| Autor: |
Carroll, W. A., Agrios, K. A., Altenbach, R. J., Buckner, S. A., Chen, Y., Coghlan, M. J., Daza, A. V., Drizin, I., Gopalakrishnan, M., Henry, R. F., Kort, M. E., Kym, P. R., Milicic, I., Smith, J. C., Tang, R., Turner, S. C., Whiteaker, K. L., Zhang, H., Sullivan, J. P. |
| Zdroj: |
Journal of Medicinal Chemistry; June 2004, Vol. 47 Issue: 12 p3180-3192, 13p |
| Abstrakt: |
Structure−activity relationships were investigated on a novel series of tricyclic dihydropyridine-containing KATP openers. This diverse group of analogues, comprising a variety of heterocyclic rings fused to the dihydropyridine nucleus, was designed to determine the influence on activity of hydrogen-bond-donating and -accepting groups and their stereochemical disposition. Compounds were evaluated for KATP activity in guinea pig bladder cells using a fluorescence-based membrane potential assay and in a pig bladder strip assay. The inhibition of spontaneous bladder contractions in vitro was also examined for a subset of compounds. All compounds studied showed greater potency to inhibit spontaneous bladder contractions relative to their potencies to inhibit contractions elicited by electrical stimulation. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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