Dopamine receptor
The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors. Dopamine receptors are implicated in ... Additionally, many antipsychotic drugs target dopamine receptors, especially D2 receptors. Dopamine receptor mutations can ... D4-adrenoceptor α1B D4-adrenoceptor β1 Dopamine receptor D1 and Dopamine receptor D5 are Gs coupled receptors that stimulate ... "Role of iso-receptors in receptor-receptor interactions with a focus on dopamine iso-receptor complexes". Rev Neurosci. 27 (1 ...
Dopamine receptor D5
It belongs to the D1-like receptor family along with the D1 receptor subtype. D5 receptor is a subtype of the dopamine receptor ... dopamine D5 receptor and D5-D2 receptor hetero-oligomers occurs by a mechanism distinct from that for dopamine D1-D2 receptor ... "Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors". British Journal of ... D5 receptor is expressed more widely in the CNS than its close structural homolog dopamine receptor D1. It is found in neurons ...
Dopamine receptor D4
The dopamine receptor D4 is a dopamine D2-like G protein-coupled receptor encoded by the DRD4 gene on chromosome 11 at 11p15.5 ... As with other dopamine receptor subtypes, the D4 receptor is activated by the neurotransmitter dopamine. It is linked to many ... "Dopamine Receptors: D4". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... Neve KA, Seamans JK, Trantham-Davidson H (August 2004). "Dopamine receptor signaling". Journal of Receptor and Signal ...
Dopamine receptor D3
"Entrez Gene: DRD3 dopamine receptor D3". Joyce JN, Millan MJ (February 2007). "Dopamine D3 receptor agonists for protection and ... a dopamine D3/D2 receptor agonist, and 7-OH-DPAT, a dopamine D3 receptor agonist, in olfactory bulbectomized rats". European ... Dopamine receptor D3 is a protein that in humans is encoded by the DRD3 gene. This gene encodes the D3 subtype of the dopamine ... "Dopamine Receptors: D3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ...
Dopamine receptor D1
... dopamine D2 receptor, dopamine D3 receptor, histamine H3 receptor, μ opioid receptor, NMDA receptor, and adenosine A1 receptor ... Dopamine receptor D1, also known as DRD1. It is one of the two types of D1-like receptor family - receptors D1 and D5. It is a ... "Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to ... NMDAR receptor complex − a target to prevent neurodegeneration D1-D3 receptor complex D1-NMDAR receptor complex D1-A1 receptor ...
Dopamine receptor D2
UNC9994 The dopamine receptor D2 has been shown to interact with EPB41L1, PPP1R9B and NCS-1. The D2 receptor forms receptor ... Hasbi A, O'Dowd BF, George SR (February 2010). "Heteromerization of dopamine D2 receptors with dopamine D1 or D5 receptors ... D1-D2 dopamine receptor heteromer D2-adenosine A2A D2-ghrelin receptor D2sh-TAAR1 The D2 receptor has been shown to form ... The dopamine D2 receptor is the main receptor for most antipsychotic drugs. The structure of DRD2 in complex with the atypical ...
D1-D2 dopamine receptor heteromer
The D1-D2 dopamine receptor heteromer is a receptor heteromer consisting of D1 and D2 protomers. D1 and D2 receptors interact ... Hasbi A, O'Dowd BF, George SR (February 2010). "Heteromerization of dopamine D2 receptors with dopamine D1 or D5 receptors ... "A novel dopamine receptor signaling unit in brain: heterooligomers of D1 and D2 dopamine receptors". TheScientificWorldJournal ... "Genetic variants of dopamine D2 receptor impact heterodimerization with dopamine D1 receptor". Pharmacological Reports. 69 (2 ...
Serotonin-norepinephrine-dopamine reuptake inhibitor
These include receptor desensitization, alterations in intracellular transduction cascades and gene expression, the induction ... A serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), also known as a triple reuptake inhibitor (TRI), is a type of ... Nieoullon, A (2002). "Dopamine and the regulation of cognition and attention". Progress in Neurobiology. 67 (1): 53-83. doi: ... 2. Potent dopamine and serotonin reuptake inhibitors". Journal of Medicinal Chemistry. 43 (6): 1215-1222. doi:10.1021/jm9905561 ...
Dopamine
Once in the synapse, dopamine binds to and activates dopamine receptors. These can be postsynaptic dopamine receptors, which ... D1 receptors are the most numerous dopamine receptors in the human nervous system; D2 receptors are next; D3, D4, and D5 ... In humans, dopamine has a high binding affinity at dopamine receptors and human trace amine-associated receptor 1 (hTAAR1). In ... dopamine can inhibit norepinephrine release by acting on presynaptic dopamine receptors, and also on presynaptic α-1 receptors ...
Etoperidone
D2 receptor (2,300 nM) > H1 receptor (3,100 nM) > mACh receptors (>35,000 nM). In addition to its receptor blockade, ... dopamine transporter (52,000 nM). Etoperidone is metabolized in part to meta-chlorophenylpiperazine (mCPP), which likely ... α1-adrenergic receptor (38 nM) > 5-HT1A receptor (85 nM) (may be a partial agonist) > α2-adrenergic receptor (570 nM); it has ... Etoperidone is as an antagonist of several receptors in the following order of potency: 5-HT2A receptor (36 nM) > ...
Transactivation
... receptor in neurons (Swift et al., 2011). These two dopamine receptors can also regulate calcium channels through a direct ... In the context of receptor signaling, transactivation occurs when one or more receptors activate yet another; receptor ... Beaulieu JM, Espinoza S, Gainetdinov RR (January 2015). "Dopamine receptors - IUPHAR Review 13". Br. J. Pharmacol. 172 (1): 1- ... Transrepression Selective glucocorticoid receptor agonist "receptor transactivation". EMBL. GO Consortium. Retrieved 6 April ...
Radioligand
... flumazenil for GABAA receptors. (+)PHNO for D2 dopamine receptors. [11C]raclopride for D2 dopamine receptors. Binding potential ... "Dopamine receptors labelled by PHNO". Synapse. 14 (4): 254-262. doi:10.1002/syn.890140403. PMID 7902615. S2CID 24111743.[dead ... for 5-HT2 receptors 18F-altanserin and 18F-setoperone for the 5-HT2A receptor 11C-ketanserin and tritiated ketanserin 11C-DASB ... "Relationship between blockade of dopamine transporters by oral methylphenidate and the increases in extracellular dopamine: ...
Imipramine
Dopamine: imipramine blocks D2 receptors. Imipramine, and its metabolite desipramine, have no appreciable affinity for the ... Sigma receptor: activity on sigma receptors is present, but it is very weak (Ki = 520 nM) and it is about half that of ... Smiałowski A (May 1991). "Dopamine D2 receptor blocking effect of imipramine in the rat hippocampus". Pharmacology, ... Schulze DR, Carroll FI, McMahon LR (August 2012). "Interactions between dopamine transporter and cannabinoid receptor ligands ...
Azapride
... is the azide derivative of the dopamine antagonist clebopride synthesized in order to label dopamine receptors. It is ... Niznik HB, Guan JH, Neumeyer JL, Seeman P (February 1985). "A photoaffinity ligand for dopamine D2 receptors: azidoclebopride ... Wouters W, Van Dun J, Laduron PM (December 1984). "Photoaffinity labelling of dopamine receptors. Synthesis and binding ... Dopamine antagonists, Organoazides, Chlorobenzenes, Salicylamide ethers, Piperidines, Irreversible antagonists, All stub ...
Neuromodulation
It acts on dopamine receptors. Parkinson's disease is at least in part related to dropping out of dopaminergic cells in deep- ... Dreyer JK, Herrik KF, Berg RW, Hounsgaard JD (October 2010). "Influence of phasic and tonic dopamine release on receptor ... AMPT prevents the conversion of tyrosine to L-DOPA, the precursor to dopamine; reserpine prevents dopamine storage within ... Acetylcholine binds to both metabotropic muscarinic receptors (mAChR) and the ionotropic nicotinic receptors (nAChR). The ...
Dihydrexidine
2002). "Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D ... D1-receptor agonists, D2-receptor agonists, D5 receptor agonists, Catechols, Biased ligands, All stub articles, ... Zhang J, Xiong B, Zhen X, Zhang A (2009). "Dopamine D1 receptor ligands: where are we now and where are we going". Med Res Rev ... Dihydrexidine (DAR-0100) is a moderately selective full agonist at the dopamine D1 and D5 receptors. It has approximately 10- ...
Nucleus accumbens
Glucocorticoids and dopamine: Glucocorticoid receptors are the only corticosteroid receptors in the nucleus accumbens shell. L- ... Dopamine action in NAc is mediated predominantly via activation of D1 or D2 dopamine receptors that are expressed by largely ... dopamine receptors. A subpopulation of MSNs contain both D1-type and D2-type receptors, with approximately 40% of striatal MSNs ... The dopamine receptors are a superfamily of heptahelical G protein-coupled receptors, and are grouped into two categories, D1- ...
Antidepressant
... and/or dopamine. Additionally, most also act as α1-adrenergic receptor antagonists. The majority of the currently marketed ... decreased dopamine; decreased norepinephrine; blockade of cholinergic and α1adrenergic receptors; inhibition of nitric oxide ... dopamine reuptake inhibition (bupropion, amineptine, nomifensine), direct modulation of monoamine receptors (vilazodone, ... a partial agonist of the 5-HT1A receptor, and antagonist of the 5-HT3 and 5-HT7 receptors. However, it can also technically be ...
Raclopride
It acts as a selective antagonist on D2 dopamine receptors. It has been used in trials studying Parkinson Disease. Its ... A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain". Biochemical Pharmacology. ... Farde L, Gustavsson JP, Jönsson E (1997). "D2 dopamine receptors and personality traits". Nature. 385 (6617): 590. Bibcode: ... allow the non-invasive assessment of the binding capacity of the cerebral D2 dopamine receptor, which can be useful for the ...
Addiction-related structural neuroplasticity
Cameron, DL (1993). "Dopamine D1 receptors facilitate transmitter release". Nature. 366 (6453): 344-47. Bibcode:1993Natur.366.. ... For LTP to occur, NMDA receptors on the dendritic spine send intracellular signals to increase the number of AMPA receptors on ... GABAergic neurons in the VTA also synapse on local dopamine cells. In non-drug models, the VTA dopamine neurons are stimulated ... These drugs induce an increase in synaptic dopamine by inhibiting the reuptake of dopamine from the synaptic cleft, effectively ...
J. W. Kebabian
His pioneering work which was published in 1979 revolutionized the understanding of the role of dopamine receptors in cognition ... Daly, Jeffrey M.; Salloway, Stephen (1 May 1994). "Dopamine Receptors in the Human Brain". Psychiatric Times. 11 (5). Retrieved ... a neuropharmacologist and neuroscientist who was the first to discover that there were multiple subtypes of dopamine receptors ...
Dopamine antagonist
... also known as an anti-dopaminergic and a dopamine receptor antagonist (DRA), is a type of drug which blocks dopamine receptors ... Dopamine receptors are all G protein-coupled receptors, and are divided into two classes based on which G-protein they are ... These drugs are not only dopamine antagonists at the receptor specified, but also act on serotonin receptor 5HT2A. (Citation ... In addition, D5 receptors have been found in the kidney D2-like receptors unlike the D1-like class, these receptors are found ...
Coincidence detection in neurobiology
Neve, Kim A.; Seamans, Jeremy K.; Trantham-Davidson, Heather (August 2004). "Dopamine receptor signaling". Journal of Receptor ... Besides the NMDA-receptor based processes, further cellular mechanisms allow of the association between two different input ... LTP in the hippocampus requires a prolonged depolarization that can expel the Mg2+ block of postsynaptic NMDA receptors. The ... The Ca2+, IP3, and DAG work together in a signal transduction pathway to internalize AMPA receptors and decrease the ...
Trimethobenzamide
"Dopamine receptor antagonists". Ann Palliat Med. 1 (2): 137-42. doi:10.3978/j.issn.2224-5820.2012.07.09. PMID 25841474. Waknine ... Trimethobenzamide is an antagonist of the D2 receptor. It is believed to affect the chemoreceptor trigger zone (CTZ) of the ...
Adenylyl cyclase
Neve KA, Seamans JK, Trantham-Davidson H (August 2004). "Dopamine receptor signaling". Journal of Receptor and Signal ... Beta adrenergic receptor kinase pathway "PDB101: Molecule of the Month: G Proteins". RCSB: PDB-101. Retrieved 24 August 2020. ... Adenylyl cyclases are often activated or inhibited by G proteins, which are coupled to membrane receptors and thus can respond ... In order to become active, a ligand must bind to the receptor and cause a conformational change. This conformational change ...
Dopamine hypothesis of schizophrenia
Dopamine Receptor Oligermization". In Neve KA (ed.). Dopamine Receptors. Springer. ISBN 9781603273336. "Dopamine Receptors: ... Dopamine receptors interact with their own kind, or other receptors to form higher order receptors such as dimers, via the ... has been found to antagonize dopamine binding (particularly at receptors known as D2 dopamine receptors) and reduce positive ... "The cloned dopamine D2 receptor reveals different densities for dopamine receptor antagonist ligands. Implications for human ...
Microphthalmia, syndromic 12 (MCOPS12)
Both D1R and D2R are dopamine receptors. RAR-beta is a transcription factor and the D2R dopamine receptor is one of its targets ... RARB encodes retinoic acid receptor beta (RAR-beta), which belongs to the retinoic acid receptor family together with the other ... The retinoic acid receptor beta (RARB) gene (Gene ID: 5915) is located on the short (p) arm of chromosome 3 (3p24.2). It ... It is caused by a single-point missense mutation in the retinoic acid receptor beta (RARB) gene. The most common disease ...
Mesulergine
It acts on serotonin and dopamine receptors. Specifically, it is an agonist of dopamine D2-like receptors and serotonin 5-HT6 ... and 5-HT7 receptors.[citation needed] It also has affinity for the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, and 5-HT5A receptors. The ... Dopamine agonists, Ergolines, Prolactin inhibitors, Serotonin receptor antagonists, Sulfamides, All stub articles, Nervous ... 177-. ISBN 978-94-011-4439-1. Closse A (May 1983). "[3H]Mesulergine, a selective ligand for serotonin-2 receptors". Life Sci. ...
Trifluoperazine
It is believed to work by blockading dopamine D1 and D2 receptors in the mesocortical and mesolimbic pathways, relieving or ... Seeman P, Lee T, Chau-Wong M, Wong K (June 1976). "Antipsychotic drug doses and neuroleptic/dopamine receptors". Nature. 261 ( ... Creese I, Burt DR, Snyder SH (1996). "Dopamine receptor binding predicts clinical and pharmacological potencies of ... Hill SJ, Young M (December 1978). "Antagonism of central histamine H1 receptors by antipsychotic drugs". European Journal of ...
Reward system
... dopamine acts on D1-like receptors or D2-like receptors to either stimulate (D1-like) or inhibit (D2-like) the production of ... Dopamine neurons in the VTA are activated by food and water, and dopamine release in the NAc is stimulated by the presence of ... Trantham-Davidson H, Neely LC, Lavin A, Seamans JK (2004). "Mechanisms underlying differential D1 versus D2 dopamine receptor ... Stoof, J. C., & Kebabian, J. W. (1984). Two dopamine receptors: biochemistry, physiology and pharmacology. Life sciences, 35(23 ...
Dopamine beta hydroxylase deficiency
September 2007). "Dopamine D1 receptor agonist and D2 receptor antagonist effects of the natural product (-)-stepholidine: ... "Dopamine receptor antagonists - Pharmacorama". www.pharmacorama.com. Retrieved 2016-12-15. Kaufmann, Horacio; Saadia, Daniela; ... Dopamine beta (β)-hydroxylase deficiency is a condition involving inadequate dopamine beta-hydroxylase. It is characterized by ... Prolactin is frequently suppressed by excessive dopamine found in the patient's central nervous system. Excess dopamine can ...