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. 1990 Dec;101(4):944–948. doi: 10.1111/j.1476-5381.1990.tb14185.x

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

A G Hayes 1, P J Birch 1, N J Hayward 1, M J Sheehan 1, H Rogers 1, M B Tyers 1, D B Judd 1, D I Scopes 1, A Naylor 1
PMCID: PMC1917842  PMID: 1964823

Abstract

1. This paper describes the opioid receptor pharmacology and in vivo activity of several novel benzene-acetamidopiperidine and benzeneacetamidopiperazine analogues. 2. These compounds all showed potent, naloxone-reversible, full agonist activity in the field-stimulated rabbit vas deferens, indicating that they are kappa-opioid agonists; but showed very little activity in the rat or hamster vas deferens, indicating good selectivity with regard to mu- and delta-opioid receptors. 3. They were all potent antinociceptive agents, the most potent compound, GR 103545, having an ED50 value in the mouse abdominal constriction test of 0.25 micrograms kg-1 s.c. The compounds also produced sedation and diuresis, but had little effect on respiration rate or gastrointestinal motility. 4. It is concluded that the seven novel compounds described are all potent and selective agonists for the kappa-opioid receptor.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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