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Effect of urapidil on rat brain catecholamine synthesis
The Journal of Pharmacy and Pharmacology
|September 1, 1986
Summary
Urapidil, an antihypertensive drug, increases noradrenaline (NA) and dopamine (DA) synthesis in rat brains. This suggests urapidil may lower blood pressure by reducing central sympathetic nervous system activity.
Area of Science:
- Neuropharmacology
- Cardiovascular Pharmacology
Background:
- Urapidil is an effective antihypertensive medication.
- Understanding its central nervous system effects is crucial for its clinical application.
Purpose of the Study:
- To investigate the in-vivo effects of urapidil on the synthesis rates of noradrenaline (NA) and dopamine (DA) in the rat brain.
- To elucidate the potential central mechanisms underlying urapidil's hypotensive action.
Main Methods:
- Rats were administered urapidil at varying doses (3-30 mg kg-1 i.p.).
- Dopa decarboxylase was inhibited using NSD 1015.
- Dopa concentrations in the brain stem and striatum were measured to assess NA and DA turnover.
Main Results:
- Urapidil caused a significant, dose-dependent increase in dopa concentration in the brain stem and striatum.
- This indicates an elevated turnover rate of noradrenaline (NA) and dopamine (DA).
- The effect is likely due to the central blockade of alpha 1-adrenergic and dopamine receptors.
Conclusions:
- Urapidil's central hypotensive action may be partly mediated by reduced noradrenaline (NA) influence in the brain stem.
- This reduction in NA activity likely decreases central sympathetic outflow.
- Urapidil's neuropharmacological effects contribute to its antihypertensive efficacy.