alpha-Adrenoceptors and Acute Migraine Therapy.
In contrast to the well-established role of serotonin (5-hydroxytryptamine; 5-HT) 5-HT(1B) receptors in mediating constriction within the carotid vascular bed of dogs and pigs, the role of alpha-adrenoceptors and their subtypes has not been as well understood. Using experimental animal models and alpha(1)-adrenoceptor and alpha(2)-adrenoceptor agonists (phenylephrine and BHT-933, respectively) and antagonists (prazosin and rauwolscine, respectively), it was recently shown that activation of either receptor produces a cranioselective vasoconstriction. Subsequently, investigations employing relatively selective antagonists at alpha(1)- (alpha(1A), alpha(1B), alpha(1D)) and alpha(2)- (alpha(2A), alpha(2B), alpha(2C)) adrenoceptor subtypes revealed that specific receptors mediate carotid vasoconstrictor responses. Since alpha(1B)-adrenoceptors and alpha(2C)-adrenoceptors do not seem to play an important role in the cardiovascular regulation, it is suggested that selective agonists at these receptors may provide a promising novel avenue for the development of acute antimigraine drugs. (c) 2002 Prous Science. All rights reserved.
Willems
Edwin W.
EW
Valdivia
Luis Felipe
LF
Villalon
Carlos M.
CM
Saxena
Pramod R.
PR