Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Michael R. Stillings"'
Publikováno v:
British Journal of Pharmacology. 110:1017-1022
1. The imidazoline alpha 2-adrenoceptor antagonist, efaroxan, stimulates insulin secretion from rat isolated islets and antagonizes the ability of diazoxide to inhibit glucose-induced insulin secretion. These effects result from closure of ATP-sensit
Publikováno v:
European Journal of Pharmacology. 204:41-48
The actions of efaroxan, a highly selective and potent α 2 -adrenoceptor antagonist, on insulin secretion, cAMP levels, 86 Rb4 + efflux and ATP-regulated potassium (K + ATP ) channels have been studied using isolated pancreatic islets of Langerhans
Publikováno v:
Biochemical and Biophysical Research Communications. 176:1545-1551
The selective alpha 2-antagonist DG-5128 provoked a dose-dependent stimulation of insulin release from isolated rat islets. DG-5128 was only weakly effective as an antagonist of noradrenaline-induced inhibition of insulin secretion but, surprisingly,
Autor:
Nigel C. Phillips, David C. Atkinson, Peter Myers, Anthony P. Welbourn, Michael R. Stillings, Keith E. Godfrey
Publikováno v:
Journal of Medicinal Chemistry. 26:1353-1360
The synthesis and antiinflammatory activity of a series of substituted (2-phenoxyphenyl)acetic acids are described. Initial screening in the adjuvant arthritis test showed that halogen substitution in the phenoxy ring enhanced activity considerably.
Autor:
Christopher B. Chapleo, John C. Doxey, C. F. C. Smith, Peter Myers, Malcolm Myers, Michael R. Stillings
Publikováno v:
European Journal of Medicinal Chemistry. 24:619-622
A preliminary communication reported on the pharmacology of the potent partial α2-agonist (2-(1,4-benzodioxan-6-ylamino)-2-imidazoline, a 1,4-dioxan derivative of clonidine. Its degree of agonism/antagonism depended upon the peripheral or central α
Publikováno v:
Journal of Medicinal Chemistry. 29:2280-2284
This paper describes the synthesis and pharmacological evaluation of a number evaluation of a number of substituted 1,3,4-thiadiazoles. The first member of the series, 2-(aminomethyl)-5-(2-biphenylyl)-1,3,4-thiadiazole (7) was found to possess potent
Autor:
Richard C. M. Butler, C. F. C. Smith, Alan Geoffrey Roach, Christopher B. Chapleo, J. A. Davis, John C. Doxey, Peter Myers, Michael R. Stillings, S. D. Higgins, Malcolm Myers
Publikováno v:
Journal of Medicinal Chemistry. 27:570-576
Modification of the 1,4-benzodioxan ring present in RX 781094 has not previously been considered. This paper describes a number of analogues of this ring system, including compounds in which one of the oxygen atoms has been replaced by a methylene gr
Publikováno v:
Journal of Medicinal Chemistry. 29:1780-1783
We have recently reported the synthesis and alpha 2-antagonist activity of the methoxy derivative 2 [2-(2-methoxy-1,4-benzodioxan-2-yl)-2-imidazoline] and described the enhanced potency of this compound over the parent 1,4-benzodioxan, idazoxan, in r
Autor:
Peter Myers, Michael R. Stillings, Christopher B. Chapleo, Richard C. M. Butler, John C. Doxey, C. D. England, Malcolm Myers, Anthony P. Welbourn, N. Tweddle, J. A. Davis
Publikováno v:
Journal of Medicinal Chemistry. 28:1054-1062
The synthesis and pharmacological activity of a series of 2-substituted derivatives of the selective alpha 2-adrenoreceptor antagonist idazoxan (RX 781094) is described. Substitution in this position by alkyl, alkenyl, cycloalkenyl, and alkoxy groups
Publikováno v:
Tetrahedron. 34:1381-1383
The ratio of endo -CHO: exo -CHO in the Diels-Alder addition of a trans -αβ-unsaturated aldehyde to cyclopentadiene can be changed from 1:2 to 8:1, depending on temperature and BF 3 -catalysis.