The alpha 1d-adrenoceptor subtype is involved in the noradrenaline-induced contractions of rat aorta.
The pA2 value of several alpha 1-adrenoceptor antagonists on noradrenaline-induced contractions of rat aorta, and their affinity for the cloned alpha 1a-, alpha 1b- and alpha 1d-adrenoceptor subtypes were evaluated. Selective or moderately selective alpha 1d-, partially selective alpha 1b-, selective alpha 1a- and non subtype-selective alpha 1-adrenoceptors antagonists were included in the study. The potency of these compounds on rat aorta was well correlated with the affinity observed for the alpha 1d-adrenoceptor subtype. A poor correlation was found for the alpha 1b- and alpha 1a-subtypes. These results suggest that the alpha 1d-subtype plays a determining role in rat aorta contractions induced by noradrenaline.
Testa
R
R
Research & Development Department, RECORDATI S.p.A., Milano, Italy.
Destefani
C
C
Guarneri
L
L
Poggesi
E
E
Simonazzi
I
I
Taddei
C
C
Leonardi
A
A
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology; D000818:Animals; D001011:Aorta / Q000502:physiology*; D008024:Ligands; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects / Q000502:physiology*; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology*; D009638:Norepinephrine / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D018340:Receptors, Adrenergic, alpha-1 / Q000145:classification / Q000502:physiology*
D000317:Adrenergic alpha-Antagonists; D008024:Ligands; D018340:Receptors, Adrenergic, alpha-1; D009638:Norepinephrine