Autor: |
Sebhat, I. K., Martin, W. J., Ye, Z., Barakat, K., Mosley, R. T., Johnston, D. B. R., Bakshi, R., Palucki, B., Weinberg, D. H., MacNeil, T., Kalyani, R. N., Tang, R., Stearns, R. A., Miller, R. R., Tamvakopoulos, C., Strack, A. M., McGowan, E., Cashen, D. E., Drisko, J. E., Hom, G. J., Howard, A. D., MacIntyre, D. E., Ploeg, L. H. T. van der, Patchett, A. A., Nargund, R. P. |
Zdroj: |
Journal of Medicinal Chemistry; October 2002, Vol. 45 Issue: 21 p4589-4593, 5p |
Abstrakt: |
Synthetic and natural peptides that act as nonselective melanocortin receptor agonists have been found to be anorexigenic and to stimulate erectile activity. We report the design and development of 1, a potent, selective (1184-fold vs MC3R, 350-fold vs MC5R), small-molecule agonist of the MC4 receptor. Pharmacological testing confirms the food intake lowering effects of MC4R agonism and suggests another role for the receptor in the stimulation of erectile activity. |
Databáze: |
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