Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Charon R. Ganellin"'
Autor:
G. J. Durant, R W Brimblecombe, J W Black, Michael E. Parsons, Charon R. Ganellin, W. A. M. Duncan
Publikováno v:
British Journal of Pharmacology. 160:S52-S53
Burimamide and metiamide which have been described previously (Black, Duncan, Durant, Ganellin & Parsons, 1972; Black, Duncan, Emmett, Ganellin, Hesselbo, Parsons & Wyllie, 1973) are histamine H2-receptor antagonists. This communication describes som
Publikováno v:
Philosophical Transactions of the Royal Society of London. B, Biological Sciences. 272:75-85
The specificity of binding between small molecules and macromolecular receptors may be studied by comparing theoretically calculated conformational potential energy surfaces of a series of chemically similar molecules which have a range of receptor b
Autor:
G.B. Leslie, W. A. M. Duncan, G. J. Durant, R W Brimblecombe, Charon R. Ganellin, John Colin Emmett, Michael E. Parsons
Publikováno v:
Gastroenterology. 74:339-347
The concept of two classes of histamine receptor, H 1 and H 2 , is introduced and the chemical derivation of histamine H 2 -receptor antagonists is outlined briefly. Starting from the structure of histamine, chemical modification led eventually to bu
Publikováno v:
Agents and Actions. 7:31-37
S-[3-(N,N-Dimethylamino)propyl]isothiourea (dimaprit), has been shown to be a highly specific histamine H2-receptor agonist. Parallel line assays showed that in vitro at H2-receptors it had approximately 17.5% the activity of histamine on the rat ute
Publikováno v:
Agents and Actions. 7:39-43
Dimaprit, S-[3-(N,N-dimethylamino)propyl]isothiourea, appears to be a highly specific histamine H2-receptor agonist. Further indications of specificity are obtained from chemical considerations. Dimaprit has two basic centres (pKa values respectively
Autor:
W. A. M. Duncan, Charon R. Ganellin, Michael E. Parsons, R W Brimblecombe, G. J. Durant, John Colin Emmett
Publikováno v:
Journal of International Medical Research. 3:86-92
Cimetidine is a non-thiourea analogue of metiamide. It is a specific competitive histamine H2-receptor antagonist and is an effective inhibitor of gastric secretion in animals and man with similar pharmacological properties to metiamide. No renal dam
Autor:
Charon R. Ganellin, B. K. Leigh, C. A. Price, I. R. Smith, Wasyl Tertiuk, Robert Blakemore, Michael E. Parsons
Publikováno v:
Agents and Actions. 19:18-25
Dimaprit analogues having alkyl substituents on the isothiourea group have no detectable H2-agonist activity on the guinea-pig atrium. N-Methyldimaprit [S-[3-(N,N-dimethylamino)propyl]-N'-methylisothiourea] (SKF92054) is identified as a compound whic
Autor:
D. A. A. Owen, Charon R. Ganellin
Publikováno v:
Agents and Actions. 7:93-96
Burimamide, a histamine H2-receptor antagonist, has been shown to cause pressor responses in pithed rats. The response can be prevented by prior removal of the adrenal glands or by pretreatment with the alpha-adrenoceptor antagonist, phentolamine, 5
Autor:
G. J. Durant, Robert Blakemore, Terence F. Walker, Michael E. Parsons, A. C. Rasmussen, P. Blurton, Thomas Henry Brown, D. A. Rawlings, Charon R. Ganellin
Publikováno v:
European Journal of Medicinal Chemistry. 24:65-72
A series of 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-4-pyrimidones was synthesised based on oxmetidine 2 , in which the methylenedioxyphenyl group of 2 was replaced by a heterocyclic ring. Good H 2 -receptor antagonist activity was retained
Publikováno v:
Agents and Actions. 9:26-28