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. 2010 Dec;62(4):565–578. doi: 10.1124/pr.110.002774

TABLE 3.

Classification of the kisspeptin receptor

Previous names GPR54, AXOR12, hOT7T175
Structural information 7TM
    Human 398 aa (SwissProt Q969F8) chr. 19p13.3 (Entrez 84634)
    Rat 396 aa (SwissProt Q924U1) chr. 7q11 (Entrez 78976)
    Mouse 396 aa (SwissProt Q91V45) chr. 10C1 (Entrez 114229)
Functional assays CHO cells transfected with the kisspeptin receptor Hori et al., 2001
In vitro pharmacology using human isolated vessels Mead et al., 2007b
Endogenous agonists KP-54 (EC50 = 5.5 nM) Kotani et al., 2001
KP-54 (pEC50 = 8.9 nM) Mead et al., 2007b
Selective agonists 4-fluorobenzoyl-F-G-l-RW-NH2 (EC50 = 0.7 nM) Tomita et al., 2007
[dY]1KP-10 Curtis et al., 2010
Antagonists Peptide234 ac[(D)-A]NWNGFG[(D)-W]RF Roseweir et al., 2009
Antagonist potencies Peptide 234 (IC50 = 7.0 nM)
Radioligands 125I-Tyr45-KP-54 (KD = 0.1 nM) Ohtaki et al., 2001
125I-KP-14 (KD = 0.1 nM) Mead et al., 2007b
125I-KP-10 (KD = 1.9 nM) Kotani et al., 2001
Transduction mechanisms Coupled to Gαq/11 proteins Kotani et al., 2001; Muir et al., 2001; Becker et al., 2005
Receptor distribution
    Human RT-PCR showed highest expression of KISS1R mRNA in placenta, pituitary, spinal cord and pancreas. Kotani et al., 2001; Ohtaki et al., 2001.
Kisspeptin receptor protein expression detected in the cerebral cortex, thalamus, pons-medulla and cerebellum by immunohistochemistry. Muir et al., 2001
Radioligand binding and immunohistochemistry found expression in aorta, coronary artery and umbilical vein. Mead et al., 2007b
    Rat RT-PCR detected Kiss1r mRNA in cortex, frontal cortex and striatum and in ovary. Lee et al., 1999; Castellano et al., 2006
Kisspeptin-receptor immunoreactivity has been detected in the pituitary. Richard et al., 2008
    Mouse RT-PCR showed Kiss1r expression in heart and in brain and reproductive tissues (uterus, oviduct, and testis). Stafford et al., 2002; Funes et al., 2003
Tissue function Metastasis inhibitor, stimulator of LH release, inhibitor of trophoblast migration, vasoconstrictor of coronary artery, and umbilical vein. Ringel et al., 2002; Bilban et al., 2004; Irwig et al., 2004; Navarro et al., 2004a; Mead et al., 2007b

aa, amino acid(s); RT-PCR, reverse transcription-polymerase chain reaction.