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Table 3 Characteristics of kisspeptin receptor antagonists

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

(Kobayashi et al. 2010 [108, 109])