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- Publications
- Influence
International Union of Pharmacology. XIII. Classification of histamine receptors.
- S. Hill, C. R. Ganellin, +6 authors H. Haas
- Chemistry, Medicine
- Pharmacological reviews
- 1 September 1997
The classification of histamine receptors has to date been based on rigorous classical pharmacological analysis, and as yet, the classification of the three histamine receptors that have been defined… Expand
BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, Hydrochloride], a Nonimidazole Inverse Agonist/Antagonist at the Human Histamine H3 Receptor: Preclinical Pharmacology
- X. Ligneau, D. Perrin, +17 authors J. Schwartz
- Medicine, Chemistry
- Journal of Pharmacology and Experimental…
- 1 January 2007
Histamine H3 receptor inverse agonists are known to enhance the activity of histaminergic neurons in brain and thereby promote vigilance and cognition.… Expand
Histamine and its receptors
- M. Parsons, C. R. Ganellin
- Chemistry, Medicine
- British journal of pharmacology
- 1 January 2006
This article reviews the development of our knowledge of the actions of histamine which have taken place during the course of the 20th century. Histamine has been shown to have a key physiological… Expand
Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.
- X. Ligneau, J. Lin, +7 authors J. Schwartz
- Chemistry, Medicine
- The Journal of pharmacology and experimental…
- 1 November 1998
Ciproxifan, i.e., cyclopropyl-(4-(3-1H-imidazol-4-yl)propyloxy) phenyl) ketone, belongs to a novel chemical series of histamine H3-receptor antagonists. In vitro, it behaved as a competitive… Expand
Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
- R. C. Young, R. C. Mitchell, +7 authors N. E. Sore
- Chemistry, Medicine
- Journal of medicinal chemistry
- 1 March 1988
A rational approach to the design of centrally acting agents is presented, based initially upon a comparison of the physicochemical properties of three typical histamine H2 receptor antagonists which… Expand
Characterization and inhibition of a cholecystokinin-inactivating serine peptidase
- C. Rose, F. Vargas, +7 authors J. Schwartz
- Biology, Medicine
- Nature
- 4 April 1996
A cholecystokinin (CCK)-inactivating peptidase was purified and identified as a membrane-bound isoform of tripeptidyl peptidase II (EC 3.4.14.10), a cytosolic subtilisin-like peptidase of previously… Expand
Protean agonism at histamine H3 receptors in vitro and in vivo
- F. Gbahou, A. Rouleau, +10 authors Jean-Michel Arrang
- Biology, Medicine
- Proceedings of the National Academy of Sciences…
- 5 September 2003
G protein-coupled receptors (GPCRs) are allosteric proteins that adopt inactive (R) and active (R*) conformations in equilibrium. R* is promoted by agonists or occurs spontaneously, leading to… Expand
Distinct pharmacology of rat and human histamine H3 receptors: role of two amino acids in the third transmembrane domain
- X. Ligneau, S. Morisset, +6 authors J. Arrang
- Biology, Medicine
- British journal of pharmacology
- 1 December 2000
Starting from the sequence of the human histamine H3 receptor (hH3R) cDNA, we have cloned the corresponding rat cDNA. Whereas the two deduced proteins show 93.5% overall homology and differ only by… Expand
S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist.
- M. Garbarg, J. Arrang, +4 authors C. R. Ganellin
- Chemistry, Medicine
- The Journal of pharmacology and experimental…
- 1 October 1992
The effects of a new agonist of histamine (HA) H3 receptors, Imetit (S-[2-(4-(imidazolyl)ethyl]isothiourea) were investigated in vitro and in vivo and compared to those of (R)-alpha-methylhistamine… Expand
Enhancement of Hippocampal Pyramidal Cell Excitability by the Novel Selective Slow-Afterhyperpolarization Channel Blocker 3-(Triphenylmethylaminomethyl)pyridine (UCL2077)
- Mala M. Shah, M. Javadzadeh-Tabatabaie, D. Benton, C. R. Ganellin, D. Haylett
- Chemistry, Medicine
- Molecular Pharmacology
- 1 November 2006
The slow afterhyperpolarization (sAHP) in hippocampal neurons has been implicated in learning and memory. However, its precise role in cell excitability and central nervous system function has not… Expand