Dopamine Receptors

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  1. DAT and SLC6A2 inhibitor

    GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.
  2. dopamine re-uptake inhibitor

    Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI.
  3. dopamine D2 receptor agonist

    UNC 9994 hydrochloride, unique, beta-arrestin-biased functionally selective dopamine D2 receptor (D2R) agonist (Ki value 30 nM; EC50 value 50 nM in ??-arrestin-2 recruitment assay) that exhibits antipsychotic activity in vivo. UNC9994 markedly inhibited PCP-induced hyperlocomotion in wild-type mice, which effect was completely abolished in ??-arrestin-2 knockout mice.
  4. Reboxetine is an antidepressant compound that selectively inhibits norepinephrine uptake (IC50s = 8.2 and 1,070 nM for norepinephrine and serotonin transporters, respectively). It displays greater than 1,000-fold affinity for binding rat norepinephrine receptors compared to serotonin, histamine, acetylcholine, or dopamine receptors (Kis = 1.1, 129, 1,400, 3,900, and >10,000 nM, respectively).
  5. Domperidone blocks the action of dopamine. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which, among others, regulates nausea and vomiting (area postrema on the floor of the fourth ventricle and rhomboid fossa).
  6. H1 antagonist

    Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.
  7. Clozapine displays a broad range of pharmacological actions; the antipsychotic effects are thought to be mediated principally by 5-HT2A/2C and dopamine receptor blockade.
  8. dopamine receptor agonist

    Nalmefene hydrochloride is an opioid receptor antagonist.
  9. Dopamine Receptor agonist

    Rotigotine hydrochloride is a dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.
  10. dopamine D2 receptor antagonist

    Metoclopramide HCl is a selective dopamine D2 receptor antagonist.
  11. Dopamine Receptor antagonist

    Paliperidone(Invega) is an atypical antipsychotic.
  12. BP 897, is an antagonist at human dopamine D3 receptors and at rat somatodendritic dopamine D3 receptors
  13. dopamine D2-receptor antagonist

    Sulpiride is a dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid.
  14. D2 dopamine receptor antagonist

    L-741626 is a potent and selective antagonist for the dopamine receptor D2. It has good selectivity over the related D3 and D4 subtypes and other receptors.
  15. Dopamine D2 autoreceptor agonist

    NMI 8739 is a dopamine D2 autoreceptor agonist, which is an amine conjugate of the DHA carrier and the neurotransmitter dopamine.
  16. Dopamine receptor antagonist

    cis-(Z)-Flupentixol dihydrochloride is a dopamine receptor antagonist, antipsychotic, neuroleptic agent.
  17. Nur77 LBD Antagonist

    TMPA is a novel small molecule that binds to orphan Nuclear Receptor Nur77 with high affinity (Kd = 1.45 ?? 0.35 μM), and interferes with the Nur77-LKB1 interaction.
  18. dopamine release inhibitor

    Pentiapine is a novel dopamine release inhibitor.
  19. Pramipexole dihydrochloride is a dopamine receptor agonist exhibiting selectivity for the D3 receptor.
  20. serotonin/dopamine/norepinephrine reuptake inhibitior

    SPD-473 citrate is a serotonin/dopamine/norepinephrine reuptake inhibitior.
  21. D2 receptor antagonist

    Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7).
  22. Dopamine D3 receptor antagonist

    GR 103691 is an effective and selective receptor antagonist of the dopamine D3 receptor (D3DR).
  23. D1/D5 receptor antagonist

    SCH 23390 hydrochloride is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively).
  24. D2 agonist

    Naxagolide is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders.
  25. dopamine D2-receptor agonist

    ent Naxagolide Hydrochloride is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders. This compound is an antiparkinsonian drug.
  26. dopamine uptake inhibitor

    GBR 12783 dihydrochloride is a very potent and selective inhibitor of dopamine uptake (IC50 for inhibition of [3H]-dopamine uptake in rat striatal synaptosomes is 1.8 nM).
  27. D2 receptor antagonist

    Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms.
  28. D2 dopamine partial agonist

    Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD).
  29. dopamine β-hydroxylase (DBH) inhibitor

    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects.
  30. dopamine D3 Receptor (DRD3) antagonist

    GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.
  31. dopamine D2 receptor agonist

    Bromocriptine mesylate is a potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM).1,2 As a result, it has found applications in combination therapy for Parkinsonism.
  32. Dopamine receptor agonist

    Cabergoline, a lysergic acid amide derivative, is a potent dopamine D2 receptor agonist.
  33. dopaminergic agonist

    Pergolide mesylate is a dopaminergic agonist that also decrease plasma prolactin concentrations.
  34. Dopamine D2 Receptor Antagonist

    SB269652 is a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
  35. Dopamine receptor agonist

    (+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM).
  36. D2DR and D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia.
  37. Dopamine receptor antagonist

    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  38. Dopamine D1/2 receptor antagonist

    Melitracen HCl ia potential dopamine D1/2 receptor antagonist used to treat depression. It is often co-administered with flupenthixol as a treatment for trigeminal neuralgia. It does not effect cardiovascular function.
  39. D2DR inhibitor

    Promazine Hydrochloride is a phenothiazine compound and D2DR inhibitor. Promazine Hydrochloride has been employed in studies investigating dopamine-stimulated glycosylation of brain proteins in vitro. It has actions similar to chlorpromazine but with less antipsychotic activity.
  40. MAO inhibitor

    Molindone HCl is a D2 dopamine receptor antagonist. It also acts as a MAO inhibitor.
  41. D2 receptor blocker

    Trimethobenzamide hydrochloride is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.
  42. dopamine D2 receptor agonist

    Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor.
  43. Dopamine D2 antagonist

    Metoclopramide hydrochloride hydrate is a dopamine D2 antagonist that is used as an antiemetic.
  44. D2DR/D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
  45. Bromperidol, also known as Impromen and R-11333, is used as a means of long-term maintenance treatment of schizophrenia. Bromperidol is a close structural analogue of haloperidol. C3435T polymorphism is associated with some therapeutic response to bromperidol in schizophrenic patients, possibly by different drug concentration in the brain.
  46. 5-HT receptor /dopamine receptors antagonist

    Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
  47. Levomepromazine, also known as methotrimeprazine, is a phenothiazine neuroleptic drug. Levomepromazine is used for the treatment of psychosis, particularly those of schizophrenia, and manic phases of bipolar disorder.
  48. dopamine D2 receptor antagonist

    Haloperidol hydrochloride is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.
  49. Dopamine Receptor Agonist?€?

    SKF38393 HCl is a D1 agonist with IC50 of 110 nM.
  50. Nurr1 activator

    C-DIM12 is a novel synthetic activator of Nurr1. C-DIM12 induces dopaminergic gene expression and protects against 6-hydroxydopamine neurotoxicity in vitro.

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