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(±)‐CP‐96,345, a selective tachykinin NK 1 receptor antagonist, has non‐specific actions on neurotransmission
Author(s) -
Wang ZunYi,
Håkanson Rolf
Publication year - 1992
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1992.tb14520.x
Subject(s) - taenia coli , vas deferens , carbachol , tachykinin receptor , endocrinology , medicine , chemistry , seminal vesicle , receptor , stimulation , guinea pig , biology , neuropeptide , substance p , prostate , cancer
1 The non‐specific effects of the non‐peptide tachykinin receptor antagonist (±)‐CP‐96,345, were assessed in several smooth muscle‐nerve preparations. The preparations were the iris sphincter muscle of the rabbit and the taenia coli, vas deferens and seminal vesicle of the guinea‐pig. 2 (±)‐CP‐96,345 concentration‐dependently inhibited the elctrically evoked, tachykinin‐mediated contractile responses of the iris sphincter and the taenia coli. The pIC 50 values were 5.4 ± 0.2 (mean ± s.e.mean) and 5.7 ± 0.08 respectively. 3 (±)‐CP‐96,345 also inhibited non‐tachykinin‐mediated contractile responses to electrical stimulation of the iris sphincter, taenia coli, vas deferens and seminal vesicle. The pIC 50 values were 4.3 ± 0.02, 4.8 ± 0.03, 4.7 ± 0.02 and 4.4 ± 0.05 respectively. These values differ significantly from the pIC 50 values of the inhibition of the tachykinin‐mediated response in the iris sphincter and taenia coli. 4 (±)‐CP‐96,345 was without effect on carbachol‐ and noradrenaline‐evoked contractions of the iris sphincter but inhibited carbachol‐ and prostaglandin F 2α (PGF 2α )‐evoked contractions of the taenia coli. 5 We suggest that (±)‐CP‐96,345, apart from its NK 1 receptor blocking activity, induces non‐specific suppression of neurotransmission, exerted at both pre‐ and post‐junctional sites.