Dopamine receptor subtypes

There are five primary dopamine receptor subtypes 218... 

TABLE 12-3 Properties of human dopamine receptor subtypes... 

Dopamine receptors are found primarily in brain, although they also exist in kidney [33]. Two subtypes of dopamine receptor were initially identified based primarily on differences in their drug specificities and signaling mechanisms. D receptors were found to stimulate adenylyl cyclase activity, while D2 receptors inhibited this enzyme (Fig. 12-6). Subsequently, multiple Dr and D2-like receptors were identified by molecular cloning (Table 12-3) [33], All dopamine receptor subtypes are... 

There is still some controversy over the precise anatomical location of the dopamine receptor subtypes, but there is now evidence that the D2 receptors are located presynaptically on the corticostriatal neurons and postsynaptically in the striatum and substantia nigra. Conversely, the receptors are found presynaptically on nigrostriatal neurons, and postsynaptically in the cortex. It is possible to differentiate these receptor types on the basis of their agonist and antagonist affinities. 

A. Hilditch, G. M. Drew (1985). Peripheral dopamine receptor subtypes—a closer look. Trends Pharmacol. Sci. 6 396 00. 

Shows a 100-fold lower affinity for the receptor (approximately equivalent to that of risperidone and haloperidol) than for the other dopamine receptor subtypes. 

The role of these agents, either as primary or adjunctive treatments for mood disorders, has yet to be fully explored ( 106, 108, 279, 280 and 281). Theories have included the differential effects of clozapine on dopamine receptor subtypes (e.g., increased activity at the receptors, which exist in high density in the limbic system) and the greater 5-HT2 to D2 antagonism of most novel agents in comparison with neuroleptics (282). More recently, controlled trials indicate that novel antispychotics (NAPs) may play an important and perhaps unique role for more severe, psychotic, and/or refractory mood disorders ( 112, 283, 384). 

Holmes A, Lachowicz JE, Sibley DR Phenotypic analysis of dopamine receptor knockout mice recent insights into the functional specificity of dopamine receptor subtypes. Neuropharmacology 2004 47 1117. [PMID 15567422]... 

Zhang A, NeumeyerJL, Baldessarini RJ. Recent progress in development of dopamine receptor subtype-selective agents Potential therapeutics for neurological and psychiatric disorders. Chem Rev 2007 107 274. 

Dopaminergic Mouse Mutants Investigating the Roles of the Different Dopamine Receptor Subtypes and the Dopamine Transporter Shirlee Tan, Bettina Hermann, and Emiliana Borrelli... 

There are a number of reasons to try to characterize dopamine receptor in addition to the fact that it is fashionable. Two of the major reasons well described by Goldberg and Kohli are (1) the importance of dopamine receptors subtypes responsible for physiological and pharmacological actions and (2) the utilization of the concept of selective dopamine receptors in the design and characterization of new drugs for cardiovascular and renal therapies. 

To carry out design it is required, by definition, that an end point be identified. That is, what is the therapeutic goal Or, on the molecular level, what is the target for the drug The confusion over dopamine receptor subtypes will be commented on by others at this symposium but represents a serious obstacle to design of selective dopamine agonists. A focus on peripheral agonists simplifies matters, for at least in this... 

Requip Ropinirole HC1 0.25,0.5,1,2,3,4, 5 mg Tablet Parkinson s disease A nonergoline dopamine Croscarmellose Na, lactose agonist with high hydrous, magnesium stearate, relative in vitro MCC specificity and full intrinsic activity at the D2 and D3 dopamine receptor subtypes GSK... 

Moran-Gates, T., Grady, C., Park, Y., Baldessarim, R., Tarazi, F. (2007). Effects of risperidone on dopamine receptor subtypes in developing rat brain. European Neuropsychopharmacology, 17, 444—455. 

Filloux F, Dawson TM, Wamsley JK. 1988. Localization of nigrostriatal dopamine receptor subtypes and adenylate cyclase. Brain Res Bull 20 447-459. 

Hess EJ, Bracha HS, Kleinman JE, Creese I. 1987. Dopamine receptor subtype imbalance in schizophrenia. Life Sci 40 1487-1497. 

Huntley GW, Morrison JH, Prikhozhan A, Sealfon SC. 1992. Localization of multiple dopamine receptor subtype mRNAs in human and monkey motor cortex and striatum. Brain Res Mol Brain Res 15 181-188. 

Le Moine C, Gaspar P. 1998. Subpopulations of cortical GABAergic intemeurons differ by their expression of D1 and D2 dopamine receptor subtypes. Brain Res Mol Brain... 

Sidhu A, Niznik HB. 2000. Coupling of dopamine receptor subtypes to multiple and diverse G proteins. Int J Dev... 

Surmeier DJ, Eberwine J, Wilson CJ, Cao Y, Stefani A, Kitai ST (1992) Dopamine receptor subtypes colocalize in rat striatonigral neurons. Proc Natl Acad Sci USA 59 10178-10182. 

Brunig I, Sommer M, Hatt H, Bormann J (1999) Dopamine receptor subtypes modulate olfactory bulb gamma-aminobutyric acid type A receptors. Proc Natl Acad Sci USA 96 2456-2460. 

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