Biological activities of N6, C8-disubstituted adenosine derivates as partial agonists a rat brain adenosine A1 receptors

European Journal of Pharmacology

Volumn 334, Issue 2-3, 1997, Pages 299-307

  Lorenzen, Anna ^a   Sebastião, Ana M ^b   Sellink, Andrea ^c   Vogt, Heidrun ^a   Schwabe, Ulrich ^a   Ribeiro, J Alexandre ^b   Ijzerman, Adriaan P ^c  

^a UNIVERSITY OF HEIDELBERG   (Germany)

^b INSTITUTO GULBENKIAN DE CIÊNCIA   (Portugal)

^c LEIDEN UNIVERSITY   (Netherlands)

Author keywords

Adenosine A1 receptor; Agonism; Excitatory postsynaptic potential; G protein; Hippocampus; Intrinsic activity; Partial

Indexed keywords

6 N CYCLOPENTYLADENOSINE; ADENOSINE A1 RECEPTOR; ADENOSINE DERIVATIVE; ADENOSINE RECEPTOR STIMULATING AGENT; ADENYLATE CYCLASE; ADENOSINE; ADENOSINE RECEPTOR; DRUG DERIVATIVE; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); N(6) CYCLOPENTYLADENOSINE; N(6)-CYCLOPENTYLADENOSINE;

ANIMAL TISSUE; ARTICLE; BRAIN SLICE; CONTROLLED STUDY; ENZYME ACTIVITY; EXCITATORY POSTSYNAPTIC POTENTIAL; HEART RATE; HIPPOCAMPUS; IN VITRO STUDY; MALE; MEAN ARTERIAL PRESSURE; NONHUMAN; PRIORITY JOURNAL; RAT; SYNAPTIC TRANSMISSION; ANIMAL; CHEMISTRY; COMPARATIVE STUDY; DRUG EFFECT; DRUG POTENTIATION; ENZYMOLOGY; FOREBRAIN; MEMBRANE; METABOLISM; PHYSIOLOGY; STRUCTURE ACTIVITY RELATION; WISTAR RAT;

ADENOSINE; ADENYLATE CYCLASE; ANIMALS; EXCITATORY POSTSYNAPTIC POTENTIALS; GTP-BINDING PROTEINS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HIPPOCAMPUS; MALE; MEMBRANES; PROSENCEPHALON; RATS; RATS, WISTAR; RECEPTORS, PURINERGIC P1; STRUCTURE-ACTIVITY RELATIONSHIP; SYNAPTIC TRANSMISSION;

EID: 0030609091     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(97)01193-X     Document Type: Article

References (28)

1. 2-adrenoceptor. Nature 374, 272-276.
2. 2A receptors in the rat hippocampus. Brain Res. 649, 208-216.
3. Cunha, R.A., Correia-de-Sá, P., Sebastião, A.M., Ribeiro, J.A., 1996. Preferential activation of excitatory adenosine receptors at rat hippocampal and neuromuscular synapses by adenosine formed from released adenine nucleotides. Br. J. Pharmacol. 119, 253-260.
4. Dunwiddie, T.V., Fredholm, B.B., 1985. Adenosine modulation of synaptic responses in rat hippocampus: Possible role of inhibition or activation of adenylate cyclase. Adv. Cyclic Nucleotide Protein Phosphorylation Res. 19, 259-272.
5. s Mol. Pharmacol. 45, 696-702.
6. 1-adenosine receptor with recombinant G protein a-subunits. J. Biol. Chem. 266, 17778-17783.
7. 1A receptor. Biochemistry 33, 4283-4290.
8. Hoyer, D., Boddeke, H.W.G.M., 1993. Partial agonists, full agonists, antagonists: Dilemmas of definition. Trends Pharmacol. Sci. 14, 270-275.
9. Jasper, J.R., Insel, P.A., 1992. Evolving concepts of partial agonism. The β-adrenergic receptor as a paradigm. Biochem. Pharmacol. 43, 119-130.
10. Kenakin, T., 1995. Agonist-receptor efficacy II: Agonist trafficking of receptor signals. Trends Pharmacol. Sci. 16, 232-238.
11. 1 adenosine receptors. J. Neurochem. 45, 1761-1770.
12. 6-cyclohexyladenosine: An adenosine derivative with antagonist properties at adenosine receptors. Eur. J. Pharmacol. 156, 157-160.
13. 35S]thio)triphosphate binding. Mol. Pharmacol. 44, 115-123.
14. 1 adenosine receptor with receptor/G protein complexes in rat brain membranes. Mol. Pharmacol. 49, 915-926.
15. 2-adrenoceptor. Mol. Pharmacol. 48, 316-325.
16. 1 receptor. Br. J. Pharmacol. 116, 1957-1964.
17. o. J. Biol. Chem. 266, 22285-22289.
18. Perez, D.M., Hwa, J., Gaivin, R., Mathur, M., Brown, F., Graham, R.M., 1996. Constitutive activation of a single effector pathway: Evidence for multiple activation states of a G protein-coupled receptor. Mol. Pharmacol. 49, 112-122.
19. Peterson, G.L., 1977. A simplification of the protein assay method of Lowry et al. which is more generally applicable. Anal. Biochem. 83, 346-356.
20. 6,C8-Disubstituted adenosine derivatives as partial agonists for adenosine A1 receptors. J. Med. Chem. 39, 1463-1471.
21. 2-adrenergic receptor. J. Biol. Chem. 268, 4625-4636.
22. Sebastião, A.M., Stone, T.W., Ribeiro, J.A., 1990. On the inhibitory adenosine receptor at the neuromuscular junction and hippocampus of the rat: Antagonism by 1,3,8-substituted xanthines. Br. J. Pharmacol. 101, 453-459.
23. 2+ channel agonists Bay K 8644 produce a synergistic stimulation of the GTPase activity in rat frontal cortical membranes. J. Neurochem. 64, 2034-2042.
24. Taylor, M.D., Moos, W.H., Hamilton, H.W., Szotek, D.S., Patt, W.C., Badger, E.W., Bristol, J.A., Bruns, R.F., Heffner, T.G., Mertz, T.E., 1986. Ribose-modified adenosine analogues as adenosine receptor agonists. J. Med. Chem. 29, 346-353.
25. 35S]thio)triphosphate binding to membranes from human neuroblastoma SH-SY5Y cells. Mol. Pharmacol. 47, 848-854.
26. Van der Wenden, E.M., Von Frijtag Drabbe Künzel, J.K., Mathôt, R.A.A., Danhof, M., IJzerman, A.P., Soudijn, W., 1995a. Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor. J. Med. Chem. 38, 4000-4006.
27. 1 receptor. Eur. J. Pharmacol. (Mol. Pharmacol. Section) 290, 189-199.
28. Whaley, B.S., Yuan, N., Birnbaumer, L., Clark, R.B., Barber, R., 1994. Differential expression of the β-adrenergic receptor modifies agonist stimulation of adenylyl cyclase: A quantitative evaluation. Mol. Pharmacol. 45, 481-489.