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A series of novel, highly potent and selective agonists for the κ‐opioid receptor
Author(s) -
Hayes A.G.,
Birch P.J.,
Hayward N.J.,
Sheehan M.J.,
Rogers H.,
Tyers M.B.,
Judd D.B.,
Scopes D.I.C.,
Naylor A.
Publication year - 1990
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1990.tb14185.x
Subject(s) - vas deferens , pharmacology , opioid , agonist , κ opioid receptor , chemistry , (+) naloxone , ed50 , hamster , receptor , opioid receptor , diprenorphine , medicine , biochemistry
1 This paper describes the opioid receptor pharmacology and in vivo activity of several novel benzeneacetamidopiperidine and benzeneacetamidopiperazine analogues. 2 These compounds all showed potent, naloxone‐reversible, full agonist activiy in the field‐stimulated rabbit vas deferens, indicating that they are κ‐opioid agonists; but showed very little activity in the rat or hamster vas deferens, indicating good selectivity with regard to μ‐ and δ‐opioid receptors. 3 They were all potent antinociceptive agents, the most potent compound, GR103545, having an ED 50 value in the mouse abdominal constriction test of 0.25 μg 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 κ‐opioid receptor.