Dopamine D2(High) receptors moderately elevated by sertindole. 2008

Philip Seeman
Department of Pharmacology, Medical Science Building, University of Toronto, Toronto, Ontario, Canada M5S 1A8. philip.seeman@utoronto.ca

Because long-term administration of antipsychotics can cause behavioral dopamine supersensitivity, this study examined whether the antipsychotic sertindole could elicit biochemical changes indicative of dopamine supersensitivity. In rats, behavioral dopamine supersensitivity is consistently associated with an increased proportion of dopamine receptors that have high affinity for dopamine, namely D2(High), in homogenized striata. Nine days of subcutaneously injected sertindole (1.25 mg/kg/day) increased the proportion of D2(High) receptors between 186% and 215%, although the total population of D2 receptors did not change. Although the findings suggest that rats or patients treated with sertindole might exhibit behavioral dopamine supersensitivity, the drug-induced increase in D2(High) receptors was less than that previously found with haloperidol.

UI MeSH Term Description Entries
D007093 Imidazoles Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D010078 Oxazines Six-membered heterocycles containing an oxygen and a nitrogen.
D004294 Domperidone A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. Apo-Domperidone,Domidon,Domperidon,Domperidon AL,Domperidon Hexal,Domperidon Stada,Domperidon-TEVA,Domperidona Gamir,Domperidone Maleate,Domperidone Maleate (1:1),Domperidone Monohydrochloride,Gastrocure,Motilium,Nauzelin,Novo-Domperidone,Nu-Domperidone,PMS-Domperidone,Péridys,R-33,812,R-33812,Ratio-Domperidone,Apo Domperidone,Domperidon TEVA,Gamir, Domperidona,Hexal, Domperidon,Maleate, Domperidone,Monohydrochloride, Domperidone,Novo Domperidone,Nu Domperidone,PMS Domperidone,R33,812,R33812,Ratio Domperidone,Stada, Domperidon
D006150 Guanine Nucleotides Guanine Nucleotide,Guanosine Phosphates,Nucleotide, Guanine,Nucleotides, Guanine,Phosphates, Guanosine
D006220 Haloperidol A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279) Haldol
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
D014150 Antipsychotic Agents Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. Antipsychotic,Antipsychotic Agent,Antipsychotic Drug,Antipsychotic Medication,Major Tranquilizer,Neuroleptic,Neuroleptic Agent,Neuroleptic Drug,Neuroleptics,Tranquilizing Agents, Major,Antipsychotic Drugs,Antipsychotic Effect,Antipsychotic Effects,Antipsychotics,Major Tranquilizers,Neuroleptic Agents,Neuroleptic Drugs,Tranquillizing Agents, Major,Agent, Antipsychotic,Agent, Neuroleptic,Drug, Antipsychotic,Drug, Neuroleptic,Effect, Antipsychotic,Major Tranquilizing Agents,Major Tranquillizing Agents,Medication, Antipsychotic,Tranquilizer, Major
D017072 Neostriatum The phylogenetically newer part of the CORPUS STRIATUM consisting of the CAUDATE NUCLEUS and PUTAMEN. It is often called simply the striatum.

Related Publications

Philip Seeman
February 1988, Science (New York, N.Y.),
Philip Seeman
February 1988, Science (New York, N.Y.),
Philip Seeman
May 2002, Cerebral cortex (New York, N.Y. : 1991),
Philip Seeman
November 2006, Journal of proteome research,
Philip Seeman
August 1994, The Journal of pharmacology and experimental therapeutics,
Philip Seeman
January 1998, Advances in pharmacology (San Diego, Calif.),
Copied contents to your clipboard!