Dopamine Receptors

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  1. dopamine re-uptake inhibitor

    Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI.
  2. DAT and SLC6A2 inhibitor

    GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.
  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 Receptor antagonist

    Paliperidone(Invega) is an atypical antipsychotic.
  11. dopamine D2 receptor antagonist

    Metoclopramide HCl is a selective dopamine D2 receptor antagonist.
  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. Amfebutamone (Bupropion) is an atypical antidepressant and smoking cessation aid.
  16. Dopamine Receptor antagonist

    Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.
  17. Chlorprothixene exerts strong antagonism at the following receptors: 5-HT2; D1, D2, D3; H1;mACh; α1-adrenergic.
  18. Dopamine (abbreviated as DA), a simple organic chemical in the catecholamine family, is a monoamine neurotransmitter - a chemical released by nerve cells to send signals to other nerve cells.
  19. CYP2D6 inhibitor

    Haloperidol (Haldol) is an antipsychotic and butyrophenone.
  20. dopamine beta-hydroxylase inhibitor

    Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.
  21. 5-HT Receptors/D2 dopamine receptor antagonist

    Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
  22. Dopamine Receptor Agonist

    Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating early-stage Parkinson's disease (PD) and restless legs syndrome (RLS).
  23. Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorder.
  24. D2 dopamine agonist

    U-95666E is a D2 selective dopamine agonist with an ED50 of about 46 nM, was investigated for its effect on rat striatal acetylcholine (ACh) concentration
  25. 5-HT (serotonin) and dopamine receptor antagonist

    Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  26. Piribedil D8 is the deuterium labeled Piribedil, which is an antiparkinsonian agent.
  27. partial dopamine D2 and D3 receptor agonist

    Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.
  28. triple reuptake inhibitor

    Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
  29. D1/D5 receptor full agonist

    SKF-82958 hydrobromide is a D1/D5 receptor full agonist.
  30. D1/D5 receptor full agonist

    SKF 82958 is a D1/D5 receptor full agonist.
  31. dopamine reuptake inhibitor

    Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM).
  32. D1-like dopamine receptor (D1/D5) agonist

    Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity.
  33. dopamine reuptake inhibitor

    GBR 12935 is a potent, and selective dopamine reuptake inhibitor.
  34. dopamine D2 receptor antagonist

    Haloperidol D4 is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.
  35. dopamine D2 receptor antagonist

    Haloperidol-d4-1 is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.

  36. dopamine D4 receptor partial agonist

    Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
  37. 5-HT / dopamine receptor antagonist

    Ziprasidone D8 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  38. dopamine D2/D3 receptor antagonist

    Amisulpride hydrochloride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
  39. D2R antagonist

    Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist.
  40. analgesic agent

    Tetrahydropalmatine hydrochloride (DL-Tetrahydropalmatine hydrochloride), an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
  41. dopamine D2 receptor antagonist

    Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor.
  42. dopamine D4 receptor agonist

    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.
  43. dual dopamine and serotonin receptor antagonist

    Deschloroclozapine is a dual dopamine and serotonin receptor antagonist with Kis of 200, 2500, 420, 39, 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, respectively.
  44. monoamine reuptake inhibitor

    Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
  45. dual NE/DA transporter inhibitor

    Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  46. D3 receptor and D2 receptor partial agonist

    Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
  47. dopamine D3 receptor antagonist

    SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
  48. dopamine D2 receptor antagonist

    Risperidone hydrochloride is a serotonin 5-HT2 receptor blocker and a potent dopamine D2 receptor antagonist, with Kis of 0.16, 1.4 nM for 5-HT2 and D2 receptor, respectively.
  49. dopamine D2 receptor antagonist

    Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT2 receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 receptor antagonist(Ki= 1.4 nM).
  50. dopamine D2 receptor antagonist

    JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D2 receptor antagonist with a moderate binding affinity for the dopamine D2L receptor (Ki =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder.

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