Heterogeneity of alpha-2 adrenergic receptors.

Article Details

Citation

Copy to clipboard

Bylund DB

Heterogeneity of alpha-2 adrenergic receptors.

Pharmacol Biochem Behav. 1985 May;22(5):835-43.

PubMed ID

2989948 [ View in PubMed

]

Abstract

Alpha adrenergic receptors are subdivided into alpha-1 and alpha-2 subtypes on the basis of their pharmacologic properties. An evaluation of data from radioligand binding and functional experiments indicates that the receptors classified as alpha-2 are not a homogeneous group. The best example of this heterogeneity is the differences in the pharmacologic properties of alpha-2 receptors in rodent and non-rodent mammalian species. Prazosin generally has a high affinity for rodent alpha-2 receptors, but a low affinity for non-rodent alpha-2 receptors, while oxymetazoline is more potent at non-rodent alpha-2 receptors. A definition of alpha-2 adrenergic receptor subtypes is proposed with prazosin having a lower affinity (200-300 nM) at alpha-2A receptors and a higher affinity (5-10 nM) at alpha-2B receptors. Using this definition, the human platelet appears to have only the alpha-2A subtype, while all the receptors in the neonatal rat lung are of the alpha-2B subtype. The rat brain has roughly equal amounts of alpha-2A and -2B receptors while in the rat submandibular gland, about 85% of the receptors are alpha-2A. The ability to pharmacologically define putative alpha-2 adrenergic receptor subtypes should promote the development of additional subtype selective drugs which will increase our understanding of adrenergic pharmacology and may provide new therapeutic approaches.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Prazosin	Alpha-2A adrenergic receptor	Protein	Humans	Unknown	Binder	Details
Prazosin	Alpha-2B adrenergic receptor	Protein	Humans	Unknown	Binder	Details