| Title : Loratadine analogues as MAGL inhibitors - Patel_2015_Bioorg.Med.Chem.Lett_25_1436 |
| Author(s) : Patel JZ , Ahenkorah S , Vaara M , Staszewski M , Adams Y , Laitinen T , Navia-Paldanius D , Parkkari T , Savinainen JR , Walczynski K , Laitinen JT , Nevalainen TJ |
| Ref : Bioorganic & Medicinal Chemistry Lett , 25 :1436 , 2015 |
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Abstract :
Compound 12a (JZP-361) acted as a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46nM), and was found to have almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50=7.24muM) and 35-fold higher selectivity over human alpha/beta-hydrolase-6 (hABHD6, IC50=1.79muM). Additionally, compound 12a retained H1 antagonistic affinity (pA2=6.81) but did not show cannabinoid receptor activity, when tested at concentrations 10muM. Hence, compound 12a represents a novel dual-acting pharmacological tool possessing both MAGL-inhibitory and antihistaminergic activities. |
| PubMedSearch : Patel_2015_Bioorg.Med.Chem.Lett_25_1436 |
| PubMedID: 25752982 |
Patel JZ, Ahenkorah S, Vaara M, Staszewski M, Adams Y, Laitinen T, Navia-Paldanius D, Parkkari T, Savinainen JR, Walczynski K, Laitinen JT, Nevalainen TJ (2015)
Loratadine analogues as MAGL inhibitors
Bioorganic & Medicinal Chemistry Lett
25 :1436
Patel JZ, Ahenkorah S, Vaara M, Staszewski M, Adams Y, Laitinen T, Navia-Paldanius D, Parkkari T, Savinainen JR, Walczynski K, Laitinen JT, Nevalainen TJ (2015)
Bioorganic & Medicinal Chemistry Lett
25 :1436