Analgesic effects of S and R isomers of the novel 5-HT3 receptor antagonists ADR-851 and ADR-882 in rats.

Abstract

The present study examined analgesia produced by S and R isomers of the novel 5-HT3 receptor antagonists, ADR-851 and ADR-882 (0.1-10 mg/kg s.c.) against acute thermal, mechanical and formalin-induced inflammatory pain in rats. Neither isomer of ADR-851 or ADR-882 was analgesic in the thermal or mechanical test. Similarly, neither S or R forms of ADR-882 produced significant anti-nociception in the formalin test. In contrast, ADR-851R produced significant analgesia at 3 and 10 mg/kg doses in this test, while ADR-851S produced significant analgesia only at 1 mg/kg.

• Authors: K J Sufka, J Giordano
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 204 Issue 1 Pg. 117-9 (Oct 29 1991) ISSN: 0014-2999 [Print] Netherlands
• PMID: 1804661 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Analgesics
• Benzofurans
• Bridged Bicyclo Compounds
• Bridged Bicyclo Compounds, Heterocyclic
• Serotonin Antagonists
• ADR 851
• ADR 882
• Formaldehyde
• Metoclopramide

Topics

• Analgesics (pharmacology)
• Animals
• Behavior, Animal (drug effects)
• Benzofurans (pharmacology)
• Bridged Bicyclo Compounds (pharmacology)
• Bridged Bicyclo Compounds, Heterocyclic
• Formaldehyde
• Inflammation (chemically induced, complications)
• Male
• Metoclopramide (analogs & derivatives, pharmacology)
• Motor Activity (drug effects)
• Nociceptors (drug effects)
• Pain (drug therapy, etiology)
• Rats
• Rats, Inbred Strains
• Respiration (drug effects)
• Serotonin Antagonists (pharmacology)
• Stereoisomerism