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mk 458

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Description

MK 458: a sustained release formulation of a naphthoxazine compoud with selective D-2 dopamine receptor agonism [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

naxagolide hydrochloride : The hydrochloride salt of naxagolide. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID57532
CHEMBL ID2106804
CHEBI ID177381
SCHEMBL ID122853
MeSH IDM0193488

Synonyms (49)

Synonym
100935-99-7
ent naxagolide hydrochloride
l 647,339
naxagolide hcl
l-647,339
(+)-phno hydrochloride
(4ar,10br)-4-propyl-3,4,4a,5,6,10b-hexahydro-2h-naphtho[1,2-b][1,4]oxazin-9-ol hydrochloride
(4ar,10br)-9-hydroxy-4-propyl-3,4,4a,5,6,10b-hexahydro-2h-naphtho[1,2-b][1,4]oxazin-4-ium chloride
(4ar-trans)-3,4,4a,5,6,10b-hexahydro-4-propyl-2h-naphth[1,2-b]-1,4-oxazin-9-ol hydrochloride
CHEBI:177381
mk 458
naxagolide monohydrochloride
l 647339
mk-458
l-647339
n-0500-(+)
phno-(+)
naxagolide hydrochloride
D05124
naxagolide hydrochloride (usan)
99705-65-4
(+)-propyl-9-hydroxynaphthoxazine hydrochloride
e5kfj9796w ,
(+)-(4ar,10br)-3,4,4a,5,6,10b-hexahydro-4-propyl-2h-naphth(1,2-b)-1,4-oxazin-9-ol hydrochloride
naxagolide hydrochloride [usan]
unii-e5kfj9796w
2h-naphth(1,2-b)-1,4-oxazin-9-ol, 3,4,4a,5,6,10b-hexahydro-4-propyl-, hydrochloride, (4ar-trans)-
CHEMBL2106804
naxagolide hydrochloride [mart.]
smr004701331
MLS006010256
SCHEMBL122853
(+/-)-phno hydrochloride
trans-(+/-)-4-propyl-3,4,4a,5,6,10b-hexahydro-2h-naphtho[1,2-b][1,4]oxazin-9-ol hydrochloride
J-000279
DTXSID60244221
AKOS030254483
A847237
trans-4-propyl-3,4,4a,5,6,10b-hexahydro-2h-naphtho[1,2-b][1,4]oxazin-9-ol hydrochloride
99705-65-4 (hcl)
entnaxagolidehydrochloride
(4ar,10br)-4-propyl-2,3,4a,5,6,10b-hexahydrobenzo[h][1,4]benzoxazin-9-ol;hydrochloride
2h-naphth[1,2-b]-1,4-oxazin-9-ol, 3,4,4a,5,6,10b-hexahydro-4-propyl-, hydrochloride, trans- (9ci)
Q27276897
ZDA70565
phno hydrochloride, (+)-
(4ar,10br)-4-propyl-2h,3h,4h,4ah,5h,6h,10bh-naphtho[1,2-b][1,4]oxazin-9-ol hydrochloride
naxagolidehydrochloride
E98816

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"To investigate the pharmacokinetic profile, bioavailability, and dose proportionality of the D2-agonist MK-458 (hydroxypropylmethylcellulose tablet, a sustained release formulation), a 4-period crossover study was conducted in 10 patients with mild to moderate Parkinson's disease (mean age = 63 y; 1 woman, 9 men)."( Pharmacokinetics and dose proportionality of D2-agonist MK-458 (HPMC) in parkinsonism.
Cutler, NR; Hand, EL; McLean, LF; Porras, AG; Reines, SA; Sramek, JJ, 1992
)
0.28

Bioavailability

ExcerptReferenceRelevance
" The bioavailability (approximately 5%) was very similar for the 3 tablet formulations tested."( Pharmacokinetics and dose proportionality of D2-agonist MK-458 (HPMC) in parkinsonism.
Cutler, NR; Hand, EL; McLean, LF; Porras, AG; Reines, SA; Sramek, JJ, 1992
)
0.28
" In dogs the in vivo absorption rate was similar to the in vitro dissolution rate, but in humans it was only about half."( Preparation of controlled release granules of TA-5707F using enteric polymers and ethylcellulose, and their in vivo evaluation.
Maejima, T; Matsukawa, Y; Osawa, T; Yamakita, H, 1996
)
0.29
"The present investigation concerns the development of the floating matrix tablets, which after oral administration are designed to prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs."( Optimisation of floating matrix tablets and evaluation of their gastric residence time.
Baumgartner, S; Kristl, J; Vodopivec, P; Vrecer, F; Zorko, B, 2000
)
0.31
" Absolute bioavailability and comparative bioavailability of the tested tablet were studied."( Preparation and evaluation of a sustained-release formulation of nifedipine HPMC tablets.
Ding, D; Li, H; Yan, G; Zhang, R, 2000
)
0.31
"The aim of the present study was to investigate the effect of hydroxypropylmethylcellulose (HPMC-2208), used as an excipient for controlled release of drug, on the release profiles and bioavailability of the poorly water-soluble nifedipine (NP) from a tablet prepared using macrogol 6000 (PEG) and HPMC."( Effect of hydroxypropylmethylcellulose (HPMC) on the release profiles and bioavailability of a poorly water-soluble drug from tablets prepared using macrogol and HPMC.
Endo, H; Ishikawa, T; Matsumoto, M; Takayama, K; Watanabe, Y, 2000
)
0.31
"For the development of omeprazole buccal adhesive tablets, we studied the release and bioavailability of omeprazole delivered by buccal adhesive tablets composed of sodium alginate, hydroxypropylmethylcellulose (HPMC), magnesium oxide and croscarmellose sodium."( Formulation and in vivo evaluation of omeprazole buccal adhesive tablet.
Choi, H; Han, J; Jung, J; Kim, C; Lee, M; Park, K; Rhee, C; Yong, CS, 2000
)
0.31
" The bioavailability of the CPH gel formulation prepared with HPMC was almost identical to that of the oral route."( In vivo studies on nasal preparations of ciprofloxacin hydrochloride.
Akev, N; Birteksöz, S; Can, A; Gerçeker, A; Ozsoy, Y; Tunçel, T, 2000
)
0.31
" The synchronous matrices increased SP bioavailability after intra-intestinal administration."( Synchronized release of sulpiride and sodium decanoate from HPMC matrices: a rational approach to enhance sulpiride absorption in the rat intestine.
Assaf, P; Baluom, M; Friedman, M; Haj-Yehia, AI; Rubinstein, A, 2000
)
0.31
"SP bioavailability after intestinal administration can be improved only if SP is released together with SD along the entire intestinal route."( Synchronized release of sulpiride and sodium decanoate from HPMC matrices: a rational approach to enhance sulpiride absorption in the rat intestine.
Assaf, P; Baluom, M; Friedman, M; Haj-Yehia, AI; Rubinstein, A, 2000
)
0.31
"The goals of this study were to examine whether formulations, capable of releasing sulpiride (SP) in synchrony with the p-Glycoprotein (P-gp) inhibitors, verapamil (Ver) or quinidine (Qn) can increase SP relative bioavailability and to suggest a rationale approach for oral administration of SP."( Improved intestinal absorption of sulpiride in rats with synchronized oral delivery systems.
Baluom, M; Friedman, M; Rubinstein, A, 2001
)
0.31
" The release and bioavailability of omeprazole delivered by the buccal adhesive tablets were studied."( Physicochemical characterization and evaluation of buccal adhesive tablets containing omeprazole.
Choi, HG; Jung, JH; Kim, CK; Rhee, JD; Yong, CS, 2001
)
0.31
"This study was undertaken with an objective to increase the dissolution rate and bioavailability of a poorly water soluble drug gliclazide (Gz) by complexation with beta-cyclodextrin (CD) in the presence of hydroxypropylmethylcellulose (HPMC)."( Studies on solubility and hypoglycemic activity of gliclazide beta-cyclodextrin-hydroxypropylmethylcellulose complexes.
Aggarwal, S; Mishra, B; Singh, PN, 2002
)
0.31
"0 hours, and its relative bioavailability was 96%."( [Studies on heart-protecting musk pH-dependent gradient-release pellets].
Bi, KS; Guo, T; Li, X; Ma, Y; Song, HT; Zhang, RH, 2002
)
0.31
"To prepare naftopidil bioadhesive sustained-release capsule and study their pharmacokinetics and relative bioavailability in the dog."( [Improving bioavailability of naftopidil by using bioadhesion in dogs].
Ding, JS; Jiang, XH; Yuan, M, 2001
)
0.31
" The naftopidil concentrations in plasma were determined by a newly developed HPLC method and the pharmacokinetic parameters as well as the relative bioavailability were measured."( [Improving bioavailability of naftopidil by using bioadhesion in dogs].
Ding, JS; Jiang, XH; Yuan, M, 2001
)
0.31
" The bioadhesive formulations and the non-bioadhesive one were not bioequivalent, the relative bioavailability of the two bioadhesive sustained-release capsules were respectively 150% +/- 14% and 154% +/- 23% when compared with the non-bioadhesive capsule."( [Improving bioavailability of naftopidil by using bioadhesion in dogs].
Ding, JS; Jiang, XH; Yuan, M, 2001
)
0.31
"It is much improving bioavailability of naftopidil by using bioadhesion."( [Improving bioavailability of naftopidil by using bioadhesion in dogs].
Ding, JS; Jiang, XH; Yuan, M, 2001
)
0.31
" The relative bioavailability of GSSC to GSW was 95."( Preparation and evaluation of pH-dependent gradient-release pellets for TCM.
Ci, L; Tang, X; Tian, X, 2004
)
0.32
"The bioavailability of propranolol from a matrix-in-cylinder system for sustained drug delivery, consisting of a hot-melt extruded ethylcellulose pipe surrounding a drug-containing HPMC-Gelucire 44/14 core, was determined."( Human bioavailability of propranolol from a matrix-in-cylinder system with a HPMC-Gelucire core.
Augustijns, P; Korst, A; Mehuys, E; Mols, R; Porter, C; Remon, JP; Van Bortel, L; Vervaet, C, 2005
)
0.33
" No significant in vivo bioavailability differences were observed in healthy human volunteers."( Formulation, release characteristics and bioavailability of novel monolithic hydroxypropylmethylcellulose matrix tablets containing acetaminophen.
Cao, QR; Choi, YW; Cui, JH; Lee, BJ, 2005
)
0.33

Dosage Studied

ExcerptRelevanceReference
"Two types of multiple controlled release dosage forms, hydroxypropylmethyl cellulose acetyl succinate (HPMC-AS) coated granules and double layer coated granules with HPMC-AS and ethyl cellulose (EC), were prepared for the newly developed antihistaminergic drug, TA-5707F, using a centrifugal fluidizing granulator."( Preparation of controlled release granules of TA-5707F using enteric polymers and ethylcellulose, and their in vivo evaluation.
Maejima, T; Matsukawa, Y; Osawa, T; Yamakita, H, 1996
)
0.29
" The model (which is based on the Hopfenberg equation) takes into account the three dimensions of a tablet dosage form."( Modeling of drug release from erodible tablets.
Friedman, M; Goldberger, A; Hoffman, A; Katzhendler, I, 1997
)
0.3
" 75, 198-207, 1997) have suggested that dosing chemicals to newly weaned male rats for 1 month may yield a useful assay for antiandrogens."( The weanling male rat as an assay for endocrine disruption: preliminary observations.
Ashby, J; Lefevre, PA, 1997
)
0.3
"The objective of this study, was to examine the influence of critical formulation and processing variables as described in the AAPS/FDA Workshop II report on scale-up of oral extended-release dosage forms, using a hydrophilic polymer hydroxypropyl methylcellulose (Methocel K100LV)."( Identification of critical formulation and processing variables for metoprolol tartrate extended-release (ER) matrix tablets.
Augsburger, LL; Hussain, AS; Malinowski, HJ; Nellore, RV; Rekhi, GS; Tillman, LG, 1999
)
0.3
" Multiple unit dosage forms (MUDFs) were subsequently obtained by encapsulating the mini-matrix tablets into hard gelatin capsules."( Development and evaluation of a multiple-unit oral sustained release dosage form for S(+)-ibuprofen: preparation and release kinetics.
Cox, PJ; Khan, KA; Munday, DL; Sujja-areevath, J, 1999
)
0.3
" The release profiles of the different three-layer systems obtained were compared, to verify if PEO could efficiently replace HPMC in this type of dosage form."( High molecular weight polyethylene oxides (PEOs) as an alternative to HPMC in controlled release dosage forms.
Bruni, R; Conte, U; Maggi, L, 2000
)
0.31
" Adalat GITS 30 was used as a reference dosage form."( Preparation and evaluation of a sustained-release formulation of nifedipine HPMC tablets.
Ding, D; Li, H; Yan, G; Zhang, R, 2000
)
0.31
" The system was used to image the physical changes that occur in solid dosage forms during dissolution in the flow-through apparatus."( NMR imaging investigations of drug delivery devices using a flow-through USP dissolution apparatus.
Blazek-Welsh, AI; Chopra, SK; Fahie, BJ; Fyfe, CA; Grondey, H, 2000
)
0.31
" The aim of this tablet dosage form is to improve the oral absorption of ddI by delivering it in small doses over an extended period and localizing it in the intestine by bioadhesion."( Oral sustained-release bioadhesive tablet formulation of didanosine.
Betageri, GV; Deshmukh, DV; Gupta, RB, 2001
)
0.31
" The in vitro drug release of this kind of two-layer dosage was controlled by the amount of hydroxypropylmethylcellulose (HPMC) in the drug-loading layer."( Design and evaluation of a two-layer floating tablet for gastric retention using cisapride as a model drug.
Bi, D; Wei, Z; Yu, Z, 2001
)
0.31
"The permeabilities of mixed films of pectin/chitosan/HPMC have been studied to assess their value in producing a dosage form with biphasic drug release characteristics."( Biphasic drug release: the permeability of films containing pectin, chitosan and HPMC.
Fell, JT; Ofori-Kwakye, K, 2001
)
0.31
" In this study, a new dosage form was developed by including bioadhesive polymers (polycarbophyl, hydroxypropylmethylcellulose, and hyaluronic sodium salt) into pessaries made of semisynthetic solid triglycerides."( Development of a mucoadhesive dosage form for vaginal administration.
Ceschel, GC; Lombardi Borgia, S; Maffei, P; Ronchi, C; Rossi, S, 2001
)
0.31
"The ANN could be used for predicting the dissolution profiles of sustained release dosage form and for the design of optimal formulation."( [Application of an artificial neural network in the design of sustained-release dosage forms].
Liang, WQ; Wei, XH; Wu, JJ, 2001
)
0.31
"The sodium and potassium salts of the methacrylic copolymers Eudragit L100 and Eudragit S100 were prepared with the aim to develop new low-swellable mucoadhesive materials intended for the preparation of buccal dosage forms."( Polymethacrylate salts as new low-swellable mucoadhesive materials.
Casiraghi, A; Cilurzo, F; Minghetti, P; Montanari, L; Selmin, F, 2003
)
0.32
"Hydrophilic matrix tablets based on hydroxypropylmethylcellulose (HPMC) and other cellulose derivatives rank among dosage forms with retarded effect widely used in contemporary pharmacotherapy."( [Release of diltiazem chloride and ibuprofen from hydrophilic matrix tablets].
Medvecká, G; Rabisková, M; Vostalová, L, 2003
)
0.32
" Propranolol hydrochloride (propranolol HCl) is subjected to first-pass effect, therefore formulation of buccal-adhesive dosage form can circumvent this effect."( Development and evaluation of buccoadhesive propranolol hydrochloride tablet formulations: effect of fillers.
Adrangui, M; Akbari, J; Farid, D; Nokhodchi, A; Saeedi, M; Siahi-Shadbad, MR, 2004
)
0.32
" The present paper deals with the study and development of an oral dosage form devised to release drugs following a programmed time period after administration or, when opportune design modifications are introduced, to target the colon."( Different HPMC viscosity grades as coating agents for an oral time and/or site-controlled delivery system: a study on process parameters and in vitro performances.
Foppoli, A; Gazzaniga, A; Giordano, F; Maroni, A; Sangalli, ME; Zema, L, 2004
)
0.32
" In our study, dosage reform was conducted on the TCMCR model drug--Guanxin Suhe Wan (GSW), which is in the traditional form of honey bolus, comprising Styrax, Borneolumsyntheticum, Olbanum, Radix aristolochiae and Lignum santali albi."( Preparation and evaluation of pH-dependent gradient-release pellets for TCM.
Ci, L; Tang, X; Tian, X, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
anticonvulsantA drug used to prevent seizures or reduce their severity.
antiparkinson drugA drug used in the treatment of Parkinson's disease.
dopamine agonistA drug that binds to and activates dopamine receptors.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
hydrochlorideA salt formally resulting from the reaction of hydrochloric acid with an organic base.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
D(2) dopamine receptorHomo sapiens (human)Ki0.01150.00000.651810.0000AID1067731; AID1067760; AID1067761; AID1067762
D(3) dopamine receptorHomo sapiens (human)Ki0.00100.00000.602010.0000AID1067759
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00060.00000.437510.0000AID1067732
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (109)

Processvia Protein(s)Taxonomy
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID1067760Displacement of [3H]spiperone from low-affinity state of human dopamine D2S receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
AID1067732Displacement of dopamine/[3-H]domperidone from high-affinity state of rat D2L receptor2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
AID1067731Binding affinity to high-affinity state of D2L receptor (unknown origin)2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
AID1067761Displacement of [3H]spiperone from low-affinity state of human dopamine D2L receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
AID1067758Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
AID1067762Displacement of [3H]spiperone from high-affinity state of human dopamine D2L receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
AID1067759Displacement of [3H]spiperone from human dopamine D3 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
AID1067763Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
AID1067757Displacement of [3H]SCH23390 from human dopamine D5 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Synthesis and characterization of a novel series of agonist compounds as potential radiopharmaceuticals for imaging dopamine D₂/₃ receptors in their high-affinity state.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (179)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's58 (32.40)18.2507
2000's120 (67.04)29.6817
2010's1 (0.56)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.91

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index8.91 (24.57)
Research Supply Index5.32 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.91)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials14 (7.37%)5.53%
Reviews4 (2.11%)6.00%
Case Studies1 (0.53%)4.05%
Observational0 (0.00%)0.25%
Other171 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]