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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
62 Results for "
D3R
" in MedChemExpress (MCE) Product Catalog:
Products (62)
62 Results for "D3R" in MCE Product Catalog:
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2
2 Cited Publications
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ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons .
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2 Cited Publications
Synonyms: Ordenina hydrochloride; Peyocactine hydrochloride
1
1 Cited Publications
Synonyms: SB-277011A hydrochloride
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SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively .
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 [3].
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 .
Cat. No.: HY-17514S1
CAS No.: 1217512-35-0
Synonyms: R51211-d3
Cat. No.: HY-149337
CAS No.: 2983777-91-7
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D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling .
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PG01037 dihydrochloride is a blood-brain barrier-penetrant selective dopamine D3 receptor antagonist, and blocks D3R signaling in the nucleus accumbens, with a Ki of 0.7 nM. PG01037 dihydrochloride enhances psychostimulant-induced locomotion, locomotor sensitization, and dopamine release, and promotes excitation of D1-expressing medium spiny neurons through D1-like signaling. PG01037 dihydrochloride attenuates psychostimulant-associated reward and relapse behaviors, and alleviates MPTPp-induced motor impairment and dopaminergic neurodegeneration. PG01037 dihydrochloride can be used in research related to Parkinson's disease, addictive disorders, and cancer [3] .
Cat. No.: HY-N0113S
CAS No.: 1346598-66-0
Synonyms: Ordenina-d6; Peyocactine-d6
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Isotope-Labeled Compounds Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
Hordenine-d6 (Ordenina-d6; Peyocactine-d6) is the deuterated-labeled Hordenine (HY-N0113). Hordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder [3] .
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-176287
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ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
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SK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC50 of 1109 nM. SK609 hydrochloride has the potential for parkinson research .
Cat. No.: HY-78131BS
CAS No.: 121702-86-1
Synonyms: (R)-Ibuprofen-d3
Cat. No.: HY-149386
CAS No.: 3033883-15-4
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D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
Cat. No.: HY-149387
CAS No.: 3033883-17-6
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D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
Cat. No.: HY-123889
CAS No.: 1982347-43-2
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VK4-116 (Compound 19) is a selective Dopamine D3 receptor (D3R) antagonist with a Ki of 6.84 nM.VK4-116 significantly inhibits Oxycodone-induced hyperlocomotion and locomotor sensitization in mouse models. VK4-116 with pretreatment also inhibits the acquisition of Oxycodone-induced conditioned place preference (CPP) in rat models .
Cat. No.: HY-144856S1
CAS No.: 2747956-15-4
Synonyms: (6R)-BH4-d3; (6R)-Tetrahydro-L-biopterin-d3
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-111280
CAS No.: 854924-64-4
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ST 198 is an orally active D3R antagonist. ST 198 can block the expression of nicotine-induced CPP at doses selective for D3R. ST 198 can be used for the research of neurological disease .
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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
