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Title: Solubilization and characterization of alpha-2 adrenergic receptors from the human platelet and rat cerebral cortex

Abstract

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.

Authors:
Publication Date:
Research Org.:
Missouri Univ., Columbia (USA)
OSTI Identifier:
6108460
Resource Type:
Thesis/Dissertation
Resource Relation:
Other Information: Thesis (Ph. D.)
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; BLOOD PLATELETS; BIOCHEMICAL REACTION KINETICS; 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; PROTEINS; REACTION KINETICS; RODENTS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Kawahara, R S. Solubilization and characterization of alpha-2 adrenergic receptors from the human platelet and rat cerebral cortex. United States: N. p., 1984. Web.
Kawahara, R S. Solubilization and characterization of alpha-2 adrenergic receptors from the human platelet and rat cerebral cortex. United States.
Kawahara, R S. 1984. "Solubilization and characterization of alpha-2 adrenergic receptors from the human platelet and rat cerebral cortex". United States.
@article{osti_6108460,
title = {Solubilization and characterization of alpha-2 adrenergic receptors from the human platelet and rat cerebral cortex},
author = {Kawahara, R S},
abstractNote = {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.},
doi = {},
url = {https://www.osti.gov/biblio/6108460}, journal = {},
number = ,
volume = ,
place = {United States},
year = {Sun Jan 01 00:00:00 EST 1984},
month = {Sun Jan 01 00:00:00 EST 1984}
}

Thesis/Dissertation:
Other availability
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