Role of the inhibitory guanine nucleotide regulatory protein in high affinity. cap alpha. /sub 2/ adrenergic agonist binding
Thesis/Dissertation
·
OSTI ID:7027082
The purpose of this study was to determine whether regulatory protein, N/sub i/ was required for high affinity agonist binding to the a/sub 2/ adrenergic receptor in human platelet membranes. Human platelet membranes treated under alkaline conditions (pH 11.5) exhibited a selective and complete loss of high affinity agonist binding as measured by the parital agonist (/sup 3/H)-p-aminoclonidine and full agonist (/sup 3/H)UK 14,304 in direct binding studies. The binding parameters for (/sup 3/H)UK 14,304 are as follows: for control platelet membranes, the K/sub d/ was 0.88 +/- 0.17 and nM and the B/sub max/ was 280 +/- 20 fmol/mg compared to 1.89 +/- 0.34 nM and 75 fmol/mg for pH 11.5 treated membranes. For (/sup 3/H)p-aminoclonidine, the data for pH 11.5 treated membranes is as follows: B/sub max/ = 100 +/- 20 fmol/mg, K/sub d/ = 3.4 +/- 0.1 nM, compared to control membranes: (best fit with a two site fit) K/sub d1/ = 0.7 nM, K/sub d2/ = 8 nM, B/sub max1/ = 76 fmol/mg, B/sub max2/ = 198 fmol/mg. The ..cap alpha../sub 2/ antagonists, (/sup 3/H)yohimbine, was used to assess the presence of the receptor.
- Research Organization:
- Michigan Univ., Ann Arbor (USA)
- OSTI ID:
- 7027082
- Country of Publication:
- United States
- Language:
- English
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·
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Related Subjects
550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL FUNCTIONS
BIOLOGICAL MATERIALS
BLOOD
BLOOD CELLS
BLOOD PLATELETS
BODY FLUIDS
CELL CONSTITUENTS
CELL MEMBRANES
DRUGS
FUNCTIONS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
MAN
MATERIALS
MEMBRANE PROTEINS
MEMBRANES
ORGANIC COMPOUNDS
PRIMATES
PROTEINS
REACTION KINETICS
RECEPTORS
SYMPATHOMIMETICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL FUNCTIONS
BIOLOGICAL MATERIALS
BLOOD
BLOOD CELLS
BLOOD PLATELETS
BODY FLUIDS
CELL CONSTITUENTS
CELL MEMBRANES
DRUGS
FUNCTIONS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
MAN
MATERIALS
MEMBRANE PROTEINS
MEMBRANES
ORGANIC COMPOUNDS
PRIMATES
PROTEINS
REACTION KINETICS
RECEPTORS
SYMPATHOMIMETICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES