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. 2013 Dec 17;170(8):1459–1581. doi: 10.1111/bph.12445
Nomenclature RXFP1 receptor RXFP2 receptor RXFP3 receptor RXFP4 receptor
HGNC, UniProt RXFP1, Q9HBX9 RXFP2, Q8WXD0 RXFP3, Q9NSD7 RXFP4, Q8TDU9
Principal transduction Gs, GαoB, Gαι3 1590,1595,1599 Gs, GαoB 1590,1601 Gi/o 1606,1620 Gi/o 1604
Rank order of potency H2 relaxin > H3 relaxin >> INSL3 1618 INSL3 > H2 relaxin >> H3 relaxin 1601,1618 H3 relaxin > H3 relaxin (B chain) 1604 INSL5 = H3 relaxin > H3 relaxin (B chain) 1602,1603
Endogenous antagonists (pKi) – – INSL5 (pIC50 6.3) 1605 –
Selective antagonists (pKi) LGR7-truncate 1612, B-R13/17K H2 relaxin (pEC50 6.7) 1597, (des 1-8) A-chain INSL3 analogue 1586, INSL3 B-chain analogue 1587, INSL3 B chain dimer 1616, H3 relaxin analogue 3 1613, R3(BΔ23-27)R/I5 chimeric peptide (pIC50 9.2) 1600, R3-B1-22R (pIC50 7.4) 1596 R3(BΔ23-27)R/I5 chimeric peptide (pIC50 8.64) 1600
Radioligands (Kd) [125I]H2 relaxin (Agonist, Full agonist), [33P]H2 relaxin (Agonist, Full agonist) (5x10-10–2x10-10 M) 1591,1618, [125I]INSL3 (human) (Agonist, Full agonist) (1x10-10 M) 1608, [33P]H2 relaxin (Agonist, Full agonist) (1.06x10-9–6.3x10-10 M) 1591,1618, [125I]H3 relaxin (Agonist, Full agonist) (3x10-10 M) 1604, [125I]H3-B/INSL5 A chimera (Agonist) (5x10-10 M) 1602, [125I]H3 relaxin (Agonist, Full agonist) (2x10-9–2x10-10 M) 1603, [125I]H3-B/INSL5 A chimera (Agonist) (1.2x10-9 M) 1602,
Comment europium-labelled H2 relaxin is a fluorescent ligand for this receptor (Kd=0.5 nM) 1614. europium-labelled INSL3 is a fluorescent ligand for this receptor (Kd=1 nM) 1615. europium-labelled H3-B/INSL5 A chimera is a fluorescent ligand for this receptor (Kd=5 nM) 1596. europium-labelled H3-B/INSL5 A chimera is a fluorescent probe at this receptor (Kd=5 nM) 1596, europium-labelled mouse INSL5 is a fluorescent ligand at this receptor (Kd=5 nM) 1585.