Free fatty acid receptors

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).


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Free fatty acid receptors (FFA, nomenclature as agreed by the NC-IUPHAR Subcommittee on free fatty acid receptors [7,36]) are activated by free fatty acids. Long-chain saturated and unsaturated fatty acids (C14.0 (myristic acid), C16:0 (palmitic acid), C18:1 (oleic acid), C18:2 (linoleic acid), C18:3, (α-linolenic acid), C20:4 (arachidonic acid), C20:5,n-3 (EPA), C22:6,n-3 (docosahexaenoic acid)) activate FFA1 [2,13,16] and FFA4 receptors [8,12,25], while short chain fatty acids (C2 (acetic acid), C3 (propanoic acid), C4 (butyric acid) and C5 (pentanoic acid)) activate FFA2 [3,18,23] and FFA3 [3,18] receptors. In addition, thiazolidinedione PPARγ agonists such as rosiglitazone activate FFA1 (pEC50 5.2; [17,32,35]) and small molecule allosteric modulators, such as 4-CMTB, have recently been characterised for FFA2 [11,19,33].


FFA1 receptor Show summary » More detailed page

FFA2 receptor Show summary » More detailed page

FFA3 receptor Show summary » More detailed page

FFA4 receptor Show summary » More detailed page

GPR42 Show summary » More detailed page


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Further reading

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Graeme Milligan, Celia Briscoe, Andrew Brown, Nick Holliday, Stephen Jenkinson, Leigh Stoddart, Amy E. Monaghan. Free fatty acid receptors. Accessed on 22/10/2016. IUPHAR/BPS Guide to PHARMACOLOGY,

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Davenport AP, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors. Br J Pharmacol. 172: 5744-5869.