High-affinity cannabinoid binding site in brain: A possible marijuana receptor

Thesis/Dissertation · Fri Jan 01 00:00:00 EST 1988

OSTI ID:5547702

Nye, J S

The mechanism by which delta{sup 9} tetrahydrocannabinol (delta{sup 9}THC), the major psychoactive component of marijuana or hashish, produces its potent psychological and physiological effects is unknown. To find receptor binding sites for THC, we designed a water-soluble analog for use as a radioligand. 5{prime}-Trimethylammonium-delta{sup 8}THC (TMA) is a positively charged analog of delta-{sup 8}THC modified on the 5{prime} carbon, a portion of the molecule not important for its psychoactivity. We have studied the binding of ({sup 3}H)-5{prime}-trimethylammonium-delta-{sup 8}THC (({sup 3}H)TMA) to rat neuronal membranes. ({sup 3}H)TMA binds saturably and reversibly to brain membranes with high affinity to apparently one class of sites. Highest binding site density occurs in brain, but several peripheral organs also display specific binding. Detergent solubilizes the sites without affecting their pharmacologial properties. Molecular sieve chromatography reveals a bimodal peak of ({sup 3}H)TMA binding activity of approximately 60,000 daltons apparent molecular weight.

• Research Organization: Johns Hopkins Univ., Baltimore, MD (USA)
• OSTI ID: 5547702
• Resource Relation: Other Information: Thesis (Ph. D.)
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
MARIHUANA
RECEPTORS
AFFINITY
BIOCHEMICAL REACTION KINETICS
BRAIN
CELL MEMBRANES
LIGANDS
MOLECULAR WEIGHT
NERVES
RATS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMALS
BODY
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM
HERBS
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
MAGNOLIOPHYTA
MAGNOLIOPSIDA
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANS
PLANTS
PROTEINS
REACTION KINETICS
RODENTS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques