A potent and selective CGRP2 agonist, [Cys(Et)2,7]hCGRPα: Comparison in prototypical CGRP1 and CGRP2 in vitro bioassays

Canadian Journal of Physiology and Pharmacology

Volumn 75, Issue 6, 1997, Pages 671-676

  Dumont, Yvan ^a   Fournier, Alain ^b   St Pierre, Serge ^b   Quirion, Rémi ^a  

^a MCGILL UNIVERSITY   (Canada)

^b INSTITUT NATIONAL DE LA RECHERCHE SCIENTIFIQUE   (Canada)

Author keywords

Calcitonin gene related peptide; CGRP1 and CGRP2 bioassay; Selectivity analogue

Indexed keywords

CALCITONIN GENE RELATED PEPTIDE DERIVATIVE; CALCITONIN GENE RELATED PEPTIDE RECEPTOR; RECEPTOR SUBTYPE; CALCITONIN GENE RELATED PEPTIDE; DRUG DERIVATIVE;

ANIMAL TISSUE; BIOASSAY; BRAIN HOMOGENATE; CONFERENCE PAPER; CONTROLLED STUDY; DRUG RECEPTOR BINDING; GUINEA PIG; HEART ATRIUM MUSCLE; IN VITRO STUDY; INOTROPISM; MALE; MUSCLE TWITCH; NONHUMAN; PRIORITY JOURNAL; RAT; STRUCTURE ACTIVITY RELATION; VAS DEFERENS; ANIMAL; ARTICLE; CLASSIFICATION; DRUG EFFECT; DRUG POTENTIATION; HEART; HEART ATRIUM; HEART MUSCLE; KINETICS; METABOLISM; SPRAGUE DAWLEY RAT;

ANIMALS; CALCITONIN GENE-RELATED PEPTIDE; GUINEA PIGS; HEART; HEART ATRIA; KINETICS; MALE; MYOCARDIUM; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, CALCITONIN GENE-RELATED PEPTIDE; STRUCTURE-ACTIVITY RELATIONSHIP; VAS DEFERENS;

EID: 0030610615     PISSN: 00084212     EISSN: None     Source Type: Journal    
DOI: 10.1139/cjpp-75-6-671     Document Type: Conference Paper

References (25)

1. Aiyar, NJ., Rand, K., Elshourbagy, N.A., Zeng, Z., Adamou, J.E., Bergsma, D.J., and Li, Y. 1996. A cDNA encoding the calcitonin gene-related peptide type 1 receptor. J. Biol. Chem. 271: 11 325-11 329.
2. Amara, S.G., Jonas, V., Rosenfeld, M.G., Ong, E.S., and Evans, R.M. 1982. Alternative RNA processing in calcitonin gene expression generates mRNAs encoding different polypeptide products. Nature (London), 296: 240-244.
3. Brain, S.D., William, T.J., Tippins, J.R., Morris, H.R., and MacIntyre, I. 1985. Calcitonin gene-related peptide is a potent vasodilatator. Nature (London), 313: 54-56.
4. Chiba, T., Yamaguchi, A., Yamatani, T., Nakamura, A., Morishita, T., Inui, T., Fukase, M., Noda, T., and Fujita, T. 1989. Calcitonin gene-related peptide receptor antagonist human CGRP-(8-37). Am. J. Physiol. 256: E331-E335.
5. Dennis, T., Fournier, A., St-Pierre, S., and Quirion, R. 1989. Structure-activity profile of calcitonin gene-related peptide in peripheral and brain tissues. Evidence of receptor multiplicity. J. Pharmacol. Exp. Ther. 251: 718-725.
6. 8-37, a calcitonin gene-related peptide antagonist revealing CGRP receptor heterogeneity in brain and periphery. J. Pharmacol. Exp. Ther. 254: 123-128.
7. Dennis, T., Fournier, A., Guard, S., St-Pierre, S., and Quirion, R. 1991. Calcitonin gene-related peptide (hCGRPα) binding sites in nucleus accumbens. Atypical structural requirements and marked phylogenic differences. Brain Res. 539: 59-66.
8. Jolicoeur, F.B., Menard, D., Fournier, A., and St-Pierre, S. 1992. Structure-activity of CGRP's neurobehavioral effects. Ann. N.Y. Acad. Sci. 657: 155-163.
9. Kapas, S., and Clark, A.J.L. 1995. Identification a an orphan receptor gene as type 1 calcitonin gene-related peptide receptor. Biochem. Biophys. Res. Commun. 217: 832-838.
10. Krahn, D.D., Gosnell, B.A., Levine, A.S., and Morley, J.E. 1984. Effects of calcitonin gene-related peptide on food intake. Peptides (Elmsford), 5: 861-864.
11. Luebke, A.E., Dahl, G.P., Ross, B.A., and Dickerson, I.M. 1996. Identification a a protein that confers calcitonin gene-related peptide responsiveness to oocytes by using a cystic fibrosis transmembrane conductance regulator assay. Proc. Natl. Acad. Sci. U.S.A. 93: 3455-3460.
12. Lundberg, J.M., Franco-Cereceda, A., Hua, X.Y., Hokfelt, T., and Fisher, J.A. 1985. Co-existence of substance P and calcitonin gene-related peptide immunoreactivities in relation to cardiovascular effects of capsaicin. Eur. J. Pharmacol. 108: 315-319.
13. Lynch, B., and Kaiser, E.T. 1988. Biological properties of two models of calcitonin gene-related peptide with idealized amphiphilic a helices of different lengths. Biochemistry, 27: 7600-7607.
14. Miles, K., Greengard, P., and Huganir, R.L. 1989. Calcitonin gene-related peptide regulates phosphorylation of the nicotinic acetylcholine receptor in rat myotubes. Neuron, 2: 1517-1524.
15. Mimcault, M., Fournier, A., Dumont, Y., St-Pierre, S., and Quirion, R. 1991. Comparative affinities and antagonistic potencies of various human calcitonin gene-related peptide fragments on calcitonin gene-related peptide receptors in brain and periphery. J. Pharmacol. Exp. Ther. 258: 1084-1090.
16. Poyner, D. 1995. Pharmacology of receptors for calcitonin gene-related peptide and amylin. Trends Pharmacol. Sci. 16: 424-428.
17. 2 receptor subtypes. Ann. N.Y. Acad. Sci. 657: 88-105.
18. Rosenfeld, M.G., Mermod, J.J., Amara, S.G., Swanson, L.W., Sawchenko, P.E., Rivier, J., Vale, W.W., and Evans, R.M. 1983. Production of a novel neuropeptide encoded by the calcitonin gene via tissue-specific RNA processing. Nature (London), 304: 129-135.
19. Sexton, P.M., McKenzie, J.S., Mason, R.T., Moseley, J.M., Martin, T.J., and Mendelsohn, F.A.O. 1988. Localization of binding sites for calcitonin gene-related peptide in rat brain by in vitro autoradiography. Neuroscience, 19: 1235-1245.
20. Skofitsch, G., and Jacobowitz, D.M. 1985. Calcitonin gene-related peptide: detailed immunohistochemical distribution in the central nervous system. Peptides (Elmsford), 6: 721-745.
21. Taché, Y. 1992. Inhibition of gastric acid secretion and ulcers by calcitonin gene-related peptide. Ann. N.Y. Acad. Sci. 657: 240-247.
22. Tippins, J.R., diMarzo, V.M., Panico, M., Morris, H.R., and MacIntyre, I. 1986. Investigation of the structure-activity relationship of human calcitonin gene-related peptide (CGRP). Biochem. Biophys. Res. Commun. 134: 1306-1311.
23. van Rossum, D., and Quirion, R. 1997. Neuroanatomical localization, pharmacological characterization and functions of CGRP and related peptide receptors. Neurosci. Biobehav. Rev. In press.
24. 8-37, in rat brain and peripheral tissues. J. Pharmacol. Exp. Ther. 269: 846-853.
25. 125I]Bolton Hunter-rat amylin binding sites in the rat brain. J. Pharmacol. Exp. Ther. 270: 779-787.