| Name | dopamine D2 receptor |
|---|---|
| Synonyms | D(2) dopamine receptor; D2DR; D2R; DRD 2; DRD2; Dopamine D2 receptor; Dopamine receptor D2; Dopamine D2 receptors… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 14556797 | Menegatti R, Cunha AC, Ferreira VF, Perreira EF, El-Nabawi A, Eldefrawi AT, Albuquerque EX, Neves G, Rates SM, Fraga CA, Barreiro EJ: Design, synthesis and pharmacological profile of novel dopamine D2 receptor ligands. Bioorg Med Chem. 2003 Nov 3;11(22):4807-13. The present study describes the synthesis and pharmacological profile of three novel heterocyclic compounds originally designed, on the basis of bioisosterism, as dopamine D2 receptor ligands: 1-[1-(4-chlorophenyl)-1H-pyrazol-4-ylmethyl]-4-phenyl-piperazine (LASSBio-579), 1-phenyl-4-(1-phenyl-1H-[1,2,3] triazol-4-ylmethyl)-piperazine (LASSBio-580) and 1-[1-(4-chlorophenyl)-1H-[1,2,3] triazol-4-ylmethyl]-4-phenyl-piperazine (LASSBio-581). |
82(1,1,1,2) | Details |
| 16554049 | Cosi C, Carilla-Durand E, Assie MB, Ormiere AM, Maraval M, Leduc N, Newman-Tancredi A: Partial agonist properties of the antipsychotics SSR181507, and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release. Eur J Pharmacol. 2006 Mar 27;535(1-3):135-44. Epub 2006 Mar 22. We compared the effects of the new antipsychotic agents SSR181507 ((3-exo)-8-benzoyl-N-[[(2 s) 7-chloro-2,3-dihydro-1,4-benzodioxin-1-yl] methyl]-8-azabicyclo [3.2.1] oct ane-3- monohydrochloride), bifeprunox (DU127090: 1-(2-Oxo-benzoxazolin-7-yl)-4-(3-biphenyl) methylpiperazinemesylate) and SLV313 (1-(2,3-dihydro-benzo [1,4] dioxin-5-yl)-4-[5-(4-fluorophenyl)-pyridin-3-ylm ethyl]-piperazine) with those of (7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]-butyloxy)-3,4-dihydro-2 (1 H)-quinolinone), clozapine and haloperidol, on functional measures of dopamine D2 receptor activity in vitro and in vivo: [35S]-GTPgammaS binding to membranes from Sf9 insect cells expressing human D2 Long (hD2 L) receptors, and serum prolactin levels in the rat. |
33(0,1,1,3) | Details |
| 16710314 | McCreary AC, Glennon JC, Ashby CR Jr, Meltzer HY, Li Z, Reinders JH, Hesselink MB, Long SK, Herremans AH, van Stuivenberg H, Feenstra RW, Kruse CG: SLV313 (1-(2,3-dihydro-benzo [1,4] dioxin-5-yl)-4- [5-(4--phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug. Neuropsychopharmacology. 2007 Jan;32(1):78-94. Epub 2006 May 17. |
31(0,1,1,1) | Details |
| 18305018 | Collins GT, Calinski DM, Newman AH, Grundt P, Woods JH: Food restriction alters N'-propyl-4,5,6,7-tetrahydrobenzothiazole-2,6-diamine dihydrochloride (pramipexole)-induced yawning, hypothermia, and locomotor activity in rats: evidence for sensitization of dopamine D2 receptor-mediated effects. J Pharmacol Exp Ther. 2008 May;325(2):691-7. Epub 2008 Feb 27. |
2(0,0,0,2) | Details |
| 15819386 | Sukalovic V, Zlatovic M, Andric D, Roglic G, Kostic-Rajacic S, Soskic V: Interaction of arylpiperazines with the dopamine receptor D2 binding site. Arzneimittelforschung. 2005;55(3):145-52. The results demonstrated that the interaction of protonated N1 of the piperazine ring with Asp 86 (III.32) and edge-to-face interactions of the aromatic ring of the arylpiperazine part of the ligand with 178 (VI.44), Trp 182 (VI.48) and Tyr 216 (VII.58) of the receptor, represent the major stabilizing forces. |
2(0,0,0,2) | Details |
| 15893022 | Sukalovic V, Andric D, Roglic G, Kostic-Rajacic S, Schrattenholz A, Soskic V: Synthesis, dopamine D2 receptor binding studies and docking analysis of 5-[3-(4-arylpiperazin-1-yl) propyl]-1H-benzimidazole, 5-[2-(4-arylpiperazin-1-yl) ethoxy]-1H-benzimidazole and their analogs. Eur J Med Chem. 2005 May;40(5):481-93. Epub 2005 Apr 1. The main features of ligand-D2 receptor interactions revealed by docking analyses were: salt bridge between piperazine ring protonated N1 and Asp 86, bonds of ligand bezimidazole part with Ser 141, Ser 122 and His 189, edge-to-face interactions of arylpiperazine aromatic ring with 178, Tyr 216 and Trp 182 and bond between ethereal in ethylenoxy ligands and of 185 or Trp 115. |
1(0,0,0,1) | Details |
| 11230993 | Rahman S, Engleman E, Simon J, McBride WJ: Negative interaction of dopamine D2 receptor antagonists and GBR 12909 and GBR 12935 uptake inhibitors in the nucleus accumbens. Eur J Pharmacol. 2001 Feb 23;414(1):37-44. The objective of this study was to examine the interaction of dopamine D2 receptor antagonists and uptake inhibitors on the regulation of extracellular release in the nucleus accumbens of Wistar rats employing in vivo microdialysis and in vitro uptake studies. Perfusion of the nucleus accumbens for 60 min with the uptake inhibitors, 1-[2-[bis (4-Fluorophenyl) methoxy] ethyl]-4-[3-phenylpropyl] piperazine dihydrochloride (GBR 12909; 100 microm) or 1-[2-(Diphenylmethoxy) ethyl]-4-(3-phenylpropyl)-piperazine dihydrochloride (GBR 12935; 100 microm) alone, increased the extracellular levels of in the nucleus accumbens to 400% and 350% of basal, respectively. |
1(0,0,0,1) | Details |
| 11892924 | Leslie RA: Gepirone. Curr Opin Investig Drugs. 2001 Aug;2(8):1120-7. Gepirone, a pyridinyl piperazine 5-HT1A receptor agonist, has been developed by Fabre-Kramer as an antidepressant. Mechanism of action studies have demonstrated that gepirone, compared to possesses a much greater selectivity for 5-HT1A receptors over dopamine D2 receptors. |
1(0,0,0,1) | Details |
| 17888556 | Korff S, Stein DJ, Harvey BH: Stereotypic behaviour in the deer mouse: pharmacological validation and relevance for obsessive compulsive disorder. Prog Neuropsychopharmacol Biol Psychiatry. 2008 Feb 15;32(2):348-55. Epub 2007 Aug 29. States of spontaneous stereotypy are attenuated by 5-HT (2A/C) and dopamine D2 receptor agonists. |
1(0,0,0,1) | Details |
| 15469457 | Briani C, Cagnin A, Chierichetti F, Tiberio M, Battistin L, Pizzolato G: Thiethylperazine-induced parkinsonism: in vivo demonstration of dopamine D2 receptors blockade. Eur J Neurol. 2004 Oct;11(10):709-10. Thiethylperazine is a piperazine phenothiazine employed to relieve vertigo. |
1(0,0,0,1) | Details |
| 16421514 | Auclair AL, Kleven MS, Besnard J, Depoortere R, Newman-Tancredi A: Actions of novel antipsychotic agents on apomorphine-induced PPI disruption: influence of combined 5-HT1A receptor activation and dopamine D2 receptor blockade. Neuropsychopharmacology. 2006 Sep;31(9):1900-9. Epub 2006 Jan 18. |
1(0,0,0,1) | Details |
| 16497294 | Bruins Slot LA, De Vries L, Newman-Tancredi A, Cussac D: Differential profile of antipsychotics at 5-HT1A and D2S receptors coupled to extracellular signal-regulated kinase. Eur J Pharmacol. 2006 Mar 18;534(1-3):63-70. Epub 2006 Feb 21. In contrast, SLV313, also an efficacious 5-HT1A receptor agonist, acted as a high potency dopamine D2 receptor antagonist. |
1(0,0,0,1) | Details |