Universidad Complutense de Madrid
E-Prints Complutense

Specificity and nanomolar potency of melatonin on G-protein coupled melatonin MT1 and MT2 receptors expressed in HEK-293T human embryo kidney cells

Impacto

Downloads

Downloads per month over past year

Rivas Santisteban, Rafael and Reyes Resina, Irene and Raich, Iu and Pintor, Jesús and Alkozi, Hanan Awad and Navarro Brugal, Gemma and Franco Fernández, Rafael (2019) Specificity and nanomolar potency of melatonin on G-protein coupled melatonin MT1 and MT2 receptors expressed in HEK-293T human embryo kidney cells. Melatonin Research, 2 (4). pp. 121-131. ISSN 2641-0281

[img]
Preview
PDF
Creative Commons Attribution.

524kB

Official URL: https://doi.org/10.32794/mr11250044




Abstract

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.


Item Type:Article
Additional Information:

Received: October 6, 2019; Accepted: December 11, 2019

Uncontrolled Keywords:Melatonin receptor, Sleep, cAMP, Signal transduction, Binding, Pharmacokinetics
Subjects:Sciences > Chemistry > Biochemistry
Medical sciences > Biology > Cytology
ID Code:59716
Deposited On:25 Mar 2020 10:49
Last Modified:25 Mar 2020 10:49

Origin of downloads

Repository Staff Only: item control page