BIOMAT Database Logo BIOMAT Database Logo

In vivo dopamine-D2 and serotonin-5-HT2 receptor binding study of risperidone and haloperidol. 1994

T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
Laboratory of Biological Psychiatry, University Hospitals of Cleveland, OH 44106.

An in vivo receptor binding technique was applied to evaluate the affinities of risperidone and haloperidol for dopamine-D2 receptors (D2) and serotonin-5-HT2 receptors (5-HT2) in rat brain with [3H]YM-09151-2 and [3H]ketanserin as selective ligands. Radioactivities were obtained in the striatum frontal cortex, and cerebellum of the rats treated with the ligands. Time course study of receptor occupancy at 25 to 250 min after single doses of the drugs (1 mg/kg, IP) showed higher 5-HT2 occupancy in the frontal cortex and lower D2 occupancy in the striatum by risperidone than by haloperidol. Dose-response analysis of receptor occupancy revealed risperidone demonstrated higher binding affinity for 5-HT2 than for D2, while the reverse was observed with haloperidol. It appeared that risperidone (1 mg/kg, IP), but not haloperidol (1 mg/kg, IP), demonstrated regional selectivity in D2 occupancy favouring frontal cortex more than the striatum. That risperidone displayed a higher ratio of 5-HT2 to D2 in occupancy than haloperidol is in agreement with the previous findings obtained in vitro.

UI MeSH Term Description Entries
D007555 Isoxazoles Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions. Isoxazole
D007650 Ketanserin A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients. 3-(2-(4-(4-Fluorobenzoyl)piperidinol)ethyl)-2,4(1H,3H)-quinazolinedione,R-41,468,R-41468,R 41,468,R 41468,R41,468,R41468
D008024 Ligands A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed) Ligand
D008297 Male Males
D010880 Piperidines A family of hexahydropyridines.
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
D002531 Cerebellum The part of brain that lies behind the BRAIN STEM in the posterior base of skull (CRANIAL FOSSA, POSTERIOR). It is also known as the "little brain" with convolutions similar to those of CEREBRAL CORTEX, inner white matter, and deep cerebellar nuclei. Its function is to coordinate voluntary movements, maintain balance, and learn motor skills. Cerebella,Corpus Cerebelli,Parencephalon,Cerebellums,Parencephalons
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
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

Related Publications

T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
Risperidone, a new antipsychotic with serotonin 5-HT2 and dopamine D2 antagonistic properties.
January 1992, Clinical neuropharmacology,
T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
Suppression of alcohol preference in rats induced by risperidone, a serotonin 5-HT2 and dopamine D2 receptor antagonist.
January 1993, Brain research bulletin,
T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
5-HT2 and D2 dopamine receptor occupancy in the living human brain. A PET study with risperidone.
January 1993, Psychopharmacology,
T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
Effect of clozapine and risperidone on 5-HT2 and D2-dopamine receptor binding in the post-mortem human brain. An autoradiographic study.
March 1995, European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology,
T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
In vitro and in vivo binding of (E)- and (Z)-N-(iodoallyl)spiperone to dopamine D2 and serotonin 5-HT2 neuroreceptors.
January 1990, Life sciences,
T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
Positron emission tomography studies on D2 and 5-HT2 receptor binding in risperidone-treated schizophrenic patients.
February 1995, Journal of clinical psychopharmacology,
T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
A pharmacological, pharmacokinetic and clinical overview of risperidone, a new antipsychotic that blocks serotonin 5-HT2 and dopamine D2 receptors.
March 1995, International clinical psychopharmacology,
T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.
August 1994, Journal of medicinal chemistry,
T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
A PET study of D2 and 5-HT2 receptor occupancy induced by risperidone in poor metabolizers of debrisoquin and risperidone.
June 1995, Psychopharmacology,
T Sumiyoshi, and H Kido, and H Sakamoto, and K Urasaki, and K Suzuki, and N Yamaguchi, and H Mori, and K Shiba, and K Yokogawa
An efficient synthesis of risperidone via stille reaction: antipsychotic, 5-HT2, and dopamine-D2-antagonist.
September 2005, Archives of pharmacal research,
Copied contents to your clipboard!