Mechanisms of inverse agonism of antipsychotic drugs at the D2 dopamine receptor: Use of a mutant D2 dopamine receptor that adopts the activated conformation

Journal of Neurochemistry

Volumn 77, Issue 2, 2001, Pages 493-504

  Wilson, Janet ^a   Lin, Hong ^a   Fu, Dingyi ^b,c   Javitch, Jonathan A ^b   Strange, Philip G ^a  

^a UNIVERSITY OF READING   (United Kingdom)

^b Columbia University College of Physicians and Surgeons ^*  (United States)

^c WEILL CORNELL MEDICAL COLLEGE   (United States)

Author keywords

Activated state; Antipsychotic drugs; D2 dopamine receptor; Inverse agonists; Mechanisms; Mutants

Indexed keywords

2 DIPROPYLAMINO 5 METHOXY 1 METHYLTETRALIN; ADENYLATE CYCLASE; AMINOTETRALIN; BROMOCRIPTINE; BUTACLAMOL; CLOZAPINE; DOPAMINE 2 RECEPTOR; FORSKOLIN; GUANINE NUCLEOTIDE BINDING PROTEIN; HALOPERIDOL; META TYRAMINE; NEUROLEPTIC AGENT; PRECLAMOL; SODIUM ION; SULPIRIDE; TYRAMINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG ACTIVITY; DRUG CONFORMATION; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENTIATION; ENZYME INHIBITION; HUMAN; HUMAN CELL; ISOMERISM; MUTAGENIC ACTIVITY; NONHUMAN; PRIORITY JOURNAL; RECEPTOR BINDING; RECEPTOR UPREGULATION;

1-METHYL-3-ISOBUTYLXANTHINE; 8-HYDROXY-2-(DI-N-PROPYLAMINO)TETRALIN; ANIMALS; ANTIPSYCHOTIC AGENTS; APOMORPHINE; BINDING, COMPETITIVE; BROMOCRIPTINE; BUTACLAMOL; CHLORPROMAZINE; CHO CELLS; CLOZAPINE; CRICETINAE; CRICETULUS; CYCLIC AMP; DOPAMINE AGONISTS; DOPAMINE ANTAGONISTS; DOSE-RESPONSE RELATIONSHIP, DRUG; FORSKOLIN; GTP-BINDING PROTEINS; HALOPERIDOL; HUMANS; MACROMOLECULAR SUBSTANCES; MUTAGENESIS, SITE-DIRECTED; PHENETHYLAMINES; PIPERIDINES; PROTEIN BINDING; PROTEIN CONFORMATION; RADIOLIGAND ASSAY; RECEPTORS, DOPAMINE D2; RECOMBINANT FUSION PROTEINS; SODIUM; SPIPERONE; STRUCTURE-ACTIVITY RELATIONSHIP; SULPIRIDE; TRANSFECTION; TYRAMINE;

ANIMALIA;

EID: 0035051547     PISSN: 00223042     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1471-4159.2001.00233.x     Document Type: Article

References (39)

1. A selective inverse agonist for central cannabinoid receptor inhibits mitogen-activated protein kinase activation stimulated by insulin or insulin like growth factor receptor 1. Evidence for a new model of receptor/ligand interactions
2. Gi protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: Implication for intracellular signalisation cross-regulation
3. Differences in the ligand binding properties of the long and short versions of the D2 dopamine receptor
4. 50) of an enzymatic reaction
5. Drug effects at guanine nucleotide regulatory binding protein linked receptors: Thermodyamic interpretation of negative antagonism of receptor activation in the absence of ligand
6. Regions of the α1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function
7. 2(long) dopamine receptors: Ligand binding and functional assays
8. 2(short) dopamine receptors determined in ligand binding and functional assays
9. Evidence that antipsychotic drugs are inverse agonists at D2 dopamine receptors
10. 1 dopamine receptor
11. Effects of the D-3 and autoreceptor preferring dopamine antagonist (+)UH 232 in schizophrenia
12. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
13. 1A receptor by protein kinase C
14. Protein measurement with the folin phenol reagent
15. Mechanisms of agonism and inverse agonism at serotonin 5HT1A receptors
16. 3H]quinpirole binding to human D2A and D3 receptors: Effects of ions and guanine nucleotides
17. s in a ligand dependent manner
18. Unique binding characteristics of antipsychotic agents interacting with the human D2A, D2B and D3 dopamine receptors
19. Increase in dopamine D2 receptor and G protein levels following sodium butyrate treatment of a recombinant CHO cell line
20. Inverse agonism and the regulation of receptor number
21. 2 dopamine receptors by sodium and pH
22. Molecular biology of the dopamine receptors
23. Haloperidol increases prolactin release and cAMP formation in vitro - Inverse agonism at dopamine D2 receptors
24. Investigation of mechanisms of agonist action at the human Ds short dopamine receptor
25. Bicistronic vector for the creation of stable mammalian cell lines that predisposes all antibiotic resistant cells to express recombinant receptor
26. Constitutively active mutants of the alpha 2-adrenergic receptor
27. 1b adrenergic receptor subtypes
28. A highly sensitive adenylate cyclase assay
29. A mutation-induced activated state of the beta-adrenergic receptor. Extending the ternary complex model
30. 2a-adrenergic receptor
31. Reverse intrinsic activity of antagonists on G protein coupled receptors
32. Constitutive activation of the m5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6
33. Commentary on atypical neuroleptics
34. Two state and three state models
35. 2 adrenergic receptor activation of G protein: Evidence for a precoupled receptor/G protein state
36. Porcine M2 muscarinic acetylcholine receptor effector coupling in CHO cells
37. 2 dopamine receptors by magnesium and sodium ions
38. Contribution of serine residues to constitutive and agonist induced signalling via the D2s dopamine receptor: Evidence for multiple agonist specific conformations