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Results for "

human D4 receptors

" in MedChemExpress (MCE) Product Catalog:

49

Inhibitors & Agonists

15

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19989
    MK-571
    Maximum Cited Publications
    33 Publications Verification

    L-660711

    		 P-glycoprotein LPL Receptor Leukotriene Receptor Inflammation/Immunology
    MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
    MK-571
  • HY-19989A
    MK-571 sodium
    Maximum Cited Publications
    33 Publications Verification

    L-660711 sodium

    		 P-glycoprotein LPL Receptor Leukotriene Receptor Inflammation/Immunology
    MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
    MK-571 sodium
  • HY-B0075S
    Melatonin-d4

    N-Acetyl-5-methoxytryptamine-d4

    		 Isotope-Labeled Compounds Melatonin Receptor Autophagy Mitophagy Apoptosis Neurological Disease Inflammation/Immunology Cancer
    Melatonin-d4 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties . Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation .
    Melatonin-d4
  • HY-101348
    L-741626
    2 Publications Verification

    		 Dopamine Receptor Neurological Disease
    L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
    L-741626
  • HY-100820
    Sarizotan
    1 Publications Verification

    EMD 128130

    		 5-HT Receptor Dopamine Receptor Neurological Disease
    Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively .
    Sarizotan
  • HY-18137
    PF-04995274

    		5-HT Receptor Neurological Disease
    PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease .
    PF-04995274
  • HY-116941
    A-381393

    		Dopamine Receptor Neurological Disease
    A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM) .
    A-381393
  • HY-12765S
    Losartan-d4 (carboxylic acid)

    E-3174 d4; EXP-3174 d4

    		 Angiotensin Receptor Cardiovascular Disease Endocrinology Cancer
    Losartan-d4 carboxylic acid (E-3174-d4) is the deuterium labeled Losartan Carboxylic Acid (HY-12765). Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.
    Losartan-d4 (carboxylic acid)
  • HY-116326
    BayCysLT2

    		Leukotriene Receptor Inflammation/Immunology
    BayCysLT2, an isophthalic acid derivative, is a selective and potent cysteinyl leukotriene 2 (CysLT2) receptor antagonist with an IC50 value of 53 nM. BayCysLT2 inhibits calcium mobilization induced by leukotriene D4 in HEK293 cells expressing human CysLT2 receptors. BayCysLT2 reverses LTC4-induced increases in coronary artery perfusion pressure and decreases in contractility in isolated perfused guinea pig hearts .
    BayCysLT2
  • HY-14325
    L-745870
    3 Publications Verification

    		 Dopamine Receptor Neurological Disease
    L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
    L-745870
  • HY-14325B
    L-745870 hydrochloride
    3 Publications Verification

    		 Dopamine Receptor Neurological Disease
    L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
    L-745870 hydrochloride
  • HY-103409
    ABT-724 trihydrochloride

    		Dopamine Receptor Neurological Disease
    ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
    ABT-724 trihydrochloride
  • HY-16985S
    Darolutamide-d4

    ODM-201-d4; BAY-1841788-d4

    		 Isotope-Labeled Compounds Androgen Receptor Cancer
    Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide-d4
  • HY-14330
    ABT-724

    		Dopamine Receptor Neurological Disease
    ABT-724, a chemical probe, is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
    ABT-724
  • HY-W011926S
    Diisopropyl phthalate-d4

    DiPP-d4

    		 Isotope-Labeled Compounds Estrogen Receptor/ERR Others
    Diisopropyl phthalate-d4 (DiPP-d4) is the deuterium labeled Diisopropyl Phthalate (HY-W011926). Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC50 of 41000 μM .
    Diisopropyl phthalate-d4
  • HY-103405A
    NGD 94-1 dimaleate

    		Dopamine Receptor Neurological Disease
    NGD 94-1 (dimaleate) is a potent and selective dopamine D4 receptor antagonist. NGD 94-1 (dimaleate) shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD 94-1 (dimaleate) modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD 94-1 (dimaleate) can be used for neurological disease research [1][2].
    NGD 94-1 dimaleate
  • HY-19483
    ABT-670

    		Dopamine Receptor Neurological Disease
    ABT-670 is a selective, oral bioavailable agonist of dopamine D4 receptor, with EC50 of 89 nM, 160 nM, and 93 nM for human D4, ferret D4, and rat D4, respectively.
    ABT-670
  • HY-103104
    Fananserin

    RP 62203

    		 5-HT Receptor Dopamine Receptor Neurological Disease
    Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor .
    Fananserin
  • HY-123663
    U-101958 maleate

    PNU-101958 maleate

    		 Dopamine Receptor Neurological Disease
    U-101958 (PNU-101958) maleate is a highly selective ligand and antagonist for dopamine D4 receptor, with an IC50 of 2.7 nM. U-101958 maleate behaves as an agonist in HEK-293 cells expressing the human recombinant D4.4 receptor. U-101958 maleate is an antipsychotic .
    U-101958 maleate
  • HY-50935S
    Troglitazone-d4

    CS-045-d4

    		 Isotope-Labeled Compounds PPAR Autophagy Apoptosis Ferroptosis Cancer
    Troglitazone-d4 is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
    Troglitazone-d4
  • HY-115417
    Bosentan-d4

    		Endothelin Receptor Cardiovascular Disease Endocrinology
    Bosentan-d4 is the deuterium labeled Bosentan. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
    Bosentan-d4
  • HY-133677S
    Mono(2-ethyl-5-hydroxyhexyl) phthalate-d4

    MEHHP-d4

    		 Isotope-Labeled Compounds Drug Metabolite Apoptosis Aryl Hydrocarbon Receptor Cancer
    Mono(2-ethyl-5-hydroxyhexyl) phthalate-d4 (MEHHP-d4) is a deuterium labeled Mono(2-ethyl-5-hydroxyhexyl) phthalate (HY-133677). Mono (2-ethyl-5-hydroxyhexyl) phthalate is a biomarker for human exposure to DEHP (HY-B1945). By activating the tryptophan-kynurenine-aryl hydrocarbon receptor (AhR) pathway, mono (2-ethyl-5-hydroxyhexyl) phthalate significantly increases the viability of primary uterine leiomyoma cells and reduces cell apoptosis. Mono (2-ethyl-5-hydroxyhexyl) phthalate correlates with decreased sperm DNA damage. Mono (2-ethyl-5-hydroxyhexyl) phthalate can be used in studies related to uterine leiomyoma.
    Mono(2-ethyl-5-hydroxyhexyl) phthalate-d4
  • HY-17038S1
    Agomelatine-d4

    S-20098-d4

    		 Isotope-Labeled Compounds Melatonin Receptor 5-HT Receptor Endogenous Metabolite Neurological Disease
    Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
    Agomelatine-d4
  • HY-103405
    NGD94-1

    		Dopamine Receptor Neurological Disease
    NGD94-1 is a potent and selective dopamine D4 receptor antagonist. NGD94-1 shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD94-1 modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD94-1 can be used for neurological disease research [1][2].
    NGD94-1
  • HY-14325R
    L-745870 (Standard)

    		Dopamine Receptor Neurological Disease
    L-745870 (Standard) is the analytical standard of L-745870. This product is intended for research and analytical applications. L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
    L-745870 (Standard)
  • HY-101349
    L 741742

    		Dopamine Receptor Apoptosis Autophagy PDGFR ERK mTOR Neurological Disease Cancer
    L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma .
    L 741742
  • HY-173431
    Dopamine D4 receptor ligand 3

    		Dopamine Receptor Reactive Oxygen Species (ROS) Cancer
    Dopamine D4 receptor ligand 3 (Compound 16) is a dopamine D4 receptor (D4R) antagonist (pKi: 8.86). Dopamine D4 receptor ligand 3 has pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors in HEK-293T cells, respectively. Dopamine D4 receptor ligand 3 inhibits the viability of three human glioma cell lines, U87 MG, T98G, and U251 MG. Dopamine D4 receptor ligand 3 induces ROS production and mitochondrial dysfunction in glioma cells .
    Dopamine D4 receptor ligand 3
  • HY-14544AS
    Quetiapine-d4 hydrochloride

    ICI204636-D4 hydrochloride

    		 Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor Neurological Disease
    Quetiapine-d4 (hydrochloride) (ICI204636-d4 (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
    Quetiapine-d4 hydrochloride
  • HY-129103
    A-412997

    		Dopamine Receptor Neurological Disease
    A-412997 is a selective Dopamine D4 agonist with Ki values of 12 and 7.9 nM for the rat and human receptors. A-412997 improves short term memory and cognitive properties in rodent models .
    A-412997
  • HY-15731S
    Estetrol-d4

    		Isotope-Labeled Compounds Estrogen Receptor/ERR Endogenous Metabolite Cardiovascular Disease
    Estetrol-d4 is the deuterium labeled Estetrol. Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast .
    Estetrol-d4
  • HY-151546S
    MRS4596-d4

    		Isotope-Labeled Compounds P2X Receptor Neurological Disease
    MRS4596-d4 is the deuterium labeled MRS4596 (HY-151546). MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke .
    MRS4596-d4
  • HY-100820B
    Sarizotan dihydrochloride

    EMD 128130 dihydrochloride

    		 5-HT Receptor Dopamine Receptor Neurological Disease
    Sarizotan dihydrochloride (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively .
    Sarizotan dihydrochloride
  • HY-100820A
    Sarizotan hydrochloride

    EMD 128130 hydrochloride

    		 5-HT Receptor Dopamine Receptor Neurological Disease
    Sarizotan hydrochloride is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan hydrochloride (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively .
    Sarizotan hydrochloride
  • HY-101349A
    L 741742 hydrochloride

    		Dopamine Receptor Apoptosis Autophagy PDGFR ERK mTOR Neurological Disease Cancer
    L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma .
    L 741742 hydrochloride
  • HY-19186
    PD-143188

    CI 1007

    		 Dopamine Receptor Neurological Disease
    PD-143188 (CI 1007) is a selective agonist targeting dopamine (DA) receptors, with Ki values of 25.5 nM and 16.6 nM for human D2 and D3 receptors, respectively and lower affinity for D4.2 receptors (Ki=90.9 nM). PD-143188 inhibits DA release, synthesis and metabolism, while reducing cellular cyclic AMP levels, exerting antipsychotic activity. PD-143188 is promising for research of psychopharmacology .
    PD-143188
  • HY-B0031S5
    Quetiapine-d4-1 fumarate

    		Dopamine Receptor 5-HT Receptor Isotope-Labeled Compounds Neurological Disease
    Quetiapine-d4-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
    Quetiapine-d4-1 fumarate
  • HY-100820R
    Sarizotan (Standard)

    EMD 128130 (Standard)

    		 Reference Standards 5-HT Receptor Dopamine Receptor Neurological Disease
    Sarizotan (Standard) is the analytical standard of Sarizotan. This product is intended for research and analytical applications. Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively .
    Sarizotan (Standard)
  • HY-100490S
    Rilmenidine-d4

    		Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy Cardiovascular Disease Cancer
    Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
    Rilmenidine-d4
  • HY-15731S1
    Estetrol-d4 (Major)

    		Isotope-Labeled Compounds NO Synthase Endogenous Metabolite Estrogen Receptor/ERR Cardiovascular Disease
    Estetrol-d4 (Major) is the deuterium labeled Estetrol (HY-15731). Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .
    Estetrol-d4 (Major)
  • HY-12765S1
    Losartan carboxylic acid-d4 hydrochloride

    		Isotope-Labeled Compounds Angiotensin Receptor Cardiovascular Disease
    Losartan carboxylic acid-d4 (hydrochloride) is deuterium labeled Losartan Carboxylic Acid. Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure .
    Losartan carboxylic acid-d4 hydrochloride
  • HY-100057
    BMY 28674

    6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215

    		 5-HT Receptor Drug Metabolite Dopamine Receptor Neurological Disease
    BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC50s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC50s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.
    BMY 28674
  • HY-14325BR
    L-745870 hydrochloride (Standard)

    		Dopamine Receptor Neurological Disease
    L-745870 (hydrochloride) (Standard) is the analytical standard of L-745870 (hydrochloride). This product is intended for research and analytical applications. L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
    L-745870 hydrochloride (Standard)
  • HY-103409R
    ABT-724 trihydrochloride (Standard)

    		Reference Standards Dopamine Receptor Neurological Disease
    ABT-724 trihydrochloride (Standard) is the analytical standard of ABT-724 trihydrochloride (HY-103409). This product is intended for research and analytical applications. ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
    ABT-724 trihydrochloride (Standard)
  • HY-15498S
    Rimegepant-d4

    BMS-927711-d4; BHV-3000-d4

    		 Isotope-Labeled Compounds CGRP Receptor Neurological Disease
    Rimegepant-d4 (BMS-927711-d4) is the deuterium labeled Rimegepant (HY-15498). Rimegepant (BMS-927711) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC50 of 8.01 and a Ki of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .
    Rimegepant-d4
  • HY-103104R
    Fananserin (Standard)

    RP 62203 (Standard)

    		 Reference Standards 5-HT Receptor Dopamine Receptor Neurological Disease
    Fananserin (Standard) is the analytical standard of Fananserin (HY-103104). This product is intended for research and analytical applications. Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor .
    Fananserin (Standard)
  • HY-101348R
    L-741626 (Standard)

    		Reference Standards Dopamine Receptor Neurological Disease
    L-741626 (Standard) is the analytical standard of L-741626. This product is intended for research and analytical applications. L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
    L-741626 (Standard)
  • HY-111241
    SV 293

    		Dopamine Receptor Neurological Disease
    SV 293 is a selective antagonist with neutral antagonist activity. SV 293 binds to human D2 receptors with 100-fold higher affinity and has lower affinity for human D3 and D4 dopamine receptor subtypes. SV 293 was found to block the effects of the full agonist quinpirole in forskolin-dependent adenylate acylase inhibition assays and electrophysiological assays. SV 293 can be used as a useful pharmacological tool to study the role of dopamine D2-like receptor subtypes in dopamine pathways associated with neurological, neuropsychiatric and movement disorders .
    SV 293
  • HY-121675A
    2-Bromo-LSD D-Tartrate

    BOL-148 D-Tartrate; Bromolysergide D-Tartrate

    		 5-HT Receptor G protein-coupled Bile Acid Receptor 1 Neurological Disease
    2-Bromo-LSD D-Tartrate (BOL-148 D-Tartrate) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD D-Tartrate lacks 5-HT2B agonist activity. 2-Bromo-LSD D-Tartrate induces dendritogenesis and spinogenesis. 2-Bromo-LSD D-Tartrate reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
    2-Bromo-LSD D-Tartrate
  • HY-181049
    FMJ-01-054

    		Dopamine Receptor Neurological Disease
    FMJ-01-054 is a selective dopamine D4 Receptor (D4R) antagonist with a Ki od 77.7 nM. FMJ-01-054 shows subtype selectivity over D2R and D3R. FMJ-01-054 inhibits D4R-mediated β-arrestin recruitment and cAMP production with IC50 values of 3800 nM and 134 nM, respectively. FMJ-01-054 has desirable plasma half-life and brain exposure in rats. FMJ-01-054 can be used for the research of neurological disorders .
    FMJ-01-054

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