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Deviating central hypotensive activity of urapidil in the cat
The Journal of Pharmacy and Pharmacology
|November 1, 1985
Summary
Urapidil exhibits potent central hypotensive activity, distinct from known antihypertensive mechanisms. Its central action is not mediated by common neurotransmitter receptors, suggesting a novel pathway for blood pressure reduction.
Area of Science:
- Pharmacology
- Cardiovascular Research
- Neuroscience
Background:
- Urapidil is an antihypertensive drug with both peripheral alpha 1-adrenoceptor antagonism and central hypotensive effects.
- Classical centrally acting antihypertensives often target central alpha 2-adrenoceptors.
Purpose of the Study:
- To investigate the mechanism of the central hypotensive action of urapidil.
- To determine if urapidil's central effects involve known receptor systems.
Main Methods:
- Urapidil was administered via the vertebral artery in chloralose-anesthetized cats.
- The effects of pre-treatment with various receptor antagonists on urapidil's central hypotensive action were assessed.
Main Results:
- Urapidil's hypotensive effect was significantly stronger when administered centrally compared to systemically.
- Central pre-treatment with antagonists for alpha 2-, alpha 1-adrenoceptors, histamine, dopamine, muscarinic, serotonin, or opiate receptors did not block urapidil's central hypotensive effect.
Conclusions:
- The central hypotensive action of urapidil is not mediated by the investigated central receptor types.
- Urapidil's central mechanism of action appears to differ from that of established centrally acting antihypertensives like clonidine.