Evidence for the interaction of urapidil with 5-HT1A receptors in the brain leading to a decrease in blood pressure.
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.
Kolassa
N
N
Department of Pharamacology, Byk Gulden Pharmaceuticals, Konstanz, Federal Republic of Germany.
Beller
K D
KD
Sanders
K H
KH
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects*; D002319:Cardiovascular System / Q000187:drug effects; D006801:Humans; D008526:Medulla Oblongata / Q000187:drug effects*; D010879:Piperazines / Q000494:pharmacology*; D011985:Receptors, Serotonin / Q000187:drug effects*; D014664:Vasodilation / Q000187:drug effects
D010879:Piperazines; D011985:Receptors, Serotonin; C015568:urapidil