Nucleotide interactions with 5-HT1A binding sites directly labeled by [3H]-8-hydroxy-2-(DI-n-propylamino)tetralin ([3H]-8-OH-DPAT). 1986

J R Schlegel, and S J Peroutka

Nucleotide interactions were examined at 5-hydroxytryptamine1A (5-HT1A) binding sites labeled by [3H]-8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). At a 10(-4) M concentration, GTP and GDP decreased specific binding of 0.4 nM [3H]-8-OH-DPAT to 47 +/- 4 and 61 +/- 1% of control values respectively. This nucleotide effect was significantly greater (P less than 0.005) than observed at total 5-HT1 binding sites labeled by 1.5 nM [3H]-5-HT. GMP and adenine nucleotides had a minimal effect on [3H]-8-OH-DPAT binding at concentrations less than 10(-3) M. Saturation experiments demonstrated that 10(-4) M GTP increased the KD of [3H]-8-OH-DPAT for 5-HT1A binding sites (0.79 to 2.7 nM) without changing the number of binding sites (1.98 to 1.93 pmoles/g tissue). The Ki values of classic and novel putative 5-HT agonists were increased 2- to 4-fold in the presence of 10(-4) M GTP. Affinities of 5-HT antagonists for the [3H]-8-OH-DPAT site were not affected by the addition of 10(-4) M GTP to the binding assay.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D009281 Naphthalenes Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.
D011985 Receptors, Serotonin Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action. 5-HT Receptor,5-HT Receptors,5-Hydroxytryptamine Receptor,5-Hydroxytryptamine Receptors,Receptors, Tryptamine,Serotonin Receptor,Serotonin Receptors,Tryptamine Receptor,Tryptamine Receptors,Receptors, 5-HT,Receptors, 5-Hydroxytryptamine,5 HT Receptor,5 HT Receptors,5 Hydroxytryptamine Receptor,5 Hydroxytryptamine Receptors,Receptor, 5-HT,Receptor, 5-Hydroxytryptamine,Receptor, Serotonin,Receptor, Tryptamine,Receptors, 5 HT,Receptors, 5 Hydroxytryptamine
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D006150 Guanine Nucleotides Guanine Nucleotide,Guanosine Phosphates,Nucleotide, Guanine,Nucleotides, Guanine,Phosphates, Guanosine
D006153 Guanosine Diphosphate A guanine nucleotide containing two phosphate groups esterified to the sugar moiety. GDP,Guanosine 5'-Diphosphate,Guanosine 5'-Trihydrogen Diphosphate,5'-Diphosphate, Guanosine,5'-Trihydrogen Diphosphate, Guanosine,Diphosphate, Guanosine,Diphosphate, Guanosine 5'-Trihydrogen,Guanosine 5' Diphosphate,Guanosine 5' Trihydrogen Diphosphate
D006157 Guanosine Monophosphate A guanine nucleotide containing one phosphate group esterified to the sugar moiety and found widely in nature. 5'-Guanylic Acid,Guanosine 5'-Monophosphate,5'-GMP,Guanylic Acid,5' Guanylic Acid,5'-Monophosphate, Guanosine,Acid, 5'-Guanylic,Acid, Guanylic,Guanosine 5' Monophosphate,Monophosphate, Guanosine
D006160 Guanosine Triphosphate Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety. GTP,Triphosphate, Guanosine
D000262 Adenylyl Cyclases Enzymes of the lyase class that catalyze the formation of CYCLIC AMP and pyrophosphate from ATP. Adenyl Cyclase,Adenylate Cyclase,3',5'-cyclic AMP Synthetase,Adenylyl Cyclase,3',5' cyclic AMP Synthetase,AMP Synthetase, 3',5'-cyclic,Cyclase, Adenyl,Cyclase, Adenylate,Cyclase, Adenylyl,Cyclases, Adenylyl,Synthetase, 3',5'-cyclic AMP
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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