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).

Overview

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Free fatty acid receptors (FFA, nomenclature as agreed by NC-IUPHAR Subcommittee on free fatty acid receptors, [5,29]) 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 [2,10,12] and FFA4 receptors [6,9,20], while short chain fatty acids (C2 (acetic acid), C3 (propanoic acid), C4 (butyric acid) and C5 (pentanoic acid)) activate FFA2 [3,14,19] and FFA3 [3,14] receptors. In addition, thiazolidinedione PPARγ agonists such as rosiglitazone activate FFA1 (pEC50 5.2; [13,26,28]) and small molecule allosteric modulators, such as 4-CMTB, have recently been characterised for FFA2 [8,15,27].

Receptors

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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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Free fatty acid receptors. Accessed on 28/08/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=24.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors. Br J Pharmacol. 170: 1459–1581.