Molecular pharmacology of the ovine melatonin receptor: comparison with recombinant human MT1 and MT2 receptors.
Biochem Pharmacol
; 67(4): 667-77, 2004 Feb 15.
Article
en En
| MEDLINE
| ID: mdl-14757166
ABSTRACT
The variations of the pharmacological properties of melatonin receptors between different mammalian species in transfected cell lines have been poorly investigated. In the present study, melatonin analogues have been used to characterize the pharmacology of the recombinant ovine melatonin receptor (oMT1) expressed in CHO cell lines and the native oMT1 from the pars tuberalis (PT). Studies with selective ligands on native and transfected oMT1 showed similar properties for binding affinities [r2(PT/CHO) = 0.85]. The affinities and the functional activities of these ligands were compared with the human receptors (hMT1 or hMT2) expressed in CHO cells as well. The oMT1 and hMT1 receptors had similar pharmacological profiles (r2=0.82). Nevertheless, some of the selective compounds at the human receptor presented a reduced affinity at the ovine receptor. Furthermore, some compounds showed marked different functional activities at oMT1 vs. hMT1 receptors. Our findings demonstrated differences in the pharmacological properties of melatonin receptors in ovine and human species.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Receptores de Melatonina
/
Receptor de Melatonina MT1
/
Receptor de Melatonina MT2
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Biochem Pharmacol
Año:
2004
Tipo del documento:
Article
País de afiliación:
Francia