The Sound of Evolution
Guanethidine
Mechanism of action:
Guanethidine is an adrenergic neuron blocker. Within sympathetic neurons, guanethidine accumulates at nerve terminals and near storage vesicles, gradually replacing norepinephrine stored in the vesicles and reducing the amount of releasable norepinephrine. When the nerves are stimulated, sympathetic stimulation of the heart and blood vessels is markedly weakened because norepinephrine stores are depleted and its release is impaired, leading to a reduction in blood pressure.
Reference(s):
1. Joyce PI et al. (2001). Interaction of local anaesthetic agents with the endogenous norepinephrine transporter in SH-SY5Y human neuroblastoma cells. Neurosci Lett.
2. Yi E et al. (2005). Alpha-adrenergic modulation of synaptic transmission in rabbit pancreatic ganglia. Auton Neurosci.
3. Galli A et al. (1996). Norepinephrine transporters have channel modes of conduction. Proc Natl Acad Sci USA.