CHAPS solubilization of a G-protein sensitive 5-HT sub 1 A receptor from bovine hippocampus

Journal Article · Sun Jan 01 04:00:00 EST 1989 · Life Sciences; (USA)

DOI:https://doi.org/10.1016/0024-3205(89)90574-2· OSTI ID:6994832

Kline, T ^[1]; Park, H; Meyerson, L R ^[2]

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1. Mt. Sinai School of Medicine, New York, NY (USA)
2. American Cyanamid Co., Mahwah, NJ (USA)

The binding of ({sup 3}H) 8-OH-DPAT to membrane-bound 5-HT{sub 1A} receptors from bovine hippocampus was saturable and corresponded to a single high-affinity state. Solubilization of the bovine hippocampal membranes with 10 mM CHAPS containing 200 mM NaCl, renders a preparation which binds ({sup 3}H) 8-OH-DPAT with high affinity and is guanine nucleotide sensitive and ketanserin insensitive. 50% of ({sup 3}H) 8-OH-DPAT binding activity is solubilized. The presence of GMP-P(NH)P promotes a low-affinity state which is characteristic of receptors coupled to G-proteins. GMP-P(NH)P markedly accelerates the dissociation ({sup 3}H) 8-OH-DPAT from solubilized membranes while having negligible effects on association. Thus, the agonist can activate the ternary complex rather than to promote its formation. 8-OH-DPAT, WB 4101 and 5-carboxamidotryptamine dose responsively inhibit soluble ({sup 3}H) 8-OH-DPAT binding with IC{sub 50} values of 16.1, 15.6 and 1.3 nM, respectively. The CHAPS solubilized membrane preparation retains many of the ({sup 3}H) 8-OH-DPAT binding characteristics of the membrane bound form.

• OSTI ID: 6994832
• Journal Information: Life Sciences; (USA), Journal Name: Life Sciences; (USA) Vol. 45:21; ISSN 0024-3205; ISSN LIFSA
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZOLES
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
CATTLE
CELL CONSTITUENTS
CELL MEMBRANES
CENTRAL NERVOUS SYSTEM
DOMESTIC ANIMALS
DRUGS
HETEROCYCLIC COMPOUNDS
HIPPOCAMPUS
HYDROGEN COMPOUNDS
HYDROXY COMPOUNDS
INDOLES
ISOTOPE APPLICATIONS
KINETICS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PROTEINS
PYRROLES
RADIOPROTECTIVE SUBSTANCES
REACTION KINETICS
RECEPTORS
RUMINANTS
SEROTONIN
SOLUBILITY
SYMPATHOMIMETICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
TRYPTAMINES
VERTEBRATES