Reference : The triple neurokinin-receptor antagonist CS-003 inhibits neurokinin A-induced bronch...
Scientific journals : Article
Human health sciences : Cardiovascular & respiratory systems
Human health sciences : Pharmacy, pharmacology & toxicology
The triple neurokinin-receptor antagonist CS-003 inhibits neurokinin A-induced bronchoconstriction in patients with asthma
Schelfhout, V. [> > > >]
Louis, Renaud mailto [Université de Liège - ULiège > Département des sciences cliniques > Pneumologie - Allergologie]
Lenz, W. [> > > >]
Heyman, R. [> > > >]
Pauwels, R. [> > > >]
Joos, G. [> > > >]
Pulmonary Pharmacology & therapeutics
Academic Press Ltd Elsevier Science Ltd
Yes (verified by ORBi)
[en] asthma ; neuropeptides ; neurokinin A ; bronchoconstriction ; tachykinin receptor antagonist
[en] Neurokinin A (NKA) causes bronchoconstriction in asthmatic patients. In vitro both NK1 and NK2 receptors can mediate airway contraction. Moreover in guinea pigs, NK3 receptors facilitate cholinergic neurotransmission. Dual tachykinin NK1/NK2 receptor antagonism results in prevention of NKA-induced bronchoconstriction. We have now examined the effect of a single dose of the triple tachykinin receptor antagonist CS-003 on NKA-induced bronchoconstriction in asthmatics. A double blind, crossover, placebo-controlled trial in 16 mild asthmatics was performed. One single dose of CS-003 (200 mg, solution in distilled water) or matched placebo was given orally on the assessment days. NKA-provocation tests were performed pre-dose and 1, 8 and 24h after dosing. There was a significant shift to the right of the dose-response curve at 1 and 8 h after intake of CS-003. PC20 was not reached in 12/16 patients at 1 h post-dose and in 5/16 patients at 8h post-dose. This did not occur under placebo treatment. A single dose of 200 mg CS-003 protected significantly against NKA-induced bronchoconstriction at 1 and 8 h post-dose in mild asthmatics. (c) 2005 Elsevier Ltd. All rights reserved.

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