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Título

Neurogenic potential assessment and pharmacological characterization of 6-Methoxy-1,2,3,4-tetrahydro-β-carboline (Pinoline) and Melatonin-Pinoline Hybrids

AutorFuente Revenga, Mario de la; Pérez, Concepción; Morales-García, José A. ; Alonso-Gil, Sandra ; Pérez Castillo, Ana ; Yáñez, Matilde; Rodríguez-Franco, María Isabel
Palabras claveMonoamine oxidases
Antioxidants
Melatonergic receptors
Serotonergic receptors
Neurogenesis
Melatonin
Pinoline
Fecha de publicación2015
EditorAmerican Chemical Society
CitaciónACS Chemical Neuroscience 6(5): 800-810 (2015)
Resumen6-Methoxy-1,2,3,4-tetrahydro-β-carboline (pinoline) and N-acetyl-5-methoxytryptamine (melatonin) are both structurally related to 5-hydroxytryptamine (serotonin). Here we describe the design, synthesis, and characterization of a series of melatonin rigid analogues resulting from the hybridization of both pinoline and melatonin structures. The pharmacological evaluation of melatonin-pinoline hybrids comprises serotonergic and melatonergic receptors, metabolic enzymes (monoamine oxidases), antioxidant potential, the in vitro blood-brain barrier permeability, and neurogenic studies. Pinoline at trace concentrations and 2-acetyl-6-methoxy-1,2,3,4-tetrahydro-β-carboline (2) were able to stimulate early neurogenesis and neuronal maturation in an in vitro model of neural stem cells isolated from the adult rat subventricular zone. Such effects are presumably mediated via serotonergic and melatonergic stimulation, respectively.
DescripciónThis work received the honour of being the Cover of the ACS Chemical Neuroscience in its issue of May 2015
Versión del editorhttp://dx.doi.org/10.1021/acschemneuro.5b00041
URIhttp://hdl.handle.net/10261/117673
DOI10.1021/acschemneuro.5b00041
Identificadoresdoi: 10.1021/acschemneuro.5b00041
issn: 1948-7193
e-issn: 1948-7193
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