Nomenclature | GnRH1 receptor | GnRH2 receptor |
HGNC, UniProt | GNRHR, P30968 | GNRHR2, Q96P88 |
Rank order of potency | GnRH I (GNRH1, P01148) >GnRH II (GNRH2, O43555) [1284] | GnRH II (GNRH2, O43555) >GnRH I (GNRH1, P01148) (Monkey) [1282] |
Endogenous agonists | – | GnRH II (GNRH2, O43555) (pIC50 9) [1282] – Monkey, GnRH I (GNRH1, P01148) (pIC50 7.4) [1282] – Monkey |
Selective agonists | triptorelin (pK i 9.3–9.5) [112], leuprolide (pK i 8.5–9.1) [1807], buserelin, goserelin, histrelin, nafarelin | – |
Antagonists | iturelix (pK i 9.5) [1591] | – |
Selective antagonists | cetrorelix (pK i 9.3–10) [113, 114, 1807], abarelix (pK i 9.1–9.5) [1807], degarelix (pK i 8.8) [1938], ganirelix | trptorelix‐1 [1183] – Monkey |
Labelled ligands | [125I]buserelin (Agonist) (pK d 7.4) [1024] – Rat, [125I]GnRH I (human, mouse, rat) (Agonist) | – |
Comments | – | Probable transcribed pseudogene in man [1284]. |