Search narrowed by
Advanced Search
- Type of publication
- Publication (2)
- Year
- Journal / Volume / Preprint Server Sorted by frequency and by alphabetical order
- Farmaco (1)
- Sci. Cult. (1)
- Author Sorted by frequency and by alphabetical order
- Schmidt, J. (13)
- Brandt, W. (11)
- Hause, B. (9)
- Scheel, D. (8)
- Strack, D. (8)
- Wasternack, C. (8)
- Adam, G. (6)
- Feussner, I. (5)
- Rosahl, S. (5)
- Wessjohann, L. A. (5)
- Abel, S. (4)
- Clemens, S. (4)
- Miersch, O. (4)
- Porzel, A. (4)
- Ansorge, S. (3)
- Fengler, A. (3)
- Fester, T. (3)
- Fuchs, P. (3)
- Heide, L. (3)
- Knogge, W. (3)
- Kolbe, A. (3)
- Lee, J. (3)
- Li, S.-M. (3)
- Nürnberger, T. (3)
- Sung, T. V. (3)
- Abdala, G. (2)
- Anh, N. T. H. (2)
- Barre, A. (2)
- Braga, A. L. (2)
- Brunner, F. (2)
- Demuth, H.-U. (2)
- Dussle, C. (2)
- Englberger, W. (2)
- Faust, J. (2)
- Friderichs, E. (2)
- Grubb, C. D. (2)
- Göbel, C. (2)
- Hoffmann, T. (2)
- Holzgrabe, U. (2)
- Kramell, R. (2)
- Kuhl, U. (2)
- Kuhnt, C. (2)
- Kutchan, T. M. (2)
- Lübberstedt, T. (2)
- Melchinger, A. (2)
- Mrestani-Klaus, C. (2)
- Neubert, K. (2)
- Nies, D. H. (2)
- Peumans, W. J. (2)
- Proost, P. (2)
- Quint, M. (2)
- Reinhold, D. (2)
- Rougé, P. (2)
- Rudd, J. J. (2)
- Schilling, S. (2)
- Schmidt, D. (2)
- Schneider, G. (2)
- Siener, T. (2)
- Silveira, C. C. (2)
- Van Damme, E. J. M. (2)
- Vogt, T. (2)
- Walter, M. H. (2)
- Weichert, H. (2)
- Wray, V. (2)
- Wrenger, S. (2)
- Xu, M. (2)
- Adam, W. (1)
- Alemano, S. (1)
- Alpermann, H. (1)
- Anders, A. (1)
- Apel, K. (1)
- Appelt, H. R. (1)
- Bachmann, A. (1)
- Baumeister, U. (1)
- Baumert, A. (1)
- Baumruk, V. (1)
- Bellini, C. (1)
- Berlich, M. (1)
- Bloss, T. (1)
- Bloß, T. (1)
- Bonamico, B. (1)
- Bramley, P. M. (1)
- Bras, J. (1)
- Bruns, I. (1)
- Brömme, D. (1)
- Buske, A. (1)
- Bühling, F. (1)
- Cambareri, A. (1)
- Camberri, A. (1)
- Castro, G. (1)
- Champion, A. (1)
- Chapple, C. (1)
- Chen, D. L. (1)
- Chen, Y. (1)
- Choe, Y. (1)
- Craik, C. S. (1)
- Dangl, J. L. (1)
- Darvill, A. G. (1)
- De-Eknamkul, W. (1)
- Dechert, C. (1)
Displaying results 1 to 2 of 2.
Holzgrabe, U.; Cambareri, A.; Kuhl, U.; Siener, T.; Brandt, W.; Straßburger, W.; Friderichs, E.; Englberger, W.; Kögel, B.; Haurand, M.; Diazabicyclononanones, a potent class of kappa opioid analgesics Farmaco 57, 531-534, (2002) DOI: 10.1016/S0014-827X(02)01243-0
The 1,5-dimethyl 3,7-diaza-3,7-dimethyl-9-oxo-2,4-di-2-pyridine-bicyclo[3.3.1]nonane-1,5-dicarboxylate, HZ2, has a high and selective affinity for the kappa opioid receptor and an antinociceptive activity comparable to morphine. In addition, it is characterized by a long duration of action and a high oral bioavailability. QSAR studies within series of kappa agonists revealed a chair-boat conformation of a double protonated HZ2 characterized by an almost parallel orientation of the C9 carbonyl group and the N7-H group and at least one aromatic ring to be the pharmacophoric arrangement. Structural variations showed that the pyridine rings in 2 and 4 position can be replaced with p-methoxy-, m-hydroxy- and m-fluoro-substituted phenyl rings. However, all other substituents have to be kept the same for a high affinity to the kappa receptor.
Holzgrabe, U.; Friderichs, E.; Englberger, W.; Strassberger, W.; Maurand, M.; Brandt, W.; Camberri, A.; Kuhl, U.; Siener, T.; Diazabicyclononanones, a new class of opioid-type analgesics Sci. Cult. 68, 1-4, (2002)
0