D2 Receptor Antagonist
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5-HT1AR/5-HT6R ligand-1
0 ImagesCat. No.: HY-1730445-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM.
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Tropapride
0 ImagesCat. No.: HY-130041CAS No.: 76352-13-1Synonyms: MD 790501Tropapride is a dopamine D2 receptor antagonist. Tropapride can be used for the research of neurological disease.
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Norzine dimalate
0 ImagesCat. No.: HY-A0188CAS No.: 52239-63-1Synonyms: Thiethylperazine dimalateNorzine dimalate (Thiethylperazine dimalate), a Phenothiazine (HY-Y0055) derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Norzine dimalate is also a selective ABCC1activator that reduces amyloid-β load in mice. Norzine dimalate has anti-emetic, antipsychotic and antimicrobial effects.
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Octoclothepin dimaleate
0 ImagesCat. No.: HY-106587BCAS No.: 41932-42-7Synonyms: Clorotepine dimaleateOctoclothepin (Clorotepine) dimaleate is a D2 dopamine receptor antagonist and 5-HT2 serotonin receptor antagonist , with Ki values of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D2, 5-HT2A, and 5-HT2C receptors, respectively. Octoclothepin dimaleate also binds to adrenergic receptors, with Ki values of 0.66 nM, 0.56 nM, and 0.77 nM for α1a, α1b, and α1d, respectively. Octoclothepin dimaleate can be used in schizophrenia research.
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L 741742 hydrochloride
0 ImagesCat. No.: HY-101349ACAS No.: 874882-93-6L 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.
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Melperone hydrochloride
0 ImagesMelperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly.
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L-745870 trihydrochloride
0 ImagesCat. No.: HY-14325ACAS No.: 866021-03-6L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride 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.
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Aramisulpride hydrochloride
0 ImagesCat. No.: HY-109167ACAS No.: 2129505-46-8Synonyms: (R)-Amisulpride hydrochloride; (R)-Esamisulpride hydrochloride; (R)-DAN 2163 hydrochlorideAramisulpride hydrochloride is a 5-HT7 receptor antagonist with a Ki value of 22 nM. Aramisulpride hydrochloride 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 hydrochloride can be used in psychiatric research.
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Tiapride
0 ImagesCat. No.: HY-B1196ACAS No.: 51012-32-9Tiapride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride shows anti-dyskinetic activity and anxiolytic activity. Tiapride is a neuroleptic agent.
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SV 156
0 ImagesCat. No.: HY-111242CAS No.: 873445-60-4SV 156 is a potent and selective D2 dopamine receptor antagonist, with a Ki of 2.5 nM for hD2. SV 156 has approximately 40-fold binding selectivity for D2 dopamine receptors compared to the D3 receptor subtype. SV 156 can be used for L-DOPA (HY-N0304)-associated abnormal involuntary movements (AIMs) research.
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(S)-Remoxipride
0 ImagesCat. No.: HY-101313CAS No.: 80125-14-0Synonyms: (-)-Remoxipride(S)-Remoxipride ((-)-Remoxipride) is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride can be used for the research of psychotic disorder.
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Blonanserin-d8
0 ImagesCat. No.: HY-13575SCAS No.: 2732761-71-4Synonyms: AD-5423-d8Blonanserin-d8 is a deuterium labeled Blonanserin. Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic.
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FMJ-01-054
0 ImagesCat. No.: HY-181049FMJ-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.
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Promazine
0 ImagesPromazine (Romtiazin) is an antipsychotic and a dopamine receptor D2 antagonist. Promazine inhibits dopaminergic neurotransmission.
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Raclopride tartrate
0 ImagesCat. No.: HY-108976CAS No.: 98185-20-7Raclopride tartrate is a selective dopamine D2/D3 receptor antagonist with potential antipsychotic effects. Raclopride tartrate binds to D2 and D3 receptors with Kis of 1.8 nM and 3.5 nM, respectively.
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Mazapertine
0 ImagesMazapertine is an orally active antipsychotic agent. M azapertine antagonizes to dopamine D2/3/4 receptors (Ki values < 3 nM) and also strongly binds to serotonin 5-HT1A receptor (Ki =1.7 nM) and α1-adrenergic receptor (Ki = 1.3 nM). Mazapertine can be used for the research of neurological disease.
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Cinitapride monotartrate
0 ImagesCat. No.: HY-128386CAS No.: 1207859-16-2Cinitapride monotartrate is a 5-HT1A and 5-HT4 agonist. Cinitapride monotartrate is also a 5-HT2A and D2 antagonist. Cinitapride monotartrate can be used for the research of functional dyspepsia.
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Metopimazine acid-d6 (hydrochloride)
0 ImagesCat. No.: HY-143994SMetopimazine-d6 hydrochloride is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks.
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Bromopride hydrochloride
0 ImagesCat. No.: HY-B1164ACAS No.: 52423-56-0Bromopride hydrochloride is a selective, irreversible, competitive, and orally active dopamine D2 receptor antagonist. Bromopride hydrochloride can pass through the blood-brain barrier, inhibit the vomiting center, and enhance gastrointestinal motility, exerting antiemetic and gastrointestinal motility effects. Bromopride hydrochloride antagonizes dopamine-mediated vomiting reflexes and promotes gastrointestinal smooth muscle contraction, and has no adverse effects on abdominal wall healing in rats with postoperative abdominal infection. Bromopride hydrochloride can be used for the study of digestive system diseases (such as gastric hypomotility, nausea and vomiting).
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NRA-0562
0 ImagesCat. No.: HY-182504CAS No.: 244276-65-1NRA‑0562 is a dopamine antagonist with high affinities for dopamine D1/D2/D3/D4, 5‑HT2A and α1‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED50 = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia..
