3839-20-1Relevant articles and documents
Discovery of novel, orally active dual NK1/NK2 antagonists
Bernstein, Peter R.,Aharony, David,Albert, Jeffrey S.,Andisik, Donald,Barthlow, Herbert G.,Bialecki, Russell,Davenport, Timothy,Dedinas, Robert F.,Dembofsky, Bruce T.,Koether, Gerard,Kosmider, Benedict J.,Kirkland, Karin,Ohnmacht, Cyrus J.,Potts, William,Rumsey, William L.,Shen, Lihong,Shenvi, Ashok,Sherwood, Scott,Stollman, David,Russell, Keith
, p. 2769 - 2773 (2007/10/03)
Exploration of the SAR around selective NK2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK1 and NK2 antagonists. ZD6021 inhibited binding of [3H]-NKA or [3H]-SP to human NK1 and NK2 receptors, with high-affinity (Ki=0.12 and 0.62 nM, respectively). In functional assays ZD6021 had, at 10-7 M, in human pulmonary artery pKB=8.9 and in human bronchus pKB=7.3, for NK1 and NK2, respectively. Oral administration of ZD6021 to guinea pigs dose-dependently attenuated ASMSP induced extravasation of plasma proteins, ED50=0.5 mg/kg, and NK2 mediated bronchoconstriction, ED50=13 mg/kg.
SELECTIVE HYDROLYSIS OF NITRILES UNDER MILD CONDITIONS BY AN ENZYME
Cohen, Mark A.,Sawden, Janette,Turner, Nicholas J.
, p. 7223 - 7226 (2007/10/02)
A wide range of aromatic/aliphatic nitriles and dinitriles have been selcetively hydrolysed using a commercially available enzyme preparation from a Rhodococcuc sp.
