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Literature DB >> 2850924

A novel series of potent and selective agonists at the opioid kappa-receptor.

G F Costello¹, B G Main, J J Barlow, J A Carroll, J S Shaw.

Abstract

Three novel opioid agonists are described. These compounds were found to bind with high affinity and selectivity to the kappa-opioid receptor. Isolated tissue studies using the field-stimulated mouse vas deferens and guinea-pig ileum preparations confirmed the high agonist potency and naloxone-reversibility of these agents. All three compounds exhibited potent antinociceptive activity in the mouse abdominal constriction model. These compounds should prove useful as tools to investigate kappa-receptor function.

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Year: 1988 PMID： 2850924 DOI： 10.1016/0014-2999(88)90546-8

Source DB: PubMed Journal: Eur J Pharmacol ISSN： 0014-2999 Impact factor: 4.432

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Cited

8 in total

A novel series of potent and selective agonists at the opioid kappa-receptor.

1. Neuroprotective actions of GR89696, a highly potent and selective kappa-opioid receptor agonist.

2. NMR structure and dynamics of the agonist dynorphin peptide bound to the human kappa opioid receptor.

3. CI-977, a novel and selective agonist for the kappa-opioid receptor.

4. ICI 204448: a kappa-opioid agonist with limited access to the CNS.

5. Central and peripheral actions of the novel kappa-opioid receptor agonist, EMD 60400.

6. A pharmacological profile of the novel, peripherally-selective kappa-opioid receptor agonist, EMD 61753.

7. A series of novel, highly potent and selective agonists for the kappa-opioid receptor.

8. Computational design of syntheses leading to compound libraries or isotopically labelled targets.