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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
41 Results for "
D2R
" in MedChemExpress (MCE) Product Catalog:
Products (41)
41 Results for "D2R" in MCE Product Catalog:
2
2 Cited Publications
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Aripiprazole lauroxil, an N-acyloxymethyl proagent of Aripiprazole (HY-14546), is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia and a ligand of dopamine receptor D2R/D4R. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity.
2
2 Cited Publications
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UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .
2
2 Cited Publications
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UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity .
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Prochlorperazine dimaleate is an orally active phenothiazine-type dopamine D2 receptor (D2R) antagonist. Prochlorperazine exhibits anti-cancer activity in vitro against various cancer cell lines. Prochlorperazine dimaleate exhibits IC50 values of 6.4 μM, 4.5 μM and 2.3 μM for NOX1, NOX2 and NOX5, respectively. Prochlorperazine dimaleate has antedesmosidic activity against dengue virus (DENV). Prochlorperazine dimaleate can be used for research on nausea, vomiting, migraine, and schizophrenia [2] .
Synonyms: ACR16; ASP2314; FR310826
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Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
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MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM) [2].
Synonyms: (S)-Amisulpride; (S)-Aramisulpride; (S)-DAN 2163
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Esamisulpride ((S)-Amisulpride) is the S-isomer of Amisulpride (HY-14545). Esamisulpride is a potent dopamine D2/D3 receptor antagonist with Ki values of 4.43 nM for D2R and 0.72 nM for D3R. Esamisulpride is a 5-HT7 receptor antagonist with a Ki of 900 nM. Esamisulpride can be used in the research of schizophrenia and depression [2] .
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Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity .
Synonyms: (R)-Amisulpride; (R)-Esamisulpride; (R)-DAN 2163
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Aramisulpride (R-(+)-Amisulpride) is the R-isomer of Amisulpride (HY-14545). Aramisulpride is a 5-HT7 receptor antagonist with a Ki value of 22 nM. Aramisulpride is a D2/D3 receptor antagonist with a Ki value of 140 nM for D2R and a Ki value of 13.9 nM for D3R. Aramisulpride can be used in psychiatric research [2].
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SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
Cat. No.: HY-P3294
CAS No.: 778630-77-6
Synonyms: BIM-23A760; TBR-760
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Cat. No.: HY-P10450
CAS No.: 220846-62-8
Synonyms: D2R; (D)2-Rhodamine 110
Cat. No.: HY-175504
CAS No.: 932544-59-7
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MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .
Cat. No.: HY-129089
CAS No.: 81264-57-5
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(-)-MDO-NPA is an N-propylnorapomorphine analog and a D1R/D2R dual-target ligand. (-)-MDO-NPA has EC50 values of 1949 nM (D1R) and 520 nM (D2R) for β-arrestin. (-)-MDO-NPA has EC50 values of 717.5 nM (D1R) and 7.7 nM (D2R) for cAMP. (-)-MDO-NPA can be used in the research of dopamine-related diseases such as Parkinson’s disease .
Cat. No.: HY-W004758
CAS No.: 38212-33-8
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1-(4-Chlorophenyl)piperazine is a chemical intermediate, and can be used for synthesis of D2R ligand .
Cat. No.: HY-116445
CAS No.: 1354030-19-5
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UNC9975 is a D2R agonist that displays signaling bias via β-arrestin–ergic signaling and a simultaneously antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9975 can be utilized in antipsychotic research .
Cat. No.: HY-156239
CAS No.: 2899250-94-1
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Dopamine D3 receptor ligand-5 (13a), a Cariprazine (HY-14763) analogue, is a dopamine D3 receptor ligand, with Ki values of 2.85 nM and 0.14 nM for D2R and D3R, respectively .
Cat. No.: HY-175532
CAS No.: 3062458-27-6
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M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
Cat. No.: HY-124583
CAS No.: 2040055-84-1
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PF-4363467, a dopamine D3/D2 receptor antagonist, attenuates opioid drug-seeking behavior without
concomitant D2 side effects. PF-4363467 exhibits Ki values of 3.1 nM and 692 nM for D3R and D2R .
Cat. No.: HY-123788
CAS No.: 1953181-29-7
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BRD5814 is a D2R antagonist. BRD5814 can be used in schizophrenia research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
