Impact of FDA-Approved Drugs on the Prostaglandin Transporter OATP2A1/SLCO2A1 was written by Kamo, Shunsuke;Nakanishi, Takeo;Aotani, Rika;Nakamura, Yoshinobu;Gose, Tomoka;Tamai, Ikumi. And the article was included in Journal of Pharmaceutical Sciences in 2017.Electric Literature of C18H17NO5 This article mentions the following:
To understand interaction of drugs with the prostaglandin transporter OATP2A1/SLCO2A1 that regulates disposition of prostaglandins, we explored the impact of 636 drugs in an FDA-approved drug library on 6-carboxyfluorescein (6-CF) uptake by OATP2A1-expressing HEK293 cells (HEK/2A1). Fifty-one and 10 drugs were found to inhibit and enhance 6-CF uptake by more than 50%, resp. Effect of the 51 drugs on 6-CF uptake was pos. correlated with that on PGE2 uptake (r = 0.64, p < 0.001). Among those, 5 drugs not structurally related to prostaglandins, suramin, pranlukast, zafirlukast, olmesartan medoxomil, and losartan potassium, exhibited more than 90% PGE2 uptake inhibition. Inhibitory affinity of suramin to OATP2A1 was the highest (IC50,2A1 of 0.17 μM), and its IC50 values to MRP4-mediated PGE2 transport (IC50,MRP4) and PGE2 synthesis in human U-937 cells treated with phorbol 12-myristate 13-acetate (IC50,Syn) were 73.6 and 336.7 times higher than IC50,2A1, resp. Moreover, structure-activity relationship study in 29 nonsteroidal anti-inflammatory drugs contained in the library displayed inhibitory activities of anthranilic acid derivatives, but enhancing effects of propionic acid derivatives These results demonstrate that suramin is a potent selective inhibitor of OATP2A1, providing a comprehensive information about drugs in clin. use that interact with OATP2A1. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Electric Literature of C18H17NO5).
2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Electric Literature of C18H17NO5
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics