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Loratadine analogues as MAGL inhibitors.
Patel, Jayendra Z; Ahenkorah, Stephen; Vaara, Miia; Staszewski, Marek; Adams, Yahaya; Laitinen, Tuomo; Navia-Paldanius, Dina; Parkkari, Teija; Savinainen, Juha R; Walczynski, Krzysztof; Laitinen, Jarmo T; Nevalainen, Tapio J.
Afiliação
  • Patel JZ; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland. Electronic address: jayendra.patel@uef.fi.
  • Ahenkorah S; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland.
  • Vaara M; School of Medicine, Institute of Biomedicine/Physiology, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland.
  • Staszewski M; Department of Synthesis and Technology of Drugs, Faculty of Pharmacy, Medical University of Lodz, 90-151 Lodz, Poland.
  • Adams Y; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland.
  • Laitinen T; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland.
  • Navia-Paldanius D; School of Medicine, Institute of Biomedicine/Physiology, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland.
  • Parkkari T; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland.
  • Savinainen JR; School of Medicine, Institute of Biomedicine/Physiology, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland.
  • Walczynski K; Department of Synthesis and Technology of Drugs, Faculty of Pharmacy, Medical University of Lodz, 90-151 Lodz, Poland.
  • Laitinen JT; School of Medicine, Institute of Biomedicine/Physiology, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland.
  • Nevalainen TJ; School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland.
Bioorg Med Chem Lett ; 25(7): 1436-42, 2015 Apr 01.
Article em En | MEDLINE | ID: mdl-25752982
ABSTRACT
Compound 12a (JZP-361) acted as a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46 nM), and was found to have almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50=7.24 µM) and 35-fold higher selectivity over human α/ß-hydrolase-6 (hABHD6, IC50=1.79 µM). Additionally, compound 12a retained H1 antagonistic affinity (pA2=6.81) but did not show cannabinoid receptor activity, when tested at concentrations ⩽ 10 µM. Hence, compound 12a represents a novel dual-acting pharmacological tool possessing both MAGL-inhibitory and antihistaminergic activities.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Loratadina / Inibidores Enzimáticos / Monoacilglicerol Lipases Limite: Humans Idioma: En Ano de publicação: 2015 Tipo de documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Loratadina / Inibidores Enzimáticos / Monoacilglicerol Lipases Limite: Humans Idioma: En Ano de publicação: 2015 Tipo de documento: Article