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Related Experiment Videos

Variable receptor affinity hypothesis.

J A Bevan1, R D Bevan, S M Shreeve

  • 1Department of Pharmacology, University of Vermont, Burlington 05405.

FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology
|April 1, 1989
PubMed
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Tissue sensitivity and alpha 1-adrenoceptor affinity for norepinephrine (NE) correlate in mammals. This explains variations in tissue response and suggests a continuous receptor affinity, not distinct types.

Area of Science:

  • Pharmacology
  • Physiology
  • Biochemistry

Background:

  • Mammalian arteries exhibit varying contractile responses to norepinephrine (NE).
  • Alpha-1 adrenoceptors mediate responses to NE in vascular tissues.
  • Understanding receptor-ligand interactions is crucial for pharmacology and physiology.

Purpose of the Study:

  • To investigate the relationship between alpha 1-adrenoceptor affinity and tissue sensitivity to NE.
  • To determine if variations in receptor affinity explain differences in contractile responses.
  • To explore the implications of variable receptor affinity for receptor classification and physiological function.

Main Methods:

  • Comparative analysis of contractile responses to NE in arteries from three mammalian species.

Related Experiment Videos

  • Quantitative assessment of alpha 1-adrenoceptor affinity and tissue sensitivity.
  • Evaluation of factors potentially influencing adrenergic antagonist affinity.

    • Main Results:

    • Tissue sensitivity and alpha 1-adrenoceptor affinity for NE were found to covary significantly across species.
    • A quantitative relationship suggests that affinity variations largely explain sensitivity differences.
    • Evidence indicates continuous variation in affinity, challenging discrete receptor subtypes.

    Conclusions:

    • Variable receptor affinity is a key factor in tissue-specific responses to NE.
    • Continuous variation in affinity may underlie functional differences in alpha 1-adrenoceptors.
    • The hypothesis of variable receptor affinity offers a framework for understanding physiological and pathological changes.