Reference

Influences of mizolastine on rat paw edema induced by arachidonic acid

Influences of mizolastine on rat paw edema induced by arachidonic acid. Fu, Meng; Zhang, Yanguo; Liu, Yufeng; Wang, Zhipeng; Zhang, Xin; Du, Junfeng (Xijing Hospital, The 4th Military Medical University, Xian 710032, Peop. Rep. China).Chemicals with cas numbers 108612-45-9 and 79794-75-5 also play role. Zhonghua Pifuke Zazhi, 36(10), 591-592 (Chinese) 2003 Zhongguo Yixue Kexueyuan Pifubing Yanjiuso. CODEN: CHFTAJ. ISSN: 0412-4030. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Study the anti-inflammatory properties of mizolastine and explore its possible mechanisms. Edema at hind-paw of rat was induced by a single injection of arachidonic acid (AA), each contg. 0.1 mL of prepd. AA (0.3%). The intensity of AA-induced reactions was expressed as an increasing of rat paw thickness, which was measured by micrometer. After the drugs (mizolastine, loratadine, cetirizine) were given orally sep., the inhibitory effects were detd. by the decreasing of edema intensity. Zileuton and mizolastine were given orally sep. and the inhibitory effects were compared subsequently. The intensity of AA-induced edema was significantly inhibited by mizolastine, but not by loratadine or cetirizine. There was no significant difference between mizolastine and zileuton in the inhibition of AA-induced edema. The results indicated that mizolastine possessed anti-inflammatory properties in vivo, which might be related to the inhibition of the 5-lipoxygenase pathway. .

Common Pharmacophores for Uncharged Human Ether-a-go-go-Related Gene (hERG) Blockers

All Rights Reserved.Some chemicals with cas registry numbers like 108612-45-9 and 155213-67-5 are also used. Common Pharmacophores for Uncharged Human Ether-a-go-go-Related Gene (hERG) Blockers. Aronov, Alex M. (Vertex Pharmaceuticals Inc., Cambridge, MA 02139-4242, USA). Journal of Medicinal Chemistry, 49(23), 6917-6921 (English) 2006 American Chemical Society. CODEN: JMCMAR. ISSN: 0022-2623. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) In silico approaches are widely used to predict human ether-a-go-go-related gene (hERG) channel blockade. Published pharmacophore models of hERG blockers typically contain a basic nitrogen center flanked by arom. or hydrophobic groups. However, hERG blockade has been obsd. in series lacking the basic nitrogen. By utilizing screening data for 194 potent uncharged hERG actives, we propose a pharmacophore for neutral hERG blockers, and provide guidance on eliminating hERG liability in an uncharged hERG active chem. series. .