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DRD2  -  dopamine receptor D2

Canis lupus familiaris

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Disease relevance of DRD2

  • The effects of quinpirole, a specific dopamine D2 receptor agonist, were investigated on cardiovascular responses and plasma levels of catecholamines and vasopressin in two groups of conscious dogs: (1) control dogs and (2) dogs with diabetes insipidus (i.e. animals surgically deprived of vasopressin) [1].
  • The emesis induced by cisplatin (3 mg/kg, i.v.) was inhibited by the intravenous administration of ICS205930 (2 x 0.01 or 2 x 0.1 mg/kg) and MDL72222 (2 x 0.5 mg/kg), 5-HT3 receptor antagonists, but not by the intravenous administration of metoclopramide (2 x 0.5 mg/kg), a dopamine D2 receptor antagonist [2].

High impact information on DRD2


Biological context of DRD2


Anatomical context of DRD2


Associations of DRD2 with chemical compounds

  • Effects of dopamine D1 and dopamine D2 receptor agonists on coronary and peripheral hemodynamics [5].
  • Among the compounds, 5-chloro-N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)-2-methoxy-4-methylaminobenzamide (82), 5-bromo (110), and 5-iodo (112) analogues exhibited a much higher affinity for the dopamine D2 receptor than that of metoclopramide (IC50=17.5-61.0 nM vs. 483 nM) [9].
  • In behavioral studies, haloperidol (a dopamine D2 receptor antagonist) prevents MAP-induced behavioral sensitization, and cocaine (a dopamine reuptake blocker) has the cross-behavioral sensitization with MAP [10].
  • Dopamine D2 receptor binding subunits of the porcine anterior pituitary were visualized by autoradiography following photoaffinity labeling with [125I]N-azidophenethylspiperone and sodium dodecyl-sulfate polyacrylamide gel electrophoresis [11].
  • Introduction of one methyl group on the nitrogen atom at the 4-position and/or modification of the substituent at the 5-position of the 4-amino-5-chloro-2-methoxybenzoyl moiety caused a marked increase in the dopamine D2 receptor binding affinity along with a potent 5-HT3 receptor binding affinity [9].

Analytical, diagnostic and therapeutic context of DRD2


  1. Involvement of vasopressin in the cardiovascular effects of quinpirole. Damase-Michel, C., Montastruc, J.L., Tran, M.A., Gharib, C., Geelen, G., Montastruc, P. Eur. J. Pharmacol. (1990) [Pubmed]
  2. Vagal afferent fibers and peripheral 5-HT3 receptors mediate cisplatin-induced emesis in dogs. Fukui, H., Yamamoto, M., Sato, S. Jpn. J. Pharmacol. (1992) [Pubmed]
  3. Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity. Hirokawa, Y., Fujiwara, I., Suzuki, K., Harada, H., Yoshikawa, T., Yoshida, N., Kato, S. J. Med. Chem. (2003) [Pubmed]
  4. Dopamine receptors labelled by [3H]quinpirole. Seeman, P., Schaus, J.M. Eur. J. Pharmacol. (1991) [Pubmed]
  5. Effects of dopamine D1 and dopamine D2 receptor agonists on coronary and peripheral hemodynamics. Zhao, R.R., Fennell, W.H., Abel, F.L. Eur. J. Pharmacol. (1990) [Pubmed]
  6. A dopamine D2 receptor photolabel: azidoclebopride. Niznik, H.B., Guan, J.H., Neumeyer, J.L., Seeman, P. Eur. J. Pharmacol. (1984) [Pubmed]
  7. Effect of stage of anestrus on the induction of estrus by the dopamine agonist cabergoline in dogs. Verstegen, J.P., Onclin, K., Silva, L.D., Concannon, P.W. Theriogenology (1999) [Pubmed]
  8. Involvement of the transmitter systems of the neostriatum in automation of motor skills in dogs. Shapovalova, K.B. Neurosci. Behav. Physiol. (2006) [Pubmed]
  9. Synthesis and structure-activity relationships of 4-amino-5-chloro-N-(1,4-dialkylhexahydro-1,4-diazepin-6-yl)-2-methoxybenzamide derivatives, novel and potent serotonin 5-HT3 and dopamine D2 receptors dual antagonist. Hirokawa, Y., Harada, H., Yoshikawa, T., Yoshida, N., Kato, S. Chem. Pharm. Bull. (2002) [Pubmed]
  10. Effects of haloperidol and cocaine pretreatments on brain distribution and kinetics of [11C]methamphetamine in methamphetamine sensitized dog: application of PET to drug pharmacokinetic study. Nakamura, H., Hishinuma, T., Tomioka, Y., Ishiwata, S., Ido, T., Iwata, R., Funaki, Y., Itoh, M., Fujiwara, T., Yanai, K., Sato, M., Numachi, Y., Yoshida, S., Mizugaki, M. Nucl. Med. Biol. (1997) [Pubmed]
  11. Deglycosylation and proteolysis of photolabeled D2 dopamine receptors of the porcine anterior pituitary. Jarvie, K.R., Niznik, H.B. J. Biochem. (1989) [Pubmed]
  12. Synthesis and evaluation of high affinity, aryl-substituted [18F]fluoropropylbenzamides for dopamine D-2 receptor studies. Mathis, C.A., Bishop, J.E., Gerdes, J.M., Whitney, J.M., Brennan, K.M., Jagust, W.J. International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology. (1992) [Pubmed]
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