2+ channels play an important role Ca2+ influx. L-type calcium currents typically require a strong depolarization for activation and are long-lasting1.The common pharmacological profile of L-type channels is determined by the α1 subunit, which forms the Ca2+ selective pore, and is encoded by one of the CaV1 (α 1S) channel genes2. Cav1.2 (CACNA1C) in humans is widely expressed in cardiac myocytes, smooth muscle myocytes, endocrine cells, neuronal cell bodies and proximal dendrites1.Lomerizine dihydrochloride is a Ca2+ channel blocker with relatively selective CNS effects. Lomerizine was developed as a potential agent for the selective improvement of the ocular or cerebrovascular circulation with minimal adverse cardiovascular effects3, and it is used as an anti migraine drug4. Lomerizine selectively relaxes smooth muscle cells by inhibiting L-type Ca2+ influx, thereby reducing tone and increasing blood flow in cerebral vessels4.Lomerizine blocked Ba2+ current through the voltage-gated Ca2+ channel in rat pheochromocytoma (PC12) cells5, and it is suggested to bind to the 1, 4-dihydropyridine binding site, as obtained by a [3H]nitrendipine binding study6.