Inverse agonism at dopamine D2 receptors: Haloperidol-induced prolactin release from GH4C1 cells transfected with the human D2 receptor is antagonized by R(-)-n-propylnorapomorphine, raclopride, and phenoxybenzamine

Neuropsychopharmacology

Volumn 15, Issue 1, 1996, Pages 53-61

  Nilsson, Christer L ^a   Ekman, Agneta ^b   Hellstrand, Monika ^b   Eriksson, Elias ^b  

^a UNIVERSITY OF GOTHENBURG   (Sweden)

^b NONE

Author keywords

Dopamine D2 receptor; Flupenthixol; GH4C1 cells; Haloperidol; Inverse agonism; Negative antagonism; Phenoxybenzamine; Prolactin; R( ) n Propylnorapomorphine; Raclopride; Reverse agonism

Indexed keywords

DOPAMINE; DOPAMINE RECEPTOR; DOPAMINE RECEPTOR BLOCKING AGENT; FLUPENTIXOL; HALOPERIDOL; NEUROLEPTIC AGENT; PHENOXYBENZAMINE; PROLACTIN; PROPYLNORAPOMORPHINE; RACLOPRIDE;

ARTICLE; CELL CULTURE; HUMAN; HUMAN CELL; PRIORITY JOURNAL;

EID: 0030200664     PISSN: 0893133X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0893-133X(95)00156-8     Document Type: Article

References (39)

1. 2 adrenoceptor: Evidence for empty receptor stimulation of the adenylate cyclase cascade. Biochem J 303:803-808
2. 2 receptor to inhibition of adenylyl cyclase and prolactin secretion. J Biol Chem 265:2098-2104
3. 1 cells. Biochem Biophys Res Comm 193:801-807
4. 2C receptors reveal novel inverse agonist activity of receptor ligands. J Biol Chem 269:11687-11690
5. 1 cells. Mol Cell Endocrinol 37:41-50
6. The British Isles Raclopride Study Group (1992): A double-blind comparison of raclopride and haloperidol in the acute phase of schizophrenia. Acta Psychiatr Scand 86:391-398
7. 1 cells. Proc Soc Exp Biol Med 205:226-235
8. Carlsson A, Waters N, Svensson K, Löfberg L (1991): New trends in the molecular biology and pharmacology of dopaminergic transmission. In Racagni G, Brunello N, Fukuda T (eds), Biological Psychiatry, vol 2, Amsterdam, Elsevier, pp 687-689
9. 2 dopamine receptor. J Neurochem 60:372-375
10. Chidiac P, Hebert TE, Valiquette M, Dennis M, Bouvier M (1994): Inverse agonist activity of β-adrenergic antagonists. Mol Pharmacol 45:490-499
11. Clement-Cormier YC, Heindel JJ, Robison GA (1977): Adenylyl cyclase from a prolactin producing tumor cell: The effects of phenotiazines. Life Sci 21:1357-1364
12. Costa T, Herz A (1989): Antagonists with negative intrinsic activity at δ opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci USA 86:7321-7325
13. Costa T, Ogino Y, Munson PJ, Onaran HO, Rodbard D (1992): Drug efficacy at guanine nucleotide-binding regulatory protein-linked receptors: Thermodynamic interpretation of negative antagonism and of receptor activity in the absence of ligand. Mol Pharmacol 41:549-560
14. De Camilli P, Macconi D, Spada A (1979): Dopamine inhibits adenylate cyclase in human prolactin-secreting pituitary adenomas. Nature 278:252-254
15. 2 dopamine receptors inhibits protein kinase C activity in striatal synaptoneurosomes. J Neurochem 63:169-176
16. 1 cells by chlorpromazine and a heat-stable factor. Endocrinology 108:310-317
17. Hilf G, Jakobs KH (1992): Agonist-independent inhibition of G protein activation by muscarinic acetylcholine receptor antagonists in cardiac membranes. Eur J Pharmacol [Mol Sect] 225:245-252
18. 3 cells. J Mol Endocrinol 7:131-136
19. 2 dopamine receptors via basal and ligand-regulated GTP binding studies. FASEB J 9: abstract 3879
20. 2C receptor expressed in Sf9 cells. Can J Physiol Pharmacol 72(Suppl 1): P18.9.35, 546
21. 2 receptor act as inverse agonists in rat myometrial cells. J Biol Chem 269:25970-25973
22. Lefkowitz RJ, Cotecchia S, Samama P, Costa T (1993): Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci 14:303-307
23. Markwell MAK, Haas SM, Bieber LL, Tolbert NE (1978): A modification of the Lowry procedure to simplify protein determination in membrane and lipoprotein samples. Anal Biochem 87:206-210
24. Mewes T, Dutz S, Ravens U, Jakobs KH (1994): Evidence for G-protein involvement in spontaneous activity of cardiac empty β-adrenoceptors. Naunyn Schmiedeberg's Arch Pharmacol 349(suppl):R10
25. Milligan G, Bond RA, Lee M (1995): Inverse agonism: Pharmacological curiosity or potential therapeutic strategy? Trends Pharmacol Sci 16:10-13
26. i protein subtypes. J Biol Chem 266: 23392-23398
27. Munson PJ, Rodbard D (1980): LIGAND: A versatile computerized approach for characterization of ligand-binding systems. Anal Biochem 107:220-239
28. 2 receptors? J Neural Transm [Gen Sect] 92:213-220
29. Nilsson CL, Eriksson E (1995): Effects of remoxipride and raclopride on prolactin release from clonal pituitary tumour cells. Pharmacol Toxicol 76:85-88
30. Onaran HO, Costa T, Rodbard D (1993): βγ-Subunits of guanine nucleotide-binding proteins and regulation of spontaneous receptor activity: Thermodynamic model for the interaction between receptors and guanine nucleotide-binding protein subunits. Mol Pharmacol 43:245-256
31. 2s dopamine receptor in protease-deficient Saccharomyces cerevisiae strains. Eur J Biochem 226:697-705
32. Schütz W, Freissmuth M (1992): Reverse intrinsic activity of antagonists on G protein-coupled receptors. Trends Pharmacol Sci 13:376-380
33. 2 receptors on primary cultured rat lactotrophs. Neuroendocrinology 56:397-406
34. o-linked receptors and its allosteric regulation by monovalent cations. Life Sci 52:1899-1907
35. 1B receptor subtype. J Biol Chem 269:27925-27931
36. Vogel WK, Mosser VA, Bulseco DA, Schimerlik MI (1995): Porcine m2 muscarinic acetylcholine receptor-effector coupling in Chinese hamster ovary cells. J Biol Chem 270:15485-15493
37. Westphal RS, Sanders-Bush E (1994): Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists. Mol Pharmacol 46:937-942
38. 2-dopamine receptor of the anterior pituitary gland. Mol Pharmacol 26:214-227
39. 3 cells. Proc Soc Exp Biol Med 202:193-200