- Design and Synthesis of Highly Potent and Specific ABHD6 Inhibitors
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Fine-tuning than complete disruption of 2-arachidonoylglycerol (2-AG) metabolism in the brain represents a promising pharmacological approach to limit potential untoward effects associated with complete blockade of monoacylglycerol lipase (MGL), the prima
- Chandrashekhar, Honrao,Farah, Shrouq I.,Lamani, Manjunath,Makriyannis, Alexandros,Malamas, Michael S.,Miyabe, Christina Yume,Mohammad, Khadijah A.,Rajarshi, Girija,Wood, JodiAnne,Wu, Simiao,Zvonok, Nikolai
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supporting information
(2021/09/08)
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- Synthesis and biological evaluation of new N-substituted 4-(arylmethoxy)piperidines as dopamine transporter inhibitors
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The library of new N-substituted 4-(arylmethoxy)piperidines as dopamine transporter inhibitors was designed and synthesized. H-Bond donors in piperidine ring were found to be important for reduced locomotor activity in mice. 4-[Bis(4-fluorophenyl)methoxy]piperidine has IC50 17.0 ± 1.0 nm for dopamine transporter and locomotor activity, which is lower than that for cocaine.
- Lapa, Gennady B.,Lapa, Alla A.
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p. 203 - 205
(2019/04/25)
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- Vascular effects of diphenylmethoxypiperidine-derived dopamine uptake inhibitors
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Vascular effects of 4-aryl methoxypiperidinol compounds previously shown to share with cocaine the ability to inhibit the dopamine transporter are described. All the compounds tested inhibit KCl-induced and noradrenaline- dependent contractions in mesente
- Pulgar, Victor M.,Keith Harp, Jill
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p. 2429 - 2432
(2014/05/20)
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- Synthesis of eosinophil infiltration inhibitors with antihistaminic activity.
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A series of [1, 2, 4]triazolo[1, 5-b]pyridazines (5) and imidazo[1, 2-b]pyridazines (6) having cyclic amines was synthesized and evaluated for antihistaminic activity and inhibitory effect on eosinophil infiltration. When a piperidine or a piperazine containing a benzhydryl group and a suitable spacer was incorporated at the 6-position, the fused pyridazines were found to exhibit both antihistaminic activity and an inhibitory effect on eosinophil chemotaxis. Above all, 6a showed potent antihistaminic activity, but little blockade of central H(1) receptors in contrast with its complete blockade of peripheral H(1) receptors as determined by an ex vivo binding assay. Furthermore, 6a inhibited eosinophil infiltration of the skin caused by a topical antigen challenge in sensitized guinea pigs, while an antihistamine terfenadine was not effective. After the pharmacokinetic study, 6a was found to be rapidly hydrolyzed to 6o, which was also orally active. Compound 6o, 2-[6-[[3-[4-(diphenylmethoxy)piperidino]propyl]amino]imidazo[1, 2-b]pyridazin-2-yl]-2-methylpropionic acid dihydrate (TAK-427), having both antihistaminic and antiinflammatory activity, is currently undergoing clinical trials as a therapeutic agent for atopic dermatitis and allergic rhinitis.
- Gyoten, Michiyo,Nagaya, Hideaki,Fukuda, Shigeru,Ashida, Yasuko,Kawano, Yasuhiko
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p. 122 - 133
(2007/10/03)
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