| Nomenclature | FFA1 receptor | FFA2 receptor |
| HGNC, UniProt | FFAR1, O14842 | FFAR2, O15552 |
| Endogenous agonists | docosahexaenoic acid [223, 872], α ‐linolenic acid [223, 872, 1043], oleic acid [223, 872, 1043], myristic acid [223, 872, 1043] | propanoic acid [231, 1117, 1465, 1741], acetic acid [231, 1117, 1465, 1741], butyric acid [231, 1117, 1465, 1741], trans‐2‐methylcrotonic acid [1741], 1‐methylcyclopropanecarboxylic acid [1741] |
| Selective agonists | AMG‐837 [1176], compound 4 [347], TUG‐770 [346], TUG‐905 [345], GW9508 (Partial agonist) [222], fasiglifam [935, 1434, 1862, 1985] | compound 1 [840] – Rat |
| Selective antagonists | GW1100 (pIC50 6) [222, 1875] | GLPG0974 (pIC50 8.1) [1423, 1584], CATPB (pIC50 6.5) [841] |
| Comments | Antagonist GW1100 is also an oxytocin receptor antagonist [222]. Fasiglifam, TUG‐770 and GW9508 are approximately 100 fold selective for FFA1 over FFA4 [222, 346, 1434]. AMG‐837 and the related analogue AM6331 have been suggested to have an allosteric mechanism of action at FFA1, with respect to the orthosteric fatty acid binding site [1176, 2153]. | – |
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