Table 2.
Affinities and potencies of relaxin family peptides for human relaxin family peptide receptors 1–4
H1 relaxin |
H2 relaxin |
H3 relaxin |
hINSL3 |
hINSL5 |
Porcine relaxin |
Rhesus monkey relaxin |
Rat relaxin |
|||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
B | F | B | F | B | F | B | F | B | F | B | F | B | F | B | F | |
RXFP1 | 8.84a | 9.10a | 9.35b | 10.60a | 7.48d | 7.72d | 5.80d | 5.40a | 8.56b | 9.09b | 9.39b | 9.76b | 7.27b | 7.70b | ||
10.21b | 9.57b | 8.01b | 8.19a | 5.97a | ||||||||||||
10.04d | 9.42c | 8.50a | 8.82g | |||||||||||||
9.70h | 9.21d | 8.70g | ||||||||||||||
10.00h | ||||||||||||||||
RXFP2 | 8.83a | 8.30b | 7.72b | 6.97a | >5a | 9.66a | 9.40a | 7.87b | 8.05b | 7.81b | 5.40b | No bindng | ||||
8.82h | 7.94a | 9.68b | 8.16b | |||||||||||||
9.07d | 8.04d | 9.72d | 9.24c | |||||||||||||
9.27b | 8.80h | 9.85h | 8.38d | |||||||||||||
9.80h | ||||||||||||||||
RXFP3 | 9.38e | 9.25a | 6.30h | Antag h | ||||||||||||
9.40h | 9.38g | |||||||||||||||
9.52g | 9.46f | |||||||||||||||
9.52h | ||||||||||||||||
RXFP4 | 8.84e | 8.96i | 8.82h | 8.92h | ||||||||||||
8.92i | 9.04g | |||||||||||||||
8.96g | ||||||||||||||||
9.00h |
Abbreviations: H1, human gene 1 relaxin; H3, human gene 2 relaxin; H3, human gene 3 relaxin; INSL, insulin-like peptide; RXFP, relaxin family peptide receptor.
Competition-binding studies (B) with RXFP1 and RXFP2 were conducted with [33P]-H2 relaxin (B33) and those with RXFP3 and RXFP4 with [125I]-H3 relaxin. Functional studies (F) with RXFP1 and RXFP2 examined cAMP accumulation and those with RXFP3 and RXFP4 examined inhibition of forskolin stimulated cAMP accumulation.
Bathgate et al. (2006) (pKi and pEC50 (cAMP)).
Halls et al. (2005) (pKi and pEC50 (cAMP)).
Halls et al. (2006) (pEC50 (cAMP)).
Sudo et al. (2003) (pIC50 and pEC50 (cAMP)).
Chen et al. (2005) (pIC50).
Liu et al. (2003) (pEC50 (cAMP inhib)).
Liu et al. (2005) (pKi and pEC50 (CRE reporter, β-gal)).
Liu et al. (2005) (pKi and pEC50 (cAMP). NB [125I]-INSL3 for RXFP2).
Liu et al. (2003) (pKi and pEC50 (cAMP)).