Synthesis and characterization of a radiolabeled derivative of the phencyclidine/N-methyl-D-aspartate receptor ligand (+)MK-801 with high specific radioactivity

Journal Article · Fri Jan 01 00:00:00 EST 1988 · Life Sci.; (United States)

DOI:https://doi.org/10.1016/0024-3205(88)90541-3· OSTI ID:6292660

Keana, J F.W.; Scherz, M W; Quarum, M; Sonders, M S; Weber, E

A (/sup 3/H)-labelled derivative of the drug (+)MK-801 with a high specific radioactivity was synthesized by first preparing a tribromo derivative of (+)MK-801 followed by catalytic reduction in the presence of (/sup 3/H)-gas and subsequent purification of the radioactive product by reversed-phase high performance liquid chromatography (RP-HPLC). This resulted in pure (+) (/sup 3/H)MK-801 with a specific radioactivity of 97 Ci/mmol. The (+) (/sup 3/H)MK-801 was shown to interact with high affinity and selectivity with the phencyclidine (PCP) receptor in guinea pig brain membrane suspensions. The PCP receptor is associated with a cation channel that is chemically gated by glutamate and N-methyl-D-aspartate (NMDA). Drugs that interact with the PCP receptor block this channel. The (+) (/sup 3/H)MK-801 described here will be useful to investigate the biochemistry of PCP/NMDA receptors in experiments where a high specific radioactivity is essential.

• Research Organization: Univ. of Oregon, Eugene (USA)
• OSTI ID: 6292660
• Journal Information: Life Sci.; (United States), Vol. 43:12
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
PIPERIDINES
CHEMICAL PREPARATION
AFFINITY
BIOCHEMICAL REACTION KINETICS
BRAIN
CELL MEMBRANES
CHEMICAL COMPOSITION
GUINEA PIGS
LIGANDS
LIQUID COLUMN CHROMATOGRAPHY
RADIOACTIVITY
RECEPTORS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
AMINES
ANIMALS
AZINES
BODY
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM
CHROMATOGRAPHY
HETEROCYCLIC COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PROTEINS
PYRIDINES
REACTION KINETICS
RODENTS
SEPARATION PROCESSES
SYNTHESIS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques