Characterization of a novel serotonin receptor coupled to adenylate cyclase in the hybrid neuroblastoma cell line NCB. 20

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

OSTI ID:7003290

Conner, D A

Pharmacological characterization of the serotonin activation of adenylate cyclase in membrane preparation using over 40 serotonergic and non-serotonergic compounds demonstrated that the receptor mediating the response was distinct from previously described mammalian serotonin receptors. Agonist activity was only observed with tryptamine and ergoline derivatives. Potent antagonism was observed with several ergoline derivatives and with compounds such as mianserin and methiothepine. A comparison of the rank order of potency of a variety of compounds for the NCB.20 cell receptor with well characterized mammalian and non-mammalian serotonin receptors showed a pharmacological similarity, but not identity, with the mammalian 5-HT{sub 1C} receptor, which modulates phosphatidylinositol metabolism, and with serotonin receptors in the parasitic trematodes Fasciola hepatica and Schistosoma mansoni, which are coupled to adenylate cyclase. Equilibrium binding analysis utilizing ({sup 3}H)serotonin, ({sup 3}H)lysergic acid diethylamide or ({sup 3}H)dihydroergotamine demonstrated that there are no abundant high affinity serotonergic sites, which implies that the serotonin activation of adenylate cyclase is mediated by receptors present in low abundance. Incubation of intact NCB.20 cells with serotinin resulted in a time and concentration dependent desensitization of the serotonin receptor.

• Research Organization: Stanford Univ., CA (USA)
• OSTI ID: 7003290
• Resource Relation: Other Information: Thesis (Ph. D.)
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
CYCLASES
ENZYME ACTIVITY
RECEPTORS
CHEMICAL COMPOSITION
SEROTONIN
BIOCHEMICAL REACTION KINETICS
CELL MEMBRANES
DOSE-RESPONSE RELATIONSHIPS
LYSERGIC ACID
TIME DEPENDENCE
TRACER TECHNIQUES
TREMATODES
TRITIUM COMPOUNDS
TUMOR CELLS
ALKALOIDS
AMINES
ANIMAL CELLS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZOLES
CARBOXYLIC ACIDS
CELL CONSTITUENTS
DRUGS
ENZYMES
HELMINTHS
HETEROCYCLIC ACIDS
HETEROCYCLIC COMPOUNDS
HYDROGEN COMPOUNDS
HYDROXY COMPOUNDS
INDOLES
ISOTOPE APPLICATIONS
KINETICS
LYASES
MEMBRANE PROTEINS
MEMBRANES
NEUROREGULATORS
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PLATYHELMINTHS
PROTEINS
PYRROLES
RADIOPROTECTIVE SUBSTANCES
REACTION KINETICS
SYMPATHOMIMETICS
TRYPTAMINES
550201* - Biochemistry- Tracer Techniques