Assessment of α2-adrenoceptor antagonist potency with GTPase assay

European Journal of Pharmacology

Volumn 338, Issue 3, 1997, Pages 293-296

  Virolainen, Sami ^a   Jansson, Christian C ^a   Scheinin, Mika ^a  

^a UNIVERSITY OF TURKU   (Finland)

Author keywords

Antagonist potency; CHO cell; GTPase; 2 Adrenoceptor subtype

Indexed keywords

2 (2 METHOXY 1,4 BENZODIOXAN 2 YL) 2 IMIDAZOLINE; ALPHA 2 ADRENERGIC RECEPTOR; CHLORPROMAZINE; GUANOSINE TRIPHOSPHATASE; PHENTOLAMINE; PRAZOSIN; RAUWOLSCINE; RECEPTOR SUBTYPE; ALPHA ADRENERGIC RECEPTOR BLOCKING AGENT;

ANIMAL CELL; ARTICLE; CELL MEMBRANE; CHO CELL; CONTROLLED STUDY; DOSE RESPONSE; DRUG RECEPTOR BINDING; DRUG SPECIFICITY; ENZYME ACTIVITY; GENE EXPRESSION; HUMAN; IN VITRO STUDY; NONHUMAN; PRIORITY JOURNAL; TECHNIQUE; ANIMAL; DRUG ANTAGONISM; HAMSTER; METABOLISM;

ADRENERGIC ALPHA-ANTAGONISTS; ANIMALS; CHLORPROMAZINE; CHO CELLS; CRICETINAE; GTP PHOSPHOHYDROLASES; PHENTOLAMINE; PRAZOSIN; RECEPTORS, ADRENERGIC, ALPHA-2;

EID: 0030608648     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(97)81933-4     Document Type: Article

References (25)

1. Aktories K., Jakobs K.H. Epinephrine inhibits adenylate cyclase and stimulates a GTPase in human platelet membranes via α-adrenoceptors. FEBS Lett. 130:1981;235-238.
2. Arunlakshana O., Schild H.O. Some quantitative uses of drug antagonists. Br. J. Pharmacol. 14:1959;48-58.
3. Bradford M.M. A rapid and sensitive method for quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem. 72:1976;248-254.
4. Brandt D.R., Ross E.M. Catecholamine-stimulated GTPase cycle. J. Biol. Chem. 261:1986;1656-1664.
5. 2A-adrenergic receptor to multiple G-proteins. J. Biol. Chem. 269:1994;5730-5734.
6. qα: Mutational activation and coupling to receptors and phospholipase C. J. Biol. Chem. 267:1992;31-34.
7. Costa T., Herz A. Antagonists with negative intrinsic activity at δ opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. USA. 86:1989;7321-7325.
8. Costa T., Lang J., Gless C., Herz A. Spontaneous association between opioid receptors and GTP-binding regulatory proteins in native membranes: Specific regulation by antagonists and sodium ions. Mol. Pharmacol. 37:1990;383-394.
9. Costa T., Ogino Y., Munson P.J., Onaran H.O., Rodbard D. 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. 41:1992;549-560.
10. 2-adrenergic receptors to two G-proteins with opposing effects. J. Biol. Chem. 267:1992;15795-15801.
11. Hasegawa H., Negishi M., Ichikawa A. Two isoforms of the prostaglandin E receptor EP3 subtype different in agonist-independent constitutive activity. J. Biol. Chem. 271:1996;1857-1860.
12. 2-adrenergic receptor. Science. 238:1987;650-656.
13. Koski G., Klee W.A. Opiates inhibit adenylate cyclase by stimulating GTP hydrolysis. Proc. Natl. Acad. Sci. USA. 78:1981;4185-4189.
14. 2 adrenergic receptor subtypes and G proteins in reconstituted phospholipid vesicles. Biochemistry. 30:1991;3335-3341.
15. Lazareno S., Farries T., Birdsall N.J.M. Pharmacological characterization of guanine nucleotide exchange reactions in membranes from CHO cells stably transfected with human muscarinic receptors M1-M4. Life Sci. 52:1993;449-456.
16. Limbird L.E. Receptors linked to inhibition of adenylate cyclase: Additional signaling mechanisms. FASEB J. 2:1988;2686-2695.
17. Lomasney J.W., Cotecchia S., Lefkowitz R.J., Caron M.G. Molecular biology of α-adrenergic receptors: Implications for receptor classification and for structure-function relationships. Biochim. Biophys. Acta. 1095:1991;127-139.
18. 2-adrenoceptors to characterize subtype selectivity of antagonist binding. Eur. J. Pharmacol. 246:1993;219-226.
19. 2-Adrenoceptor regulation of adenylyl cyclase in CHO cells: Dependence on receptor density, receptor subtype and present activity of adenylyl cyclase. Eur. J. Pharmacol., in press.
20. Raymond J.R. Multiple mechanisms of receptor-G-protein signaling specificity. Am. Physiol. 269:1995;F141-F158.
21. 2-adrenergic receptor subtype. Proc. Natl. Acad. Sci. USA. 85:1988;6301-6305.
22. q family. J. Biol. Chem. 266:1991;9309-9313.
23. Seiler S.M., Peluso M., Tuttle J.G., Pryor K., Klimas C., Matsueda G.R., Bernatowicz M.S. Thrombin receptor activation by thrombin and receptor-derived peptides in platelet and CHRF-288 cell membranes: Receptor-stimulated GTPase and evaluation of agonists and partial agonists. Mol. Pharmacol. 49:1996;190-197.
24. m GTPase to guanine nucleotide analogs. J. Neurochem. 47:1986;1361-1369.
25. z-mediated hormonal inhibition of cyclic AMP accumulation. Science. 255:1992;339-342.