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Evidence for the interaction of urapidil with 5-HT1A receptors in the brain leading to a decrease in blood pressure
N Kolassa1, K D Beller, K H Sanders
1Department of Pharamacology, Byk Gulden Pharmaceuticals, Konstanz, Federal Republic of Germany.
Abstract:
Current knowledge about the role of serotonin (5-HT) in central cardiovascular regulation is reviewed. Results from experiments with the 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) suggest that activation of somatodendritic 5-HT1A receptors in the medulla oblongata decreases the firing of serotoninergic neurons and thus reduces their excitatory input to the sympathetic neurons in the intermediolateral cell column. As a consequence, blood pressure is reduced by 5-HT1A receptor agonists. Urapidil is an antihypertensive drug that has a dual mode of action: peripheral alpha-adrenoceptor antagonism and interaction with 5-HT1A receptors in the brain. This profile can adequately explain the vasodilation and lack of significant sympathetic activation observed during urapidil treatment.
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