Constitutive activity of the recombinant and native histamine H3 receptor

International Congress Series

Volumn 1249, Issue C, 2003, Pages 139-151

  Arrang, J M ^a   Morisset, S ^a   Rouleau, A ^a   Gbahou, F ^a   Ligneau, X ^b   Tardivel Lacombe, J ^a   Stark, H ^c   Schunack, W ^c   Ganellin, C R ^d   Schwartz, J C ^a  

^a CENTRE PAUL BROCA   (France)

^b Laboratoire Bioprojet   (France)

^c FREIE UNIVERSITÄT BERLIN   (Germany)

^d UNIVERSITY COLLEGE LONDON   (United Kingdom)

Author keywords

Arachidonic acid release; Autoreceptors; Brain; Ciproxifan; H3 receptor; Histamine; Histamine release; In vivo constitutive activity; Native receptors; Neutral antagonist; Proxyfan; 35S GTP S binding

Indexed keywords

EID: 37549048360     PISSN: 05315131     EISSN: None     Source Type: Book Series    
DOI: 10.1016/S0531-5131(03)00617-4     Document Type: Article

References (32)

1. Lefkowitz, R.J., Cotecchia, S., Samama, P., Costa, T., Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol. Sci. 14 (1993), 303-307.
2. Milligan, G., Bond, R., Inverse agonism and the regulation of receptor number. Trends Pharmacol. Sci. 18 (1997), 468-474.
3. Leurs, R., Smit, M.J., Alewijnse, A.E., Timmerman, H., Agonist-independent regulation of constitutively active G-protein-coupled receptors. Trends Biochem. Sci. 23 (1998), 418-422.
4. Chen, G., Way, J., Armour, S., Watson, C., Queen, K., Jayawickreme, C.K., Chen, W.J., Kenakin, T., Use of constitutive G protein-coupled receptor activity for drug discovery. Mol. Pharmacol. 57 (2000), 125-134.
5. Strange, P., Mechanisms of inverse agonism at G-protein-coupled receptors. Trends Pharmacol. Sci. 23 (2002), 89-95.
6. Milligan, G., Bond, R., Lee, M., Inverse agonism: pharmacological curiosity or potential therapeutic strategy?. Trends Pharmacol. Sci. 16 (1995), 10-13.
7. de Ligt, R.A.F., Kourounakis, A.P., Ijzerman, A.P., Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery. Br. J. Pharmacol. 130 (2000), 1-12.
8. 3) of histamine receptor. Nature 302 (1983), 832-837.
9. 3-receptors. Nature 327 (1987), 117-123.
10. 3 heteroreceptors. Fundam. Clin. Pharmacol. 8 (1994), 128-137.
11. Schwartz, J.C., Arrang, J.M., Histamine. Davis, K.L., Charney, D., Coyle, J.T., Nemeroff, C., (eds.) Neuropsychopharmacology: The Fifth Generation of Progress, 2002, Lippincott Williams and Wilkins, Philadelphia, 179-190.
12. 35S]GTP gamma[S] binding to pertussis toxin. Eur. J. Pharmacol. 296 (1996), 223-225.
13. Takeshita, Y., Watanabe, T., Sakata, T., Munakata, M., Ishibashi, H., Akaike, N., Histamine modulates high-voltage-activated calcium channels in neurons dissociated from the rat tuberomammillary nucleus. Neuroscience 87 (1998), 797-805.
14. 3 receptor. Mol. Pharmacol. 55 (1999), 1101-1107.
15. 3 receptor: evidence for two isoforms. NeuroReport 11 (2000), 755-759.
16. 3 receptor: gene organization and multiple isoforms. Biochem. Biophys. Res. Commun. 280 (2001), 75-80.
17. 3 receptor isoforms with different brain expression and signaling properties. Mol. Pharmacol. 59 (2001), 1-8.
18. 3 receptor. Biochem. J. 355 (2001), 279-288.
19. 2-adrenergic receptor. Extending the ternary complex model. J. Biol. Chem. 268 (1993), 4625-4636.
20. 3 receptors regulates histamine neurons in brain. Nature 408 (2000), 860-864.
21. 3 receptors. Br. J. Pharmacol. 135 (2002), 383-392.
22. 3-receptor antagonist. J. Pharmacol. Exp. Ther. 287 (1998), 658-666.
23. 3 antagonists. J. Pharmacol. Exp. Ther. 299 (2001), 908-914.
24. 3-receptor agonist. J. Pharmacol. Exp. Ther. 263 (1992), 304-310.
25. 35S]-GTPΓS binding isotherms. Neuropharmacology 40 (2001), 57-64.
26. Costa, T., Ogino, Y., Munson, P.J., Onaran, 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.
27. 3-receptor ligands on various biochemical indices of histaminergic neuron activity in rat brain. Eur. J. Pharmacol. 164 (1989), 1-11.
28. 3 receptor ligands in a new mouse dipsogenia model. Pharmacol. Biochem. Behav. 72 (2002), 741-750.
29. Lin, J.S., Brain structures and mechanisms involved in the control of cortical activation and wakefulness, with emphasis on the posterior hypothalamus and histaminergic neurons. Sleep Med. Rev. 4 (2000), 471-503.
30. 3 receptor, 1998, Elsevier, Amsterdam, 269-286.
31. 2A receptor blockade. J. Pharmacol. Exp. Ther. 288 (1999), 590-596.
32. Bacciotini, L., Passani, M.B., Mannaioni, P.F., Blandina, P., Interactions between histaminergic and cholinergic systems in learning and memory. Behav. Brain Res. 124 (2001), 183-194.