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Antinociceptive property of the nicotinic agonist AG‐4 in rodents
Author(s) -
Ghelardini Carla,
Galeotti Nicoletta,
Gualtieri Fulvio,
Bellucci Cristina,
Manetti Dina,
Borea Pier Andrea,
Bartolini Alessandro
Publication year - 1997
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/(sici)1098-2299(199705)41:1<1::aid-ddr1>3.0.co;2-m
Subject(s) - mecamylamine , nociception , chemistry , nicotinic agonist , pharmacology , agonist , (+) naloxone , atropine , endocrinology , opioid , medicine , receptor , biochemistry
AG‐4 has been characterized as a nicotinic agonist by binding (K i = 26 ± 1.4 μM) and in vitro functional assays. The antinociceptive effect of AG‐4 was examined in mice and rats, using the hot plate, abdominal constriction, and paw‐pressure tests. In both species, AG‐4 (25–150 μg per mouse icv; 100–150 μg per rat icv) produced significant antinociception which was prevented by mecamylamine (2 mg kg –1 ip) and pempidine (3 mg kg –1 i.p.), but not by atropine (5 mg kg –1 ip), naloxone (1 mg kg –1 ip) and CGP 35348 (100 mg kg –1 ip). In the antinociceptive dose range, AG‐4 did not impair mice motor coordination and spontaneous motility as well as inspection activity. The present results have shown that AG‐4 is a compound endowed with antinociceptive properties mediated via nicotinic activation and may be a promising beginning for new nicotinic agonists. Drug Dev. Res. 41:1–9, 1997. © 1997 Wiley‐Liss, Inc.