Antitussive activity of the tachykinin NK1 receptor antagonist, CP-99994, in dogs.

Abstract

CP-99994 [(+)-(2S,3S)-3-(2-methoxybenzylamino)-2-phenylpiperidine] is a selective tachykinin NK(1) receptor antagonist that inhibits cough in guinea pigs and cats. This study examined the antitussive effects of CP-99994 in dogs produced by mechanical stimulation of the intrathoracic trachea. CP-99994 (10 mg/kg, p.o.) inhibited cough frequency by 52% at 2 h, 31% at 6 h and by 21% at 24 h. Cough amplitude was inhibited by 45% at 6 h but unchanged at 2 and 24 h after CP-99994. Plasma levels of CP-99994 were highest at 2 h (75+/-26 ng/ml) and fell to 22+/-6 ng/ml at 6 h. These results demonstrate antitussive activity of CP-99994 in dogs at a dose proven to antagonize tachykinin NK(1) receptors in this species.

• Authors: Richard W Chapman, Aileen House, Fei Liu, Chander Celly, Hong Mei, John A Hey
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 485 Issue 1-3 Pg. 329-32 (Feb 06 2004) ISSN: 0014-2999 [Print] Netherlands
• PMID: 14757157 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Antitussive Agents
• Neurokinin-1 Receptor Antagonists
• Piperidines
• Receptors, Neurokinin-1
• 3-(2-methoxybenzylamino)-2-phenylpiperidine

Topics

• Animals
• Antitussive Agents (pharmacology, therapeutic use)
• Cough (drug therapy, physiopathology)
• Dogs
• Male
• Neurokinin-1 Receptor Antagonists
• Piperidines (pharmacology, therapeutic use)
• Receptors, Neurokinin-1 (physiology)