High impact information on DRD2

• The order of potency of D-2 agonists (N-propylnorapomorphine greater than NO434 greater than apomorphine greater than dopamine) and antagonists (spiroperidol greater than (+)-butaclamol greater than domperidone) with the purified preparation was found to be similar to that of the solubilized dopamine D-2 receptor [1].
• However, dopamine D2 receptor potentiation of BK current in these same cells was affected by PTX, GDP beta S, and GTP gamma S in predictable fashion [2].
• These results suggest that the BAMCC BK channel is not coupled to the mu receptor via a GTP-dependent mechanism, whereas in the same cells the dopamine D2 receptor modulates BK channel activity in a conventional GTP-dependent manner [2].
• Dopamine receptors in CVs were characterized by a dopamine D1 receptor antagonist, [3H]SCH 23390, and a dopamine D2 receptor antagonist, [3H]-spiroperidol [3].
• Adenylate cyclase activity, which was stimulated by SKF 38393 and inhibited by dopamine D2 receptor agonists, was present in the CVs [3].

Biological context of DRD2

• In order to ascertain the identity of this protein, polyclonal antibodies against the dopamine D2 receptor have been raised using synthetic peptides based on the predicted amino acid sequence of the cloned D2 receptor [4].
• These in vitro characteristics of (-)-3-PPP recognition of dopamine D2 receptor binding sites, when compared with dopamine and spiperone are seen to have clear features of both typical agonist and antagonist interactions with D2 receptors in both brain and pituitary [5].
• Dopamine receptor D2 maps to bovine chromosome 15 [6].
• Effect of 7-(3-[4-(2,3-dimethylphenyl)piperazinyl]propoxy)- 2(1H)-quinolinone (OPC-4392), a newly synthesized agonist for presynaptic dopamine D2 receptor, on tyrosine hydroxylation in rat striatal slices [7].

Anatomical context of DRD2

• Interaction of L-prolyl-L-leucyl glycinamide with dopamine D2 receptor: evidence for modulation of agonist affinity states in bovine striatal membranes [8].
• Solubilisation of the dopamine D2 receptor from a membrane preparation of bovine corpus striatum using cholate and NaCl was independently optimised with regard to cholate (0.2%, wt/vol), NaCl (1.5 M), and membrane protein (4 mg/ml) concentrations [9].
• Dopamine D2 receptor binding in adrenal medulla: characterization using [3H]spiperone [10].

Associations of DRD2 with chemical compounds

• These and other data indicate that the most abundant site is a dopamine D2 receptor while the less abundant site may be a serotonin receptor [11].
• Affinity chromatography with the immobilized agonist N-0434 yields an active and highly purified preparation of the dopamine D-2 receptor from bovine striatum [12].
• Synthesis and in vitro affinity for dopamine D-2 receptor of N-fluorine-substituted analogs of eticlopride [13].
• The inhibitory effect of OPC-4392 on in situ DOPA formation was dose-dependently reversed by addition of sulpiride, a dopamine D2 receptor antagonist, whereas no change was observed by addition of nomifensine (5 X 10(-6) M), a blocker of dopamine uptake [7].
• Dopamine D2 receptor was eluted from the affinity resin using a competing dopaminergic antagonist molecule, haloperidol [14].

Regulatory relationships of DRD2

• The fluorescence also increased when cells incubated in the presence of quinpirole, a dopamine D2-receptor agonist which inhibits prolactin secretion, were exposed to raclopride, a D-2 antagonist [15].

Other interactions of DRD2

• Beta-analogs of PLG (L-prolyl-L-leucyl-glycinamide): ex-chiral pool syntheses and dopamine D2 receptor modulating effects [16].

Analytical, diagnostic and therapeutic context of DRD2

• Purification of bovine striatal dopamine D-2 receptor by affinity chromatography [1].

References