Abstract
Histamin, through changes in its molecular structure, in situ, may exert selectivity on its two different receptors, where stimulation generally leads to responses in opposite directions. The mentioned structural changes are made possible
either by tautomerism or via conformational reshaping. These isomeric forms of histamine were found to possess certain selectivity on HI and 1-12 receptors. Changes in the ionic composition and energy avaliability of the media, through altering the ratio of the selective forms, may direct the interaction of the molecule with its two different receptors.
References
- 1. Ash, A.S.F., Schild, H.O,. Receptors mediating some actions of histamine, Br J Phar macol Chemother 27 : 427, 1966.
- 2. Black, J.M., DunCan, W.A.M., Durant, c.J., Ganellin, C.R., Parsons, E.M„ Definition and antagonism of histamine Hn•receptors, Nature 236 : 385, 1972
- 3 Bökesoy, T.A., Vasküler düz kasta histaminin bölgesel agonistik aktivitesi ve histamine duyarslzlayna, Doçentlik Tezi, Ankara 1980.
- 4. Cook, D.A., Kenakin, T.P., Krueger, C.A., Alterations in temperature and histamin re- ceptor function, Fed Proc 36 : 2584, 1977.
- 5. Durant, C.J., Ganellin ,C.R., Parsons, E.M., Chemical differentiation of histamine HI and H2-receptor agonists, J Med Chem 18 : 905, 1975.
- 6. Ganell.in, C.R., Papper, E.S., Port, G.N.J., Richards, W.G., Conformation of histamine derivatives 1. Application of molecular orbital calculations and NMR spectroscopy. I. Med Chem 16 : 611, 1973.
- 7. Ganellin, C.R., Prot) G.N.J.. Richards, W.G.•, Conformation of histamine derivatives 2. Molecular orbital calculations of preferred conformations in relation to dual • receptor activity, J Med Chem 16 : 616, 1973.
Abstract
Histamin, moleküler yapısındaki in situ değişmelerle iki değişik resep-örüne seçicilik gösterebilmektedir. Bu reseptörler genellikle iki farklı yönde cevap tan sorumludurlar. Söz konusu değişimler ya totomerizm ya da konformasyonel yeni şekillenme yoluyla olmaktadır. Histaminin bu izomerik şekilleri Hl ve H2 reseptörlerinde belirli seçicilik sağlayabilmektedir. Ortamın iyonik bileşiminde veya enerji düzeylerindeki değişim, bu reseptör seçici şekillerin oranlarını farklılandırarak, molekülün iki farklı reseptörüyle etkileşmesini yönlendirebilmektedir.
References
- 1. Ash, A.S.F., Schild, H.O,. Receptors mediating some actions of histamine, Br J Phar macol Chemother 27 : 427, 1966.
- 2. Black, J.M., DunCan, W.A.M., Durant, c.J., Ganellin, C.R., Parsons, E.M„ Definition and antagonism of histamine Hn•receptors, Nature 236 : 385, 1972
- 3 Bökesoy, T.A., Vasküler düz kasta histaminin bölgesel agonistik aktivitesi ve histamine duyarslzlayna, Doçentlik Tezi, Ankara 1980.
- 4. Cook, D.A., Kenakin, T.P., Krueger, C.A., Alterations in temperature and histamin re- ceptor function, Fed Proc 36 : 2584, 1977.
- 5. Durant, C.J., Ganellin ,C.R., Parsons, E.M., Chemical differentiation of histamine HI and H2-receptor agonists, J Med Chem 18 : 905, 1975.
- 6. Ganell.in, C.R., Papper, E.S., Port, G.N.J., Richards, W.G., Conformation of histamine derivatives 1. Application of molecular orbital calculations and NMR spectroscopy. I. Med Chem 16 : 611, 1973.
- 7. Ganellin, C.R., Prot) G.N.J.. Richards, W.G.•, Conformation of histamine derivatives 2. Molecular orbital calculations of preferred conformations in relation to dual • receptor activity, J Med Chem 16 : 616, 1973.
Details
| Primary Language | Turkish |
|---|---|
| Subjects | Basic Pharmacology |
| Journal Section | Research Article |
| Authors | |
| Publication Date | December 31, 1981 |
| Published in Issue | Year 1981 Volume: 34 Issue: 4 |