2026-06-27T23:51:49Zhttps://docta.ucm.es/rest/oai/request
oai:docta.ucm.es:20.500.14352/61132023-08-04T00:37:59Zcom_20.500.14352_14col_20.500.14352_15
Docta Complutense author Rivas Santisteban, Rafael author Reyes Resina, Irene author Raich, Iu author Pintor, Jesús author Alkozi, Hanan Awad author Navarro Brugal, Gemma author Franco Fernández, Rafael 2023-06-16T15:16:28Z 2023-06-16T15:16:28Z 2019-12-15 2641-0281 10.32794/mr11250044 https://hdl.handle.net/20.500.14352/6113 https://doi.org/10.32794/mr11250044 http://www.melatonin-research.net/index.php/MR/article/view/61 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. eng Atribución 3.0 España Specificity and nanomolar potency of melatonin on G-protein coupled melatonin MT1 and MT2 receptors expressed in HEK-293T human embryo kidney cells journal article URL https://docta.ucm.es/bitstreams/89ed4381-353c-44d9-bd3a-469fa4a94da0/download File MD5 04331c9d356f31057fd448b1bea276ec 524826 application/pdf Pintor-2019_nanomolar potency of melatonin.pdf URL https://docta.ucm.es/bitstreams/aca02b1c-e6a3-4029-86a5-17ee1fa7f8cf/download File MD5 f65cec9147217fa6d896d67ae74d8c39 37416 text/plain Pintor-2019_nanomolar potency of melatonin.pdf.txt