-transparent.png){kind=logo}
The synthesis of unsymmetrical naphth[2,3-d]imidazolium and bridged naphth[2,3-d]imidazolium derivatives and their substance P (SP) antagonist activity are described. All compounds were evaluated for their ability to displace SP from neurokinin-1 (NK-1) receptor sites using standard receptor binding methodology (rat forebrain membrane). 1,3-Diethyl-2-[3-(1,3-dihydro-1,3,3-timethyl-2H-indol-2-ylidene) -1-propenyl]-1H-naphth[2,3-d]imidazolium chloride (7a), a representative compound in this series, was further evaluated for SP antagonist activity in a guinea pig ileum contractility assay. In vivo SP antagonist activity of 7a was demonstrated using SP-induced salivation and paw edema models performed in rats.
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
November 2012,
Bioorganic & medicinal chemistry,
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
August 1995,
Journal of medicinal chemistry,
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
July 1980,
Biochemical and biophysical research communications,
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
August 1993,
Tanpakushitsu kakusan koso. Protein, nucleic acid, enzyme,
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
May 1989,
International journal of peptide and protein research,
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
December 1997,
Yao xue xue bao = Acta pharmaceutica Sinica,
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
October 1988,
Biochimica et biophysica acta,
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
December 1989,
Archiv der Pharmazie,
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
May 1983,
Il Farmaco; edizione scientifica,
K B Lawrence, and
B R Venepalli, and
K C Appell, and
R Goswami, and
M E Logan, and
B E Tomczuk, and
J M Yanni
July 1992,
European journal of pharmacology,
