Solubilization and characterization of alpha-2 adrenergic receptors from the human platelet and rat cerebral cortex
Alpha-2 adrenergic receptor heterogeneity has been hypothesized to explain functional and radioligand binding differences between rodent and non-rodent species. Computer analysis of the inhibition of (/sup 3/He)yohimbine binding by prazosin in the rat cerebral cortex indicates the possibility of at least two binding sites rather than negative cooperativity at a single site. There appear to be three alternative hypotheses which may explain the rodent vs. non-rodent differences. To develop the technical capability to distinguish between the above alternatives, the human platelet and rat cerebral cortex were solubilized and p-azidoclonidine (AZC) an alpha-2 receptor photoaffinity label was synthesized. Soluble preparations from both species showed saturable, high affinity (/sup 3/He)yohimbine binding. The rank order of potencies for various adrenergic agonists and antagonists are consistent with the notion that (/sup 3/He)yohimbine binding detected solubilized alpha-2 receptors. Sucrose density gradient centrifugation of soluble alpha-2 receptors indicated no significant molecular size difference. (/sup 3/H)AZC binding to the alpha-2 receptor in the rat cerebral cortex demonstrated high affinity saturability and the correct rank order of potency.
- Research Organization:
- Missouri Univ., Columbia (USA)
- OSTI ID:
- 6108460
- Resource Relation:
- Other Information: Thesis (Ph. D.)
- Country of Publication:
- United States
- Language:
- English
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BLOOD PLATELETS
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CEREBRUM
RECEPTORS
BIOCHEMISTRY
SYMPATHOMIMETICS
AZIDO COMPOUNDS
RATS
SOLUBILITY
TRITIUM COMPOUNDS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BIOLOGICAL MATERIALS
BLOOD
BLOOD CELLS
BODY
BODY FLUIDS
BRAIN
CENTRAL NERVOUS SYSTEM
CHEMISTRY
DRUGS
KINETICS
LABELLED COMPOUNDS
MAMMALS
MATERIALS
MEMBRANE PROTEINS
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
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550201* - Biochemistry- Tracer Techniques