From: Advances in clinical applications of kisspeptin-GnRH pathway in female reproduction
Kisspeptin receptor antagonists | Sequence | Affinity | Half-life (t½) | Potency (in vivo and in vitro) | BBB permeability | Related studies |
---|---|---|---|---|---|---|
P234 | (D-Ala)-Asn-Trp-Asn-Gly-Phe-Gly-(D-Trp)-Arg-Phe-NH2 | Reference | Unclear | 90% inhibition of KP10 activated signalings | Unclear | (Roseweir et al. 2009 [9]; Pineda et al. 2010 [70]; Albers-Wolthers et al. 2017 [106]) |
P271 | Arg-Arg-Met-Lys-Trp-Lys-Lys-Tyr-(D-Ala)-Asn-Trp-Asn-Gly-Phe-Gly-(D-Trp)-Arg-Phe-NH2 | Comparable with P234 | Unclear | Comparable with P234 | Probably Yes | (Pineda et al. 2010 [70]; Smith et al. 2011 [107]; Albers-Wolthers et al. 2017 [106]) |
Compound 15a | 2-Acylamino-4,6-diphenylpyridine | Comparable with P234 | Unclear | Lower than P234 | Probably Yes |