[3H]Spiperone labels non-cyclase-linked dopamine receptors in the ventral tegmental area of rat brain. 1982

A L Gundlach, and D McDonald, and P M Beart

The binding of [3H]spiperone, a neuroleptic/dopamine receptor ligand, to membranes of the ventral tegmental area of the rat was studied in vitro and found to be rapid, saturable, reversible, and of high affinity. Specific binding was displaced by the dopaminergic agonists dopamine, apomorphine, and 2-amino-6,7-dihydroxytetralin, and stereospecifically by the neuroleptic drugs butaclamol and flupenthixol. Bromocryptine and other ergots displaced the binding, as did the D-2 antagonists domperidone, molindone, metoclopramide, and sulpiride. Noradrenergic, histaminergic, and serotonergic components of the binding were not detected in displacement studies with various agonists and antagonists. These data are consistent with the hypothesis that [3H]spiperone labels dopamine receptors in the ventral tegmental area that are not linked to adenylate cyclase and are therefore likely to be of the D-2 type.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D011954 Receptors, Dopamine Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells. Dopamine Receptors,Dopamine Receptor,Receptor, Dopamine
D002090 Butyrophenones Compounds containing phenyl-1-butanone.
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
D001667 Binding, Competitive The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements. Competitive Binding
D013134 Spiperone A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA. Spiroperidol,Spiroperone
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D013681 Tegmentum Mesencephali Portion of midbrain situated under the dorsal TECTUM MESENCEPHALI. The two ventrolateral cylindrical masses or peduncles are large nerve fiber bundles providing a tract of passage between the FOREBRAIN with the HINDBRAIN. Ventral MIDBRAIN also contains three colorful structures: the GRAY MATTER (PERIAQUEDUCTAL GRAY), the black substance (SUBSTANTIA NIGRA), and the RED NUCLEUS. Accessory Oculomotor Nuclei,Annular Nucleus,Darkshevich's Nucleus,Interstitial Nucleus of Cajal,Mesencephalic Tegmentum,Mesencephalic Trigeminal Nucleus,Midbrain Tegmentum,Midbrain Trigeminal Nucleus,Nucleus Annularis,Nucleus Nervi Trochlearis,Nucleus Sagulum,Nucleus Tractus Mesencephalici Nervi Trigemini,Nucleus of Darkschewitsch,Peripeduncular Nucleus,Sagulum Nucleus,Tegmentum of Midbrain,Trochlear Nucleus,Ventral Tegmental Nucleus,Annulari, Nucleus,Annularis, Nucleus,Cajal Interstitial Nucleus,Darkschewitsch Nucleus,Darkshevich Nucleus,Darkshevichs Nucleus,Mesencephali, Tegmentum,Mesencephalic Tegmentums,Mesencephalus, Tegmentum,Midbrain Tegmentums,Nervi Trochleari, Nucleus,Nervi Trochlearis, Nucleus,Nuclei, Accessory Oculomotor,Nucleus Annulari,Nucleus Nervi Trochleari,Nucleus Sagulums,Nucleus, Annular,Nucleus, Darkshevich's,Nucleus, Mesencephalic Trigeminal,Nucleus, Midbrain Trigeminal,Nucleus, Peripeduncular,Nucleus, Sagulum,Nucleus, Trochlear,Nucleus, Ventral Tegmental,Oculomotor Nuclei, Accessory,Sagulum, Nucleus,Sagulums, Nucleus,Tegmental Nucleus, Ventral,Tegmentum Mesencephalus,Tegmentum, Mesencephalic,Tegmentum, Midbrain,Tegmentums, Mesencephalic,Tegmentums, Midbrain,Trigeminal Nucleus, Mesencephalic,Trigeminal Nucleus, Midbrain,Trochleari, Nucleus Nervi,Trochlearis, Nucleus Nervi
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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