/sup 125/I-Bolton-Hunter-8-methoxy-2-(N-propyl-N-propylamino)tetralin as a new selective radioligand of 5-HT1A sites in the rat brain. In vitro binding and autoradiographic studies

Journal Article · Mon Feb 01 04:00:00 EST 1988 · J. Pharmacol. Exp. Ther.; (United States)

OSTI ID:5243663

Gozlan, H; Ponchant, M; Daval, G; Verge, D; Menard, F; Vanhove, A; Beaucourt, J P; Hamon, M

In vitro binding assays with /sup 125/I-(8-methoxy-2-(N-propyl-N-(3'-iodo-4'-hydroxyphenyl)-propionamido -N'- propylamino) tetralin) (/sup 125/I-BH-8-MeO-N-PAT), a /sup 125/I-labeled derivative of the potent serotonin (5-HT) agonist 8-hydroxy-2-(di-n-propylamino)tetralin ((/sup 3/H)-8-OH-DPAT), showed that this compound recognized specific sites with nanomolar affinity for 5-HT and 5-HT1A ligands such as spiroxatrine, ipsapirone, buspirone and gepirone in rat hippocampal membranes. Comparison of the binding characteristics of /sup 125/I-BH-8-MeO-N-PAT with those of (/sup 3/H)-8-OH-DPAT revealed striking similarities: at the hippocampal level, both binding sites exhibited nanomolar affinity for their respective ligands and the same Bmax; their pharmacological profiles defined by the inhibition of each bound ligand by a series of 26 serotonin, dopamine- or norepinephrine-related agonists and antagonists were identical; and their regional distributions examined by membrane binding assays and autoradiography of labeled brain sections were highly correlated. These observations indicate that /sup 125/I-BH-8-MeO-N-PAT is the first /sup 125/I-reversible ligand for the selective labeling of 5-HT1A sites in the rat central nervous system.

• Research Organization: Institut National de la Sante et de La Recherche Medicale U. 288, Paris (France)
• OSTI ID: 5243663
• Journal Information: J. Pharmacol. Exp. Ther.; (United States), Journal Name: J. Pharmacol. Exp. Ther.; (United States) Vol. 244:2; ISSN JPETA
• Country of Publication: United States
• Language: English

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550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AUTORADIOGRAPHY
AZAARENES
AZOLES
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
DAYS LIVING RADIOISOTOPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
IN VITRO
INDOLES
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
KINETICS
LABELLED COMPOUNDS
LIGANDS
MAMMALS
MEMBRANE PROTEINS
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PROTEINS
PYRROLES
RADIOISOTOPES
RADIOPROTECTIVE SUBSTANCES
RATS
REACTION KINETICS
RECEPTORS
RODENTS
SEROTONIN
STRUCTURE-ACTIVITY RELATIONSHIPS
SYMPATHOMIMETICS
TRITIUM COMPOUNDS
TRYPTAMINES
VERTEBRATES