Characterization of alpha1-adrenoceptor subtypes in the pig

Eur J Pharmacol. 1998 Apr 24;347(2-3):301-9. doi: 10.1016/s0014-2999(98)00104-6.

Abstract

The identities of the alpha1-adrenoceptor subtypes present in various tissues of the pig were studied using [3H]prazosin radioligand binding. The subtypes were characterized by performing competition experiments for various subtype selective drugs. In the cerebral cortex, spleen and heart, both alpha1A- and alpha1B-adrenoceptors were detected. In the liver was found only the alpha1A-subtype, while in the aorta was found only the alpha1B-subtype. An alpha1-adrenoceptor subtype was present in the adrenal gland with a high affinity for prazosin, the pKd value being 9.6, but with relatively low affinities for other alpha1-adrenoceptor binding drugs. The adrenal gland alpha1-adrenoceptor did not seem to represent the classical alpha1D-subtype, since drugs selective for the alpha1D-subtype in other species, including BMY7378 and SKF104856, showed low affinities for the pig adrenal gland alpha1-adrenoceptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenal Glands / metabolism
  • Adrenergic alpha-Antagonists / pharmacology
  • Animals
  • Aorta / metabolism
  • Binding, Competitive / drug effects
  • Cerebral Cortex / metabolism
  • Liver / metabolism
  • Membranes / metabolism
  • Myocardium / metabolism
  • Prazosin / pharmacology
  • Radioligand Assay
  • Receptors, Adrenergic, alpha-1 / classification
  • Receptors, Adrenergic, alpha-1 / drug effects
  • Receptors, Adrenergic, alpha-1 / metabolism*
  • Spleen / metabolism
  • Swine

Substances

  • Adrenergic alpha-Antagonists
  • Receptors, Adrenergic, alpha-1
  • Prazosin