By P N Kourounakis
The dept of Pharmaceutical-Medicinal Chemistry, tuition of Pharmacy, Aristotelian college of Thessaloniki, organizes, some other yr, a graduate seminar in complicated medicinal chemistry, with overseas participation, in Thessaloniki. the aim of this seminar is to aid younger and impressive pharmaceutical scientists during this box by way of updating their wisdom and informing them in regards to the new developments in our technological know-how, during the displays of popular invited audio system. it's also aimed to create a discussion board for alternate of rules in medicinal chemistry, in a distinct casual atmosphere, bringinginternationally famous medicinal chemists towards their Greek colleagues. the various invited audio system during this sequence of seminars are: A.H.Beckett, A.Benakis, N.Bodor, D.D.Breimer, J.Caldwell, R.Ganellin, J.Gorrod, R.Franke, H.Kappus, P.Krogsgaard-Larsen, A.Makriyiannis, J.Seydel, H.Sies, J.Tollenaere and W.Wiegrebe.
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Additional info for Advanced Drug Design and Development: A Medicinal Chemistry Approach
10). The action of 4-PIOL was compared with that of the GABAA agonist isoguvacine. The response to 4-PIOL was competitively antagonized by bicuculline methobromide (BMB) (not illustrated). 4-PIOL was about 200 times less potent as an agonist than isoguvacine. The maximum response to 4-PIOL was only a small fraction of that of submaximal concentrations of isoguvacine, and 4-PIOL antagonized the response to isoguvacine with a parallel shift to the right of the dose-response curve . On the basis of these studies it is concluded that 4-PIOL is a low-efficacy partial GABAA agonist showing also a GABAA antagonist profile (Fig.
5, 57. , Lauridsen, J. R. (1985) J. Med. , 28, 673. O. R. (1989) J. Med. , 32, 2254. J. and Krogsgaard-Larsen, P. , 1, 138. J. and Krogsgaard-Larsen, P. S. ), Munksgaard, Copenhagen, p. 92. W. J. (1989) J. —Aided Mol. Design, 2, 321. , Krogsgaard-Larsen, P. and Schousboe, A. (1990) J. , 55, 1821. , Lodge, D. R. (1977) Nature (London), 268, 53. Gruska Institute of Drug Research, Alfred-Kowalke-Str. 4, 0–1136 Berlin, Germany SUMMARY Biological properties of chemical compounds depend in a very sensitive way on their chemical structure.
And Krogsgaard-Larsen, P. S. ), Munksgaard, Copenhagen, p. 92. W. J. (1989) J. —Aided Mol. Design, 2, 321. , Krogsgaard-Larsen, P. and Schousboe, A. (1990) J. , 55, 1821. , Lodge, D. R. (1977) Nature (London), 268, 53. Gruska Institute of Drug Research, Alfred-Kowalke-Str. 4, 0–1136 Berlin, Germany SUMMARY Biological properties of chemical compounds depend in a very sensitive way on their chemical structure. The understanding of such dependencies in terms of socalled structure-activity relationships is one of the principal goals of medicinal chemistry and at the heart of modern computer-aided drug design (CADD).
Advanced Drug Design and Development: A Medicinal Chemistry Approach by P N Kourounakis