Design of non-peptide agonists and antagonists at neuropeptide receptors starting from the chemical structure of neuropeptides |
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| Authors: | David C Horwell |
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| Institution: | (1) Parke-Davis Neuroscience Research Centre, Cambridge University Forvie Site, Robinson Way, CB2 2QB Cambridge, U.K. |
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| Abstract: | Summary Non-peptide small-molecule antagonists for cholecystokinin (CCK)-A and-B receptors, tachykinin NK-1, NK-2 and NK-3 receptors
and bombesin BB-1 receptors have been designed and synthesized starting from the chemical structure of the endogenous mammalian
neuropeptides cholecystokinin, substance-P and bombesin, respectively. A non-peptide CCK-A agonist, with weak potency but
high efficacy, was also identified from the same strategy. |
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| Keywords: | BB-1 BB-2 receptors bombesin CCK-A CCK-B cholecystokinin gastrin releasing peptide neuromedin-B NK-1 NK-2 NK-3 peptidomimetics Small-molecule non-peptide agonists and antagonists rational design substance-P tachykinins |
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