(/sup 3/)tetrahydrotrazodone binding. Association with serotonin binding sites

Journal Article · Sun May 01 00:00:00 EDT 1983 · Mol. Pharmacol.; (United States)

OSTI ID:7013660

Kendall, D A; Taylor, D P; Enna, S J

High (17 nM) and low (603 nM) affinity binding sites for (/sup 3/)tetrahydrotrazodone ((/sup 3/) THT), a biologically active analogue of trazodone, have been identified in rat brain membranes. The substrate specificity, concentration, and subcellular and regional distributions of these sites suggest that they may represent a component of the serotonin transmitter system. Pharmacological analysis of (/sup 3/)THT binding, coupled with brain lesion and drug treatment experiments, revealed that, unlike other antidepressants, (/sup 3/) THT does not attach to either a biogenic amine transporter or serotonin binding sites. Rather, it would appear that (/sup 3/)THT may be an antagonist ligand for the serotonin binding site. This probe may prove of value in defining the mechanism of action of trazodone and in further characterizing serotonin receptors.

• Research Organization: Univ. of Texas, Medical School, Houston
• OSTI ID: 7013660
• Journal Information: Mol. Pharmacol.; (United States), Vol. 23:3
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
PSYCHOTROPIC DRUGS
PHARMACOLOGY
TISSUE DISTRIBUTION
SEROTONIN
RECEPTORS
TRITIUM COMPOUNDS
BRAIN
CELL MEMBRANES
RATS
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZOLES
BODY
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
DISTRIBUTION
DRUGS
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
INDOLES
LABELLED COMPOUNDS
MAMMALS
MEMBRANES
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PYRROLES
RADIOPROTECTIVE SUBSTANCES
RODENTS
SYMPATHOMIMETICS
TRYPTAMINES
VERTEBRATES
551001* - Physiological Systems- Tracer Techniques