Differences in the effects of NK1-receptor antagonists, (+/-)-CP 96,345 and CP 99,994, on agonist-induced responses in guinea-pig trachea.
1. The effects of the NK1-receptor antagonists, (+/-)-CP 96,345 and CP 99,994, on NK1-agonist evoked contractions were compared in isolated rings of guinea-pig tracheal smooth muscle. 2. (+/-)-CP 96,345 and CP 99,994 were similarly effective in antagonizing responses evoked by septide, whereas CP 99,994 was more effective than (+/-)-CP 96,345 in inhibiting responses evoked by [Sar9Met11(O2)] substance P. 3. These results suggest that responses to septide and [Sar9Met11(O2)] substance P may be operated via different populations of NK1-receptors.
Longmore
J
J
Merck Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex.
Razzaque
Z
Z
Shaw
D
D
Hill
R G
RG
D000818:Animals; D001713:Biphenyl Compounds / Q000494:pharmacology*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology; D054833:Isoindoles; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects*; D015288:Neurokinin A / Q000037:antagonists & inhibitors*; D064729:Neurokinin-1 Receptor Antagonists; D010446:Peptide Fragments / Q000037:antagonists & inhibitors / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology*; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives; D013373:Substance P / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000494:pharmacology; D014132:Trachea / Q000187:drug effects
D001713:Biphenyl Compounds; D007211:Indoles; D054833:Isoindoles; D064729:Neurokinin-1 Receptor Antagonists; D010446:Peptide Fragments; D010880:Piperidines; C062618:substance P, Sar(9)-Met(O2)(11)-; C071693:7,7-diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one; C080755:3-(2-methoxybenzylamino)-2-phenylpiperidine; D013373:Substance P; C054725:septide; D015288:Neurokinin A; D011761:Pyrrolidonecarboxylic Acid; C066892:CP 96345