Involvement of enhanced neurokinin NK3 receptor expression in the severe asthma guinea pig model

O Mukaiyama, K Morimoto, E Nosaka… - European journal of …, 2004 - Elsevier
In this study, we investigated the involvement of neurokinin NK3 receptors in a severe
asthma model prepared by administering ovalbumin via inhalation three times to …

Effects of endogenous substance P expression on degranulation in RBL-2H3 cells

H Hu, R Zhang, X Fang, M Yu, S Yu, J Zhang… - Inflammation …, 2011 - Springer
Objective and design To determine whether RBL-2H3 cells have endogenous substance P
(SP) expression under immunoglobulin E (IgE)-activated and inactivated conditions, and to …

Synthesis and NK1/NK2 binding activities of a series of diacyl-substituted 2-arylpiperazines

DJ Blythin, X Chen, JJ Piwinski, NY Shih… - Bioorganic & medicinal …, 2002 - Elsevier
The synthesis and binding affinity for hNK1 and hNK2 receptors of a series of diacyl
substituted 2-aryl piperazines are described. SAR evaluation led to the racemic derivative …

Dual neurokinin NK1/NK2 antagonists: N-[(R, R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl) carbamoyl] allyl-N-methyl-3, 5-bis (trifluoromethyl) benzamides and 3-[N′-3 …

M Gerspacher, L La Vecchia, R Mah… - Bioorganic & medicinal …, 2001 - Elsevier
Based on the structure of N-[(R, R)-(E)-1-(4-chlorobenzyl)-3-(2-oxoazepan-3-yl) carbamoyl]
allyl-N-methyl-3, 5-bis (trifluoromethyl) benzamide (1), attempts to improve the NK2 affinity …

Dual neurokinin NK1/NK2 receptor antagonists

M Gerspacher, A Von Sprecher - Drugs of the Future, 1999 - access.portico.org
Neurokinins (NKs), also known as tachykinins (TKs), are members of a family of small
peptides sharing the common C-terminal amino acid sequence Phe-X-Gly-Leu-Met-NH2 (1 …

Greater involvement of neurokinins found in Guinea pig models of severe asthma compared with mild asthma

O Mukaiyama, K Morimoto, E Nosaka… - International archives of …, 2004 - karger.com
Background: Involvement of neurokinins in asthma has been previously pointed out by
several reports. However, the relationship between neurokinins and the severity of asthma …

N-[(R, R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-ylcarbamoyl)-allyl]-N-methyl-3, 5-bis-trifluoromethyl-benzamide: an orally active neurokinin NK1/NK2 antagonist

M Gerspacher, A von Sprecher, R Mah… - Bioorganic & medicinal …, 2000 - Elsevier
The stereoselective synthesis of N-[(R, R)-(E)-1-(4-chloro-benzyl)-3-(2-oxo-azepan-3-
ylcarbamoyl)-allyl]-N-methyl-3, 5-bis-trifluoromethyl-benzamide (4) and its NK1 and NK2 …

Importance of DNA-adduct formation and gene expression profiling of disease candidate genes in rats exposed to bitumen fumes

R Halter, T Hansen, A Seidel, C Ziemann… - Journal of occupational …, 2007 - Taylor & Francis
The equivocal experimental and epidemiological evidence of bitumen fumes and the
possible mechanisms of toxicity remain uncertain. This study therefore aimed at …

Novel pharmacological targets and progression of new antitussive drugs

RL McLeod, DB Tulshian, JA Hey - Expert Opinion on Therapeutic …, 2003 - Taylor & Francis
Cough is frequently associated with a wide array of respiratory infections, ailments and
disorders. Consequently, cough is the number one symptomatic reason why people visit …

Biphenyl derivatives as novel dual NK1/NK2-receptor antagonists

R Mah, M Gerspacher, A von Sprecher, S Stutz… - Bioorganic & medicinal …, 2002 - Elsevier
In a continuation of our efforts to simplifly the structure of our neurokinin antagonists, a series
of substituted biphenyl derivatives has been prepared. Several compounds exhibit potent …