Antinociceptive property of the nicotinic agonist AG-4 in rodents

✍ Scribed by Carla Ghelardini; Nicoletta Galeotti; Fulvio Gualtieri; Cristina Bellucci; Dina Manetti; Pier Andrea Borea; Alessandro Bartolini

• Publisher: John Wiley and Sons
• Year: 1997
• Tongue: English
• Weight: 208 KB
• Volume: 41
• Category: Article
• ISSN: 0272-4391
• DOI: 10.1002/(sici)1098-2299(199705)41:1<1::aid-ddr1>3.0.co;2-m

✦ Synopsis

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.