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*  F15063, a potential antipsychotic with D2/D3 antagonist, 5-HT 1A agonist and D4 partial agonist properties. I. In vitro...
... receptors in striatum. CONCLUSIONS AND IMPLICATIONS F15063 antagonised dopamine D(2)/D(3) receptors, a property underlying its ... KEY RESULTS Affinities (receptor and pK(i) values) of F15063 were: rD(2) 9.38; hD(2L) 9.44; hD(2S) 9.25; hD(3) 8.95; hD(4) 8.81 ... F15063 acted as a partial agonist for [(35)S]GTP gamma S binding at hD(4) (29%, 8.15) and h5-HT(1D) receptors (35%, 7.68). In ... F15063 antagonised dopamine-activated G-protein activation at hD(2), rD(2) and hD(3) receptors with potency (pK (b) values 9.19 ...
  https://www.semanticscholar.org/paper/F15063%2C-a-potential-antipsychotic-with-D2%2FD3-5-HT-Newman-Tancredi-Assi%C3%A9/22ff982b3d178074c91f9b03044e1f51c4ce1c28
*  Dopamine receptor - Wikipedia
... unless blocked by a receptor antagonist or a synthetic partial agonist. D3 is encoded by the Dopamine receptor D3 gene (DRD3). ... D4-adrenoceptor α1B D4-adrenoceptor β1 Dopamine receptor D1 and Dopamine receptor D5 are Gs coupled receptors that stimulate ... D4 is encoded by the Dopamine receptor D4 gene (DRD4). The D4 receptor gene displays polymorphisms that differ in a variable ... D1-adenosine A1 D1-D2 dopamine receptor heteromer D1-D3 dopamine receptor heteromer D2-D4 dopamine receptor heteromer D2- ...
  https://en.wikipedia.org/wiki/Dopamine_receptor
*  Dopamine receptor D3 - Wikipedia
"Entrez Gene: DRD3 dopamine receptor D3". Joyce JN, Millan MJ (February 2007). "Dopamine D3 receptor agonists for protection and ... 200-fold binding selectivity over D4, D2, 5-HT1A, and α1-receptors (-)-7-{[2-(4-Phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8 ... "The selective dopamine D3 receptor antagonists SB-277011A and NGB 2904 and the putative partial D3 receptor agonist BP-897 ... a dopamine D3/D2 receptor agonist, and 7-OH-DPAT, a dopamine D3 receptor agonist, in olfactory bulbectomized rats". European ...
  https://en.wikipedia.org/wiki/Dopamine_receptor_D3
*  Mechanism-based PK-PD model for the prolactin biological system response following an acute dopamine inhibition challenge:...
... model for the biological system prolactin response following a dopamine inhibition challenge... ... and d4 dopamine receptors: identification of the clozapine metabolite n-desmethylclozapine as a d2/d3 partial agonist. J ... Identification of amino acid determinants of dopamine 2 receptor synthetic agonist function. J Pharmacol Exp Ther 321:298-307 ... Featherstone K, White MR, Davis JR (2012) The prolactin gene: a paradigm of tissue-specific gene regulation with complex ...
  https://link.springer.com/article/10.1007%2Fs10928-012-9262-4
*  Dopamine receptor D4 - Wikipedia
... partial agonist Roxindole - D4 selective but also D2 and D3 autoreceptor agonist, 5HT1A receptor agonist, serotonin reuptake ... Current Research on the DRD4 Gene Receptors, Dopamine D4 at the US National Library of Medicine Medical Subject Headings (MeSH ... partial agonist, > 8600-fold selective over other dopamine receptor subtypes FAUC 299: partial agonist (E)-1-aryl-3-(4- ... partial agonist Flibanserin - partial agonist PD-168,077 - D4 selective but also binds to α1A, α2C and 5HT1A CP-226,269 - D4 ...
  https://en.wikipedia.org/wiki/Dopamine_receptor_D4
*  Dopamine receptor D4 - Wikipedia
Ro10-5824 - partial agonist. *Roxindole - D4 selective but also D2 and D3 autoreceptor agonist, 5HT1A receptor agonist, ... Current Research on the DRD4 Gene. *Receptors, Dopamine D4 at the US National Library of Medicine Medical Subject Headings ( ... The dopamine receptor D4 is a G protein-coupled receptor encoded by the DRD4 gene on chromosome 11 at 11p15.5.[5] ... LaHoste GJ, Swanson JM, Wigal SB, Glabe C, Wigal T, King N, Kennedy JL (May 1996). "Dopamine D4 receptor gene polymorphism is ...
  https://en.wikipedia.org/wiki/Dopamine_D4_receptor
*  PAR-11-207: National Cooperative Drug Discovery/Development Groups (NCDDG) for the Treatment of Mental Disorders, Drug or...
G-protein coupled receptors, such as the dopamine receptor, an indirect site of action for cocaine and amphetamine, or ligand ... Given the clinical availability of mu-opiate agonists, partial agonists and antagonists and the large number of NIDA-supported ... dopamine: D1, D3, D4, D5; estrogen; GABA A subunits; GABA ion channel; GABA B; glutamatergic, glycine site; metabotropic ... Intracellular targets: gene expression/transcription markers; markers of neurogenesis or neuronal cell death; markers of ...
  https://grants.nih.gov/grants/guide/pa-files/PAR-11-207.html
*  F-15063 - Wikipedia
... partial agonist at the D4 receptor, and agonist at the 5-HT1A receptors. It has greater efficacy at the 5-HT1A receptors than ... receptor antagonist and 5-HT(1A) receptor agonist properties: influence on immediate-early gene expression in rat prefrontal ... Assié, MB (June 2007). "F15063, a potential antipsychotic with dopamine D(2)/D(3) antagonist, 5-HT(1A) agonist and D(4) partial ... 5-HT1A agonist and D4 partial agonist properties: (I) in vitro receptor affinity and efficacy profile". British Journal of ...
  https://en.wikipedia.org/wiki/F-15063
*  Dopamine receptor D2 - Wikipedia
... is a partial agonist of D2 dopaminergic receptors and it potentiates dopamine-mediated prolactin secretion in lactotrophs in ... D4 receptor agonist Quinelorane - affinity for D2 > D3 Quinpirole - also D3 receptor agonist Ropinirole - full agonist ... The dopamine D2 receptor is the main receptor for most antipsychotic drugs. This gene encodes the D2 subtype of the dopamine ... LSD is also a 5-HT2A agonist. OSU-6162 - also 5-HT2A partial agonist, acts as "dopamine stabilizer" Roxindole (only at the D2 ...
  https://en.wikipedia.org/wiki/Dopamine_receptor_D2
*  Comparative pharmacology of antipsychotics possessing combined dopamine D2and serotonin 5-HT1Areceptor properties | SpringerLink
There is increasing interest in antipsychotics intended to manage positive symptoms via D2 receptor blockade and improve ... a potential antipsychotic with dopamine D2/D3 receptor antagonist, 5-HT1A receptor agonist and dopamine D4 receptor partial ... Role of 5-HT1A receptors in the ability of mixed 5-HT1A receptor agonist/dopamine D2 receptor antagonists to inhibit ... The role of 5-HT2A receptor and 5-HT2A/5-HT1A receptor interaction in the suppression of catalepsy. Genes Brain Behav 9:519-524 ...
  https://link.springer.com/article/10.1007%2Fs00213-011-2247-y
*  Textbook of Psychiatry/Psychopharmacology - Wikibooks, open books for an open world
... binds weakly at the D2 receptor (although with relatively greater net antagonism at D3 and D4 dopamine receptors) and has ... Buprenorphine is an opioid mu-receptor partial agonist (with very high affinity for this receptor) that is used as an ... 50 mg/day). Individuals with a specific polymorphism of the mu-opioid receptor gene (OPRM1), i.e., individuals with an Asp40 ... Varenicline is an alpha4beta2 nicotinic acetylcholine receptor partial agonist, with high affinity for this receptor. It is the ...
  https://en.wikibooks.org/wiki/Textbook_of_Psychiatry/Psychopharmacology
*  Frontiers | Active Reward Processing during Human Sleep: Insights from Sleep-Related Eating Disorder | Neurology
Lusher, J. M., Chandler, C., and Ball, D. (2001). Dopamine D4 receptor gene (DRD4) is associated with novelty seeking (NS) and ... 2008). Low dopamine striatal D2 receptors are associated with prefrontal metabolism in obese subjects: possible contributing ... Treatment usually concerns the management of the concomitant sleep disorders (RLS and OSA). Dopaminergic agonists are ... to partial awareness (Winkelman et al., 2011). Morning amnesia for the event is very frequent as well as the undesirable weight ...
  https://www.frontiersin.org/articles/10.3389/fneur.2012.00168/full
*  Risperidone Induced Amenorrhea Resolved by Paliperidone | OMICS International
Interestingly, aripiprazole is considered to be a prolactin-sparing agent due to its partial D2 receptor agonist activity, and ... Calarge CA, Ellingrod VL, Acion L (2009) Variants of the dopamine D2 receptor gene and risperidone-induced hyperprolactinemia ... preferential binding to D3 and D4 receptors, peculiar binding dynamics at the D2 receptors or differences in affinity to D2 ... Shim JC, Shin JC, Kelly Dl (2007) Adjunctive Treatment With a Dopamine Partial Agonist, Aripiprazole, for Antipsychotic-Induced ...
  https://www.omicsonline.org/open-access/risperidone-induced-amenorrhea-resolved-by-paliperidone-Psychiatry-1000224.php?aid=41226
*  Aberrant Dopamine D2-Like Receptor Function in a Rodent Model of Schizophrenia | Journal of Pharmacology and Experimental...
2010) Cariprazine (RGH-188), a dopamine D3 receptor-preferring, D3/D2 dopamine receptor antagonist-partial agonist ... and D4 receptors and the dopamine transporter (SLC6A3), tyrosine hydroxylase, and dopamine receptor signaling molecules RGS2, ... 2011) Converging evidence implicates the dopamine D3 receptor gene in vulnerability to schizophrenia. Am J Med Genet B ... dopamine D3 receptor (Rn00567568_m1), dopamine D4 receptor (Rn00564071_m1), dopamine transporter SLC6A3 (Rn00562224_m1), ...
  http://jpet.aspetjournals.org/content/343/2/288
*  CPDD Community Website: June 2012
... also has very high affinity for dopamine D3 receptors (it also appears to be a high affinity dopamine D4 receptor antagonist). ... which is a high affinity partial agonist at serotonin 5-HT1A receptors, ... citing the recent brain imaging and genetics study of over 400 twin pairs that elucidated the influence of genes on human brain ... Labels: Antiretroviral Therapy, Big dataset science, Cocaine Vaccine, Dopamine D3 receptors, HIV Transmission Prevention, ...
  http://www.cpddblog.com/2012/06/
*  Aripiprazole (Abilify) Full Prescribing Information | HealthyPlace
Aripiprazole functions as a partial agonist at the dopamine D2 and the serotonin 5-HT1A receptors, and as an antagonist at ... moderate affinity for dopamine D4, serotonin 5-HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors (Ki values of 44 nM ... In healthy human volunteers administered 0.5 to 30 mg/day aripiprazole for 14 days, there was dose-dependent D2 receptor ... the in vitro forward gene mutation assay in mouse lymphoma cells, the in vitro chromosomal aberration assay in Chinese hamster ...
  https://www.healthyplace.com/other-info/psychiatric-medications/aripiprazole-abilify-full-prescribing-information
*  FENS Forum 2004 - Abstracts
PHARMACOLOGICAL CHAPERONES AND THE BIOGENESIS OF THE DOPAMINE D4 RECEPTOR.. A220.7. Poster 142 - Wed 14/07, 11:30 - Hall I. ... MATERNAL DEPRIVATION AND HANDLING ALTER DOPAMINERGIC RECEPTOR LEVELS AND MODIFY THE RESPONSE TO THE D3 PARTIAL AGONIST BP897, ... Virology and Gene Therapy, Kuleuven, Belgium.. - EFFECT OF PARKIN OVEREXPRESSION IN A MOUSE MODEL FOR PARKINSON'S DISEASE.. ... MODULATION OF GLUCOCORTICOID RECEPTORS IN NUCLEUS ACCUMBENS AFFECTS ON MEMORY PROCESSING IN RATS.. A192.35. Poster 252 - Tue 13 ...
  http://fens2004.neurosciences.asso.fr/posters/Let/LetV.html
*  Modification of cocaine self-administration by buspirone (buspar®): potential involvement of D3 and D4 dopamine receptors. -...
D3 and D4 receptors, have yet to be explored for this indication in the clinic. Buspirone, a 5-HT1A partial agonist approved ... Buspirone antagonizes dopamine (DA)-induced receptor-β-arrestin interactions at human recombinant D2, D3 or D4 DA receptors. ... Gene. *Gene Expression Omnibus (GEO) Database *Gene Expression Omnibus (GEO) Datasets. *Gene Expression Omnibus (GEO) Profiles ... Modification of cocaine self-administration by buspirone (buspar®): potential involvement of D3 and D4 dopamine receptors.. ...
  https://www.ncbi.nlm.nih.gov/pubmed/22827916?dopt=Abstract
*  Antipsychotic and Anticholinergic Drugs | eNetMD
... and H1 receptors and moderate affinity for the D1 receptor. (25,27) Ziprasidone is also a partial agonist at the 5-HT 1A ... and the D4 Dopamine Antagonist Group (1997). The effects of a selective D4 dopamine receptor antagonism. (L-745, 870) in ... About 6 to 8 per cent of Caucasians and a small proportion of Asians have a polymorphism of the CYP2D6 gene, which leads to ... 22) The prefrontal cortex has relatively low concentrations of D 2 receptors and has a higher density of D3 and D4 dopamine ...
  http://www.enetmd.com/content/antipsychotic-and-anticholinergic-drugs
*  Apomorphine - Wikipedia
Ptácek R, Kuzelová H, Stefano GB (Sep 2011). "Dopamine D4 receptor gene DRD4 and its association with psychiatric disorders". ... Apomorphine is an agonist, or activator, of both D1 and D2 type dopamine receptors with higher activity at D2. The members of ... Apomorphine behaves as a partial agonist at D2S (IA = 79%), D2L (IA= 53%), D3 (IA = 82%), and D4 (IA = 45%), and as an ... Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor". The Journal ...
  https://en.wikipedia.org/wiki/Apomorphine
*  Hallucinogens as discriminative stimuli in animals: LSD, phenethylamines, and tryptamines | SpringerLink
Activity of serotonin receptor agonists, partial agonists, and antagonists at cloned human 5-HT1A receptors that are negatively ... Chemel BR, Roth BL, Armbruster B, Watts VJ, Nichols DE (2006) WAY-100635 is a potent dopamine D4 receptor agonist. ... 1998). Previous work had shown that the changes in SERT KO mice due to gene deletion are restricted almost exclusively to the ... For example, with respect to WAY-100,635, agonist activity at the dopamine D4 receptor has been reported (Chemel et al. 2006; ...
  https://link.springer.com/article/10.1007%2Fs00213-008-1356-8
*  Receptor Subtypes Involved in the Presynaptic and Postsynaptic Actions of Dopamine on Striatal Interneurons | Journal of...
Rivera A, Cuellar B, Giron FJ, Grandy DK, de la Calle A, Moratalla R (2002a) Dopamine D4 receptors are heterogeneously ... Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1. Nature 350: 614-619. ... receptor agonist quinpirole in two distinct mutants lacking D2L receptors and expressing variable contents of D2S receptors. ... F indicate a cholinergic partial cell that also expresses D5 receptors. G, J, Striatal neurons expressing DA D5 receptors in WT ...
  http://www.jneurosci.org/content/23/15/6245
*  Activation of the dopamine 1 and dopamine 5 receptors increase skeletal muscle mass and force production under non-atrophying...
1/dopamine 5 receptor agonist could be abrogated when the dopamine 1 receptor and to a lesser extent the dopamine 5 receptors ... the D1 receptor/D5 receptor group (D1-like) and the D2 receptor/D3 receptor/D4 receptor group (D2-like), based on their ... In contrast, genetic removal of the dopamine 5 receptor (with maintenance of the dopamine 1 receptor) resulted in a partial ... with splice variants of many of the dopamine receptors identified [1, 3]. Gene expression analysis of the dopamine receptors ...
  https://bmcmusculoskeletdisord.biomedcentral.com/articles/10.1186/1471-2474-12-27
*  Functional constructivism in taxonomies | Philosophical Transactions of the Royal Society B: Biological Sciences
2008 Association of the dopamine D4 receptor (DRD4) gene and approach-related personality traits: meta-analysis and new data. ... as a result of chronic stimulation by agonists (downregulation and desensitization of receptors). A single administration of ... emotional valence and functional aspects of performance appears to be only partial since all monoamine and opioid receptor ... Meanwhile some studies of DA D4 receptor genes found no associations with Extraversion [14,15]. Moreover, the early opinion ...
  http://rstb.royalsocietypublishing.org/content/373/1744/20170167
*  Olanzapine - Wikipedia
... and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist". J. ... the apparent dissociation constant of a neuroleptic at the dopamine D2 or D4 receptor varies with the affinity of the competing ... Yeung, Eugene YH; Chun, Soojin; Douglass, Alan; Lau, Timothy E (2017-05-08). "Effect of atypical antipsychotics on body weight ... It may involve antagonism of dopamine and serotonin receptors. Antagonism of dopamine receptors is associated with ...
  https://en.wikipedia.org/wiki/Olanzapine