RT Journal Article
T1 Specificity and nanomolar potency of melatonin on G-protein coupled melatonin MT1 and MT2 receptors expressed in HEK-293T human embryo kidney cells
A1 Rivas Santisteban, Rafael
A1 Reyes Resina, Irene
A1 Raich, Iu
A1 Pintor, Jesús
A1 Alkozi, Hanan Awad
A1 Navarro Brugal, Gemma
A1 Franco Fernández, Rafael
AB This is a pre-registered study, i.e. a study whose hypotheses and experiments designed to address these hypotheses have been deposited in a database before starting the experiments. The study aims at assessing the Gs versus Gi coupling and the potency of melatonin in the human version of melatonin MT1 and MT2 G-protein-coupled receptors expressed in HEK-293T cells. The results show that these receptors are Gi but not Gs coupled. By using a standard procedure of modulation of 0.5 µM forskolin-induced cAMP levels, it was found that the potency on MT2 receptor-mediated actions is in the low nanomolar range, but the potency on MT1 receptor is in the high nanomolar range.  The potency of melatonin to stimulate the MT2 receptor is similar to that of a selective agonist, N-[2-(2-methoxy-6H-isoindolo[2,1-a]indol-11-yl)ethyl]butanamide (IIK7). Overall, the data on the potency of melatonin on its receptors will provide a new look for melatonin research. It is important to consider this finding for appropriately addressing physiological or therapeutic effects based on melatonin potency. Thus, the low doses of melatonin used in the existing prolonged release preparations or in other supplements should be revisited.
PB San Antonio TX
SN 2641-0281
YR 2019
FD 2019-12-15
LK https://hdl.handle.net/20.500.14352/6113
UL https://hdl.handle.net/20.500.14352/6113
LA eng
NO Received: October 6, 2019; Accepted: December 11, 2019
DS Docta Complutense
RD 17 abr 2025