[Effects of methanobenzazonine (2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine) derivatives on the cough reflex and respiration].

Abstract

Antitussive and respiratory effects of three newly synthesized methanobenzazonine derivatives and their d- and l-isomers were investigated to understand the relationship between the cough and respiratory centers. Antitussive effects were evaluated with the PEC (puncture electrode-induced cough) method in conscious d-, dl-, and l-ST-2123; d-, dl-, and l-ST-2121 into the right carotid artery at a dose range of 0.2-0.8 mg caused no effect on respiration. dl-ST-2121 at 0.4 to 0.8 mg and l-ST-2121 at 0.2 to 0.8 mg depressed respiration dose-dependently. Codeine (0.2-0.8 mg) depressed respiration slightly. Morphine (0.2-0.8 mg) depressed respiration more strongly. All the methanobenzazonine derivatives used, when given intraperitoneally, showed antitussive potencies that were 1/3-1/2 the potency of codeine. The antitussive potencies of the d-, dl-, and l-isomers of the three derivatives used were discussed on the bases of chemical structures and drug receptors. These results provide evidence of a discrepancy between the cough and respiratory centers in the brain stem.

• Authors: S Yanaura, H Kitagawa, T Hosokawa, M Misawa
• Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica (Nihon Yakurigaku Zasshi) Vol. 80 Issue 1 Pg. 43-50 (Jul 1982) ISSN: 0015-5691 [Print] Japan
• PMID: 7173733 (Publication Type: English Abstract, Journal Article)

Chemical References

• Antitussive Agents
• Azepines
• eptazocine hydrobromide

Topics

• Animals
• Antitussive Agents
• Azepines (pharmacology)
• Cough (drug therapy)
• Guinea Pigs
• Isomerism
• Male
• Optical Rotation
• Reflex (drug effects)
• Respiration (drug effects)
• Structure-Activity Relationship