A study of antagonist affinities for the human histamine H2 receptor

British Journal of Pharmacology

Volumn 153, Issue 5, 2008, Pages 1011-1021

  Baker, J G ^a  

^a UNIVERSITY OF NOTTINGHAM   (United Kingdom)

Author keywords

Affinity; Antagonist; cAMP; GPCR; Histamine; Reporter gene

Indexed keywords

2 (2 PYRIDYL)ETHYLAMINE; 4 METHYLHISTAMINE; 5 [3 [N' (2,2,2 TRIFLUOROETHYL)GUANIDINO] 1 PYRAZOLYL]VALERAMIDE; ALPHA METHYLHISTAMINE; AMTHAMINE; CIMETIDINE; DIMAPRIT; FAMOTIDINE; G PROTEIN COUPLED RECEPTOR; HISTAMINE; HISTAMINE H2 RECEPTOR; HISTAMINE H2 RECEPTOR AGONIST; HISTAMINE H2 RECEPTOR ANTAGONIST; HISTAMINE TRIFLUOROMETHYL TOLUIDIDE; IMETIT; IMMEPIP; IMPENTAMINE; N METHYLHISTAMINE; NIZATIDINE; PROXYFAN; RANITIDINE; TIOTIDINE; UNCLASSIFIED DRUG; ZOLATIDINE;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG EFFICACY; DRUG MECHANISM; GENETIC TRANSCRIPTION; HUMAN; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION;

EID: 40149104826     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0707644     Document Type: Article

References (39)

1. Arunlakshana O, Schild HO (1959). Some quantitative uses of drug antagonists. Br J Pharmacol 14: 48–58.
2. Ash ASF, Schild HO (1966). Receptors mediating some actions of histamine. Br J Pharmacol Chemother 27: 427–439.
3. Baker JG (2005a). Sites of action of β‐ligands at the human β1‐adrenoceptor. J Pharmacol Exp Ther 313: 1163–1171.
4. Baker JG (2005b). Evidence for a secondary state of the human β3‐adrenoceptor. Mol Pharmacol 68: 1645–1655.
5. Baker JG, Hall IP, Hill SJ (2003a). Agonist actions of ‘β‐blockers’ provide evidence for two agonist activation sites or conformations of the human β1‐adrenoceptor. Mol Pharmacol 63: 1312–1321.
6. Baker JG, Hall IP, Hill SJ (2003b). Influence of agonist efficacy and receptor phosphorylation on antagonist affinity measurements: differences between second messenger and reporter gene responses. Mol Pharmacol 64: 679–688.
7. Baker JG, Hall IP, Hill SJ (2003c). Agonist and inverse agonist actions of ‘β‐blockers’ at the human β 2 ‐adrenoceptor provide evidence for agonist‐directed signalling. Mol Pharmacol 64: 1357–1369.
8. Baker JG, Hall IP, Hill SJ (2004). Temporal characteristics of CRE‐mediated gene transcription: requirement for sustained cAMP production. Mol Pharmacol 65: 986–998.
9. Baker JG, Hill SJ (2007). A comparison of the antagonist affinities for the Gi and Gs‐coupled states of the human adenosine A1 receptor. J Pharmacol Exp Ther 320: 218–228.
10. Black JW, Duncan WA, Durant CJ, Ganellin CR, Parsons ME (1972). Definition and antagonism of histamine H2‐receptors. Nature 236: 385–390.
11. Black JW, Duncan WAM, Shanks RG (1965). Comparison of some properties of pronethalol and propranolol. Br J Pharmacol 25: 577–591.
12. Clark RB, Knoll BJ, Barber R (1999). Partial agonists and G‐protein coupled receptor desensitization. Trends Pharmacol Sci 20: 279–286.
13. Donaldson J, Brown AM, Hill SJ (1988). Influence of rolipram on the cyclic‐3′,5′‐adenosine monophosphate response to histamine and adenosine in slices of guinea‐pig cerebral cortex. Biochem Pharmacol 37: 715–723.
14. Granneman JG (2001). The putative beta4‐adrenergic receptor is a novel state of the beta1‐adrenergic receptor. Am J Physiol Endocrinol Metab 280: E199–E202.
15. Hill SJ (1990). Distribution, properties and functional responses of the three classes of histamine receptors. Pharmacol Rev 42: 45–83.
16. Hill SJ (2006). G protein‐coupled receptors: past, present and future. Br J Pharmacol 147: S27–S37.
17. Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM et al. (1997). International Union of Pharmacology. XIII. Classification of histamine receptors. Pharmacol Rev 49: 253–278.
18. Hopkinson HE, Latif ML, Hill SJ (2000). Non‐competitive antagonism of β 2 ‐agonist‐mediated cyclic AMP accumulation by ICI 118551 in BC3H1 cells endogenously expressing constitutively active β 2 ‐adrenoceptors. Br J Pharmacol 131: 124–130.
19. January B, Seibold A, Allal C, Whaley B, Knoll BJ, Moore RH et al. (1998). Salmeterol‐induced desensitization, internalization and phosphorylation of the human β 2 ‐adrenoceptor. Br J Pharmacol 123: 701–711.
20. January B, Seibold A, Whaley B, Hipkin RW, Lin D, Schonbrunn A et al. (1997). 2‐Adrenergic receptor desensitization, internalization and phosphorylation in response to full and partial agonists. J Biol Chem 272: 23871–23879.
21. Kaumann AJ (1996). CGP 12177 induced increase of human atrial contraction through a putative third beta‐adrenoceptor. Br J Pharmacol 117: 93–98.
22. Kaumann AJ, Engelhardt S, Hein L, Molenaar P, Lohse M (2001). Abolition of (−)‐CGP 12177‐evoked cardiostimulation in double beta1/beta2‐adrenoceptor knockout mice. Obligatory role of beta1‐adrenoceptors for putative beta4‐adrenoceptor pharmacology. Naunyn Schmiedebergs Arch Pharmacol 363: 87–93.
23. Kaumann AJ, Preitner F, Sarsero D, Molenaar P, Revelli JP, Giacobino JP (1998). CGP 12177 causes cardiostimulation and binds to cardiac putative beta 4‐adrenoceptors in both wild‐type and beta 3‐adrenoceptor knockout mice. Mol Pharmacol 53: 670–675.
24. Kenakin T, Morgan P, Lutz M (1995). On the importance of the ‘antagonist assumption’ to how receptors express themselves. Biochem Pharmacol 50: 17–26.
25. Konkar AA, Zhu Z, Granneman JG (2000a). Aryloxypropanolamine and catecholamine ligand interactions with the β 1 ‐adrenergic receptor: evidence for interaction with distinct conformations of β 1 ‐adrenergic receptors. J Pharmacol Exp Ther 294: 923–932.
26. Konkar AA, Zhai Y, Granneman JG. (2000b). Beta1‐adrenergic receptors mediate beta3‐adrenergic‐independent effects of CGP 12177 in brown adipose tissue. Mol Pharmacol 57: 252–258.
27. Lewis CJ, Gong H, Brown MJ, Harding SE (2004). Overexpression of beta 1‐adrenoceptors in adult rat ventricular myocytes enhances CGP 12177A cardiostimulation: implications for ‘putative’ beta 4‐adrenoceptor pharmacology. Br J Pharmacol 141: 813–824.
28. Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R (2005). Evaluation of histamine H1‐, H2‐, and H3‐receptor ligands at the human histamine H4 receptor: identification of 4‐methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 314: 1310–1321.
29. Lowe MD, Lynham JA, Grace AA, Kaumann AJ (2002). Comparison of the affinity of β‐blockers for the two states of the β 1 ‐adrenoceptor in ferret ventricular myocardium. Br J Pharmacol 135: 451–461.
30. Malinowska B, Schlicker E (1996). Mediation of the positive chronotropic effect of CGP 12177 and cyanopindolol in the pithed rat by atypical beta‐adrenoceptors, different from beta 3‐adrenoceptors. Br J Pharmacol 117: 943–949.
31. Martínez‐Mir MI, Estañ L, Morales‐Olivas FJ, Rubio E (1992). Effect of histamine and histamine analogues on human isolated myometrial strips. Br J Pharmacol 107: 528–531.
32. Molenaar P (2003). The ‘state′’ of beta‐adrenoceptors. Br J Pharmacol 140: 1–2.
33. Pak MD, Fishman PH (1996). Anomalous behaviour of CGP 12177A on beta 1‐adrenergic receptors. J Recept Signal Transduct Res 16: 1–23.
34. Parsons ME, Ganellin CR (2006). Histamine and its receptors. Br J Pharmacol 147: S127–S135.
35. Qiu R, Melmon KL, Khan MM. (1990). Effects of histamine‐trifluoromethyl‐toluidide derivative (HTMT) on intracellular calcium in human lymphocytes. J Pharmacol Exp Ther 253: 1245–1252.
36. Rang HP (2006). The receptor concept: pharmacology's big idea. Br J Pharmacol 147: S9–S16.
37. Smit MJ, Leurs R, Alewijnse AE, Blauw J, Van Nieuw Amerongen GP, Van De Vrede Y et al. (1996). Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc Natl Acad Sci USA 93: 6802–6807.
38. Wilson JA, Johnston DA, Penston J, Wormsley KG (1986). Inhibition of human gastric secretion by ICI 162,846––a new histamine H2‐receptor antagonist. Br J Clin Pharmacol 21: 685–689.
39. Zakrzeska A, Schlicker E, Kwolek G, Kozłowska H, Malinowska B (2005). Positive inotropic and lusitropic effects mediated via the low‐affinity state of beta1‐adrenoceptors in pithed rats. Br J Pharmacol 146: 760–768.