Hexamethonium (Bromide)

Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models^[1][2][3][4]. IC50 & Target: nAChR^[1] In Vitro: Hexamethonium Bromide (100 µM; 60 minutes) abolishes epibatidine-induced depolarisations of smooth muscle cells^[1].
The α3β4α5 receptors have greater sensitivity to Hexamethonium Bromide than the other potential ganglionic models, α3β4, α3β2, and α3β2α5^[2].
In Vivo: Hexamethonium Bromide (0.2-25 mg/kg; i.v.) significantly reduces the renal sympathetic nerve activity (RSNA), mean arterial pressure (MAP) and heart rate (HR) in the Wistar rats and the spontaneously hypertensive rats (SHRs)^[4].
Hexamethonium Bromide (0.2-1.0 mg/kg; i.v.) treatments show no significant differences in the RSNA, MAP or HR between Wistar rats and SHRs^[4].
Hexamethonium Bromide (5.0-25 mg/kg; i.v.) results in a greater reduction in the RSNA and MAP in SHRs compared with Wistar rats^[4].