Sub-anesthetic doses of bupivacaine or lidocaine increase peripheral ICS-205 930-induced analgesia against inflammatory pain in rats.
Intraplantar co-administration of sub-anesthetic doses of bupivacaine (2.5 microg) or lidocaine (7.5 microg) increased the dose- and time-dependent analgesic effects of the 5-HT3 receptor antagonist, 3-a-tropanyl-1-H-indole-3-carboxylic ester (ICS-205 930) (1-100 microg; 50 microl) against inflammatory pain induced by hindpaw inoculation with complete Freund's adjuvant. The effects of bupivacaine were greater than lidocaine at all doses of ICS-205 930 tested. These findings may reflect facilitation of ICS-205 930 effects through negative allosteric modulation by bupivacaine and lidocaine of peripheral 5-HT3 receptors involved in nociceptive processing.
Giordano
J
J
Pain Clinic, Southeast Texas Rehabilitation Hospital, Beaumont 77707, USA.
Sacks
S M
SM
D000698:Analgesia; D000779:Anesthetics, Local / Q000008:administration & dosage / Q000494:pharmacology*; D000818:Animals; D002045:Bupivacaine / Q000008:administration & dosage / Q000494:pharmacology*; D004357:Drug Synergism; D007211:Indoles / Q000008:administration & dosage / Q000494:pharmacology*; D007249:Inflammation; D008012:Lidocaine / Q000008:administration & dosage / Q000494:pharmacology*; D008297:Male; D010146:Pain / Q000188:drug therapy; D010147:Pain Measurement; D051381:Rats; D012702:Serotonin Antagonists / Q000008:administration & dosage / Q000494:pharmacology*; D000077526:Tropisetron
D000779:Anesthetics, Local; D007211:Indoles; D012702:Serotonin Antagonists; D000077526:Tropisetron; D008012:Lidocaine; D002045:Bupivacaine