dopamine d2 receptor antagonists


Summary: Compounds and drugs that bind to and inhibit or block the activation of DOPAMINE D2 RECEPTORS.

Top Publications

  1. Stahl S. Antipsychotic polypharmacy: never say never, but never say always. Acta Psychiatr Scand. 2012;125:349-51 pubmed publisher
  2. Wang S, Han C, Lee S, Jun T, Patkar A, Masand P, et al. Investigational dopamine antagonists for the treatment of schizophrenia. Expert Opin Investig Drugs. 2017;26:687-698 pubmed publisher
    ..However, the expected benefits of the newly developed antagonists may not be great because they offer little enhanced efficacy for negative symptoms, cognition and functional outcomes. ..
  3. da Costa I, Cavalcanti J, de Queiroz D, de Azevedo E, do Rêgo A, Araujo Filho I, et al. Supplementation with Herbal Extracts to Promote Behavioral and Neuroprotective Effects in Experimental Models of Parkinson's Disease: A Systematic Review. Phytother Res. 2017;31:959-970 pubmed publisher
    ..It is suggested that further studies need be conducted to better understand the mechanisms of action of the bioactive compounds distributed in these plants. Copyright © 2017 John Wiley & Sons, Ltd. ..
  4. Ozkan M, Johnson N, Sehirli U, Woodhall G, Stanford I. Dopamine acting at D1-like, D2-like and ?1-adrenergic receptors differentially modulates theta and gamma oscillatory activity in primary motor cortex. PLoS ONE. 2017;12:e0181633 pubmed publisher
    ..These results show that DA mediates complex actions acting at dopamine D1-like and D2-like receptors, ?1 adrenergic receptors and possibly DA/?1 heteromultimeric receptors to differentially modulate theta and gamma activity in M1. ..
  5. Leysen J, Janssen P, Megens A, Schotte A. Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994;55 Suppl:5-12 pubmed
    ..Moreover, it was observed that antagonism of strong D2-receptor stimulation by apomorphine in rats was achieved at less than 50% D2 occupancy by the antipsychotics.(ABSTRACT TRUNCATED AT 250 WORDS) ..
  6. Forray C, Buller R. Challenges and opportunities for the development of new antipsychotic drugs. Biochem Pharmacol. 2017;143:10-24 pubmed publisher
  7. Bielefeldt K. From Harmful Treatment to Secondary Gain: Adverse Event Reporting in Dyspepsia and Gastroparesis. Dig Dis Sci. 2017;62:2999-3013 pubmed publisher
    ..Knowing about common and uncommon, but potentially serious risks may enable patients and providers to decide on effective and safe management strategies. ..
  8. Lungu C, Aia P, Shih L, Esper C, Factor S, Tarsy D. Tardive dyskinesia due to aripiprazole: report of 2 cases. J Clin Psychopharmacol. 2009;29:185-6 pubmed publisher
  9. Ma G, Raivio N, Sabrià J, Ortiz J. Agonist and antagonist effects of aripiprazole on D₂-like receptors controlling rat brain dopamine synthesis depend on the dopaminergic tone. Int J Neuropsychopharmacol. 2014;18: pubmed publisher
    ..Such unusual effects were not seen with the typical partial agonist preclamol and are consistent with the hypothesis that aripiprazole is a functionally selective Dâ‚‚R ligand. ..

More Information


  1. Thomsen M, Barrett A, Butler P, Negus S, Caine S. Effects of Acute and Chronic Treatments with Dopamine D2 and D3 Receptor Ligands on Cocaine versus Food Choice in Rats. J Pharmacol Exp Ther. 2017;362:161-176 pubmed publisher
    ..With the possible exception of the D3 antagonist PG01037, no ligand was promising in terms of cocaine addiction treatment. ..
  2. Khan A, Khan J, Irfan M, Naqvi S, Khan G, Shoaib M, et al. Validation and application of high performance liquid chromatographic method for the estimation of metoclopramide hydrochloride in plasma. Pak J Pharm Sci. 2017;30:143-147 pubmed
    ..The method can be effectively used for estimation of metoclopramide HCl in plasma. ..
  3. Schwalbe T, Kaindl J, Hubner H, Gmeiner P. Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. Bioorg Med Chem. 2017;25:5084-5094 pubmed publisher
    ..The disulfide- and Michael acceptor-functionalized compounds showed significant receptor affinity and an irreversible binding profile in radioligand depletion experiments. ..