*  Apomorphine - DrugBank
A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute ... a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and ... Succu S, Sanna F, Melis T, Boi A, Argiolas A, Melis MR: Stimulation of dopamine receptors in the paraventricular nucleus of the ... Mansbach RS, Brooks EW, Sanner MA, Zorn SH: Selective dopamine D4 receptor antagonists reverse apomorphine-induced blockade of ...
  https://www.drugbank.ca/drugs/DB00714
*  Dopamine receptor D4 - Wikipedia
Hübner H, Kraxner J, Gmeiner P (November 2000). "Cyanoindole derivatives as highly selective dopamine D(4) receptor partial ... selective and competitive antagonist at dopamine D4 receptors: an in vitro and in vivo comparison with L 745,870 (3-(4-[4- ... Moreland RB, Patel M, Hsieh GC, Wetter JM, Marsh K, Brioni JD (September 2005). "A-412997 is a selective dopamine D4 receptor ... dopamine neurotransmitter receptor activity. • G-protein coupled receptor activity. • protein binding. • dopamine binding. • ...
  https://en.wikipedia.org/wiki/Dopamine_D4_receptor
*  Biological Profile of L-745,870, a Selective Antagonist with High Affinity for the Dopamine D4 Receptor | Journal of...
... was evident that highly selective D4 receptor antagonists were required to evaluate whether blockade of dopamine D4 receptors ... to the rat D4 receptor (Ki 1.5 nM) compared to the human D4 receptor (Ki 0.43 nM) but still retained ,1000-fold D4 receptor ... Clozapine bound to D4 receptors with nanomolar affinity (Ki 10 nM) and was 7- and 20-fold selective for D4 receptors compared ... 1993) Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications. Eur. J. ...
  http://jpet.aspetjournals.org/content/283/2/636
*  Dopamine receptor D4 - Wikipedia
Hübner H, Kraxner J, Gmeiner P (November 2000). "Cyanoindole derivatives as highly selective dopamine D(4) receptor partial ... "Dopamine Receptors: D4". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... As with other dopamine receptor subtypes, the D4 receptor is activated by the neurotransmitter dopamine. It is linked to many ... Moreland RB, Patel M, Hsieh GC, Wetter JM, Marsh K, Brioni JD (September 2005). "A-412997 is a selective dopamine D4 receptor ...
  https://en.wikipedia.org/wiki/Dopamine_receptor_D4
*  ChemMedChem - Volume 4, Issue 3 - March 16, 2009 - Wiley Online Library
Showing an analogous binding mode as heterocyclic dopamine D4 receptor-selective lead compounds, the induction of penile ... Blue makes it happen: The non-uniform charge distribution of the blue colored azulene framework is highly suitable for the ... Structure-Affinity/Activity Relationships at α1 and 5-HT1A Receptors (pages 393-399). Claudia Sorbi, Silvia Franchini, Annalisa ... The Azulene Framework as a Novel Arene Bioisostere: Design of Potent Dopamine D4 Receptor Ligands Inducing Penile Erection ( ...
  http://onlinelibrary.wiley.com/doi/10.1002/cmdc.v4:3/issuetoc
*  Dopamine receptor D2 - Wikipedia
... highly selective Talipexole - selective for D2 over other dopamine receptors, but also acts as α2-adrenoceptor agonist and 5- ... Piribedil - also D3 receptor agonist and α2-adrenergic antagonist Pramipexole - also D3, D4 receptor agonist Quinelorane - ... The dopamine D2 receptor is the main receptor for most antipsychotic drugs. This gene encodes the D2 subtype of the dopamine ... Hasbi A, O'Dowd BF, George SR (Feb 2010). "Heteromerization of dopamine D2 receptors with dopamine D1 or D5 receptors generates ...
  https://en.wikipedia.org/wiki/Dopamine_receptor_D2
*  Pipamperone - Wikipedia
It shows much higher affinity for the 5-HT2A and D4 receptors over the D2 receptor (15-fold in the case of the D4 receptor, and ... even higher in the case of the 5-HT2A receptor), being regarded as "highly selective" for the former two sites at low doses. ... "Influence of the antipsychotic drug pipamperone on the expression of the dopamine D4 receptor". Life Sci. 80 (1): 74-81. doi: ... receptor affinity in behavioral assays selective for 5-HT(2C) receptor antagonist properties of compounds". Eur. J. Pharmacol. ...
  https://en.wikipedia.org/wiki/Pipamperone
*  Dopamine receptor D3 - Wikipedia
... subtype selective GR-103,691 GSK598809 (highly selective) Haloperidol (non-selective, blocks all dopamine receptor subtypes) N ... 200-fold binding selectivity over D4, D2, 5-HT1A, and α1-receptors (-)-7-{[2-(4-Phenylpiperazin-1-yl)ethyl]propylamino}-5,6,7,8 ... non-selective) Cariprazine CJB 090 CJ-1037 (extremely selective) FAUC 460 (highly selective) FAUC 346 (highly selective) ... non-selective dopamine agonist) Rotigotine (non-selective dopamine agonist) Aripiprazole (non-selective) BP-897 Buspirone ( ...
  https://en.wikipedia.org/wiki/Dopamine_receptor_D3
*  Role of Dopamine Receptors in Primary Focal Dystonias - Morvarid Karimi
This is a proposal to support my career development and research efforts in clarifying the role of dopamine receptors in ... Subsequently, we did not find reduced binding with a highly selective D2 ligand NMB (200-fold more selective for D2 than D3) in ... 2013) Striatal dopamine D1-like receptor binding is unchanged in primary focal dystonia. Mov Disord 28:2002-6 ... Most previous neuroimaging work in dystonia has focused on D2-like (D2, D3, D4) receptors. However, the ability of PET to ...
  http://grantome.com/grant/NIH/K23-NS069746-02
*  Dopamine Receptors: Clinical Correlates
... in the number of dopamine D2 receptor monomers. Recently, D4-selective radioligands ([125I]NGD 94-1 [99] and two other new [3H] ... The neuroleptic dissociation constant rises with highly fat-soluble radioligands, presumably because the more fat-soluble ... Dopamine D4 Receptors The dopamine D4 receptor (190,191) has many variants in the human (88). Each variant has a different ... Dopamine D2 Receptors There are three types of dopamine D2-like receptors: D2, D3 and D4. As summarized in , the dopamine D2 ...
  http://www.acnp.org/g4/GN401000027/CH027.html
*  Repinotan - Wikipedia
Repinotan HCI (BAYx3702) acts as a highly selective 5-HT1A receptor full agonist. It is blocked by the specific 5-HT1A receptor ... dopamine D2 and D4, sigma sites, and 5-HT2C. It is able to increase activity of VTA dopaminergic neurons and medial prefrontal ... Repinotan has been found to bind with high to moderate affinity to the receptors alpha-1 and alpha-2 adrenergic, 5-HT7- and 5- ... cortex dopamine release. Repinotan acts as a selective high-affinity full receptor agonist at the 5-HT1A receptor subtype. It ...
  https://en.wikipedia.org/wiki/Repinotan
*  PF-219,061 - Wikipedia
... is a drug that was under development by Pfizer which acts as a potent and highly selective agonist for the dopamine D3 receptor ... Brioni, Jorge D.; Moreland, Robert B. (2006). "Dopamine D4 receptors and the regulation of penile erection". Drug Discovery ... Selective Dopamine D3 Receptor Agonists for the Treatment of Sexual Dysfunction, WIPO Patent WO/2003/051370, granted to Pfizer ... "Targeting the dopamine D3 receptor: an overview of drug design strategies". Expert Opinion on Drug Discovery. 11 (7): 641-64. ...
  https://en.wikipedia.org/wiki/PF-219,061
*  Tài liệu Pharmacological Agents chọn lọc - TaiLieu.VN
Clozapine is a highly effective antipsychotic. It has little affinity for the D2-receptor compared with classical drugs but ... binds more avidly to other dopamine subtypes (e.g. D1, D3 and D4). It blocks muscarinic acetylcholine receptors, as do certain ... Highly selective toxicity is, therefore, harder to achieve. Identification of differences between viral and human metabolism ... Receptor blockade will outlast the persistence of the drug in the plasma. Rational treatment includes: • Atropine (1-2 mg i.v. ...
  http://tailieu.vn/tag/pharmacological-agents.html
*  WAY-100,135 - Wikipedia
However, WAY-100,635 turned out to be non-selective as well, having been shown to act additionally as a potent D4 receptor ... Chemel BR, Roth BL, Armbruster B, Watts VJ, Nichols DE (October 2006). "WAY-100635 is a potent dopamine D4 receptor agonist". ... It acts as potent 5-HT1A receptor antagonist, and was originally believed to be highly selective, but further studies have ... June 1993). "WAY100135: a novel, selective antagonist at presynaptic and postsynaptic 5-HT1A receptors". European Journal of ...
  https://en.wikipedia.org/wiki/WAY-100,135
*  Pramipexole - Wikipedia
... and D4 dopamine receptors, pramipexole may directly stimulate the underfunctioning dopamine receptors in the striatum, thereby ... D2S receptor (Ki = 3.9 nM; IA = 130%) D2L receptor (Ki = 2.2 nM; IA = 70%) D3 receptor (Ki = 0.5 nM; IA = 70%) D4 receptor (Ki ... In a single controlled study of twenty one patients, pramipexole was found to be highly effective in the treatment of bipolar ... DeBattista C, Solvason HB, Breen JA, Schatzberg AF (2000). "Pramipexole augmentation of a selective serotonin reuptake ...
  https://en.wikipedia.org/wiki/Pramipexole
*  Protocols and Video Articles Authored by Lior Rosenberg Belmaker (Translated to Swedish)
Recently, a specific dopamine D4 receptor (DRD4) agonist was shown in rats to induce penile erection through a central ... Chronic rTMS modulates cortical beta-adrenergic receptors, reduces frontal cortex 5-HT2 receptors, increases 5- ... Treatment with LiCl doses leading to blood levels of 1.3 and 1.4 mmol/l led to highly significant reduction in immobility time ... Knowledge, Action and Resistance: the Selective Use of Pre-natal Screening Among Bedouin Women of the Negev, Israel Social ...
  https://www.jove.com/author/Lior_Rosenberg+Belmaker?language=Swedish
*  Interaction with Neuronal Calcium Sensor NCS-1 Mediates Desensitization of the D2 Dopamine Receptor | Journal of Neuroscience
1992) Dopamine receptor sequences. Therapeutic levels of neuroleptics occupy D2 receptors, clozapine occupies D4. ... of dopamine on D2 receptor internalization were virtually abolished in the presence of 1 μm of the selective D2 receptor ... Dopaminergic transmission within limbic regions of the brain is highly dependent on the regulation of D2 receptor activity. ... Interaction of NCS-1 with dopamine receptors. To identify dopamine receptor interacting proteins, we used the C terminus of the ...
  http://www.jneurosci.org/content/22/19/8476
*  Frontiers | Dopamine regulates intrinsic excitability thereby gating successful induction of spike timing-dependent plasticity...
We found that dopamine via D1 receptor signaling, but not adrenergic signaling activated by the -adrenergic agonist ... and we will suggest possible reasons for the selective gating of STDP by dopamine (but not noradrenaline) in CA1. ... We found that dopamine via D1 receptor signaling, but not adrenergic signaling activated by the -adrenergic agonist ... and we will suggest possible reasons for the selective gating of STDP by dopamine (but not noradrenaline) in CA1. ...
  https://www.frontiersin.org/articles/10.3389/fnins.2013.00025/full
*  Genetics of aggression - Wikipedia
Another study evidenced that both 7R and 5R, ADHD-linked VNTR alleles of dopamine receptor D4 gene are directly associated with ... Most studies have focused on polymorphisms of serotonin receptors, dopamine receptors, and neurotransmitter metabolizing ... Selective breeding is a quick way to select for specific traits and see those selected traits within a few generations of ... A study done in 1983 (Cairns) produced both highly aggressive male and female strains of mice dependent on certain ...
  https://en.wikipedia.org/wiki/Genetics_of_aggression
*  Thioridazine hydrochloride | MALT1 inhibitor; DA antag. | CAS [130-61-0] - [50-52-2] | Axon 2193 | Axon Ligand™ with |99%...
... nanomolar affinity for dopamine and α-adrenergic receptors (Ki of 0.4 nM, 1.5 nM, 1.5 nM, 3.2 nM, 2.4 nM for D2, D3, D4, α1A, ... Highly potent and selective MALT1 inhibitor €125.00 The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or ... Apoptosis CNS D2 D3 D4 Adrenoceptor α1 MALT1 NF-κB PI3K-Akt-mTOR EC 3.4.22 Stem Cell Differentiator ...
  https://www.axonmedchem.com/product/2193
*  Positive Allosteric Modulator of the Human 5-HT2C Receptor | Molecular Pharmacology
Characterization of the functional activity of dopamine ligands at human recombinant dopamine D4 receptors. J Neurochem 63: 62- ... In this study, we discovered a positive allosteric modulator that was highly selective for 5-HT2C receptors. PNU-69176E ... Interaction with dopamine D4 receptor and dopamine D3 receptor polymorphisms. Am J Med Genet 74: 65-72. ... but not with analogous 5-HT and dopamine receptors (human 5-HT2A, 5-HT2B, 5-HT6, 5-HT7, and dopamine D2-long and D3 receptors ...
  http://molpharm.aspetjournals.org/content/64/1/78
*  Most recent papers with the keyword striatum | Read by QxMD
... and several compounds reported as selective dopamine D2 -like receptor ligands, such as the D3 receptor agonist 7-OH-PIPAT and ... Dopamine D4 Receptor Gene Associated with the Frontal-Striatal-Cerebellar Loop in Children with ADHD: A Resting-State fMRI ... Background: Low dopamine D2/3 receptor availability in the nucleus accumbens (NAcb) shell is associated with highly-impulsive ... GluN2C-containing receptors have been linked to this hypothesis due to the higher affinity of psychotomimetic doses of ketamine ...
  https://www.readbyqxmd.com/keyword/15210
*  Frontiers | Extrasynaptic Neurotransmission in the Modulation of Brain Function. Focus on the Striatal Neuronal-Glial Networks ...
Receptor-receptor interactions in G protein-coupled receptor (GPCR) heteromers play a major role, on dendritic spines and nerve ... Heteromeric complexes between GPCR and ion-channel receptors play a special role in the integration of the synaptic and ... dopamine, 5-hydroxytryptamine (5-HT) and histamine striatal afferents, the cholinergic interneurons and different types of GABA ... Receptor-receptor interactions in G protein-coupled receptor (GPCR) heteromers play a major role, on dendritic spines and nerve ...
  https://www.frontiersin.org/articles/10.3389/fphys.2012.00136/full
*  Bladder, bowel, and sexual dysfunction in Parkinson's disease.
... scarce in dopamine receptors) in response to dopamine [115, 116], presumably mediated by other receptor populations such as ... Oxytocin maintains as well as initiates female sexual behavior: effects of a highly selective oxytocin antagonistHormones and ... Polymorphisms in the dopamine D4 receptor gene (DRD4) contribute to individual differences in human sexual behavior: desire, ... Pathology studies have shown that the hypothalamus is affected in PD [231]. Recently, polymorphism in the dopamine D4 receptor ...
  http://www.biomedsearch.com/nih/Bladder-bowel-sexual-dysfunction-in/21918729.html
*  Role of Dopamine D2-like Receptors in Cocaine Self-Administration: Studies with D2 Receptor Mutant Mice and Novel D2 Receptor...
1997) Biological profile of l-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp ... to potentiate or mimic the behavioral effects of cocaine were highly correlated with their relative affinities for D3 receptors ... Third, estimates of D4 receptor occupancyin vivo suggested that 1.0 mg/kg ofl-745,870 occupies up to 90% of D4 receptors in the ... 1996) Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist. J Pharmacol Exp Ther 279:1392- ...
  http://www.jneurosci.org/content/22/7/2977.long