Publication: Cannabinoides en el tratamiento del glaucoma. Diseño y relación estructura-actividad
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2017-06
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Abstract
El glaucoma es una de las principales causas de ceguera a nivel mundial. La observación de que los fumadores de Cannabis sativa (Δ9 -THC) desarrollaban una reducción de la presión intraocular (PIO), sugirió el aislamiento de cannabinoides como posibilidad terapéutica en el tratamiento del glaucoma. El sistema cannabinoide endógeno (SEC), permitió conocer los ligandos endógenos (CB), y los receptores (CB1 y CB2) que activan para mediar sus acciones. Así, surgió la necesidad de obtener ligandos cannabinomiméticos sintéticos, en concreto con mayor afinidad CB1, ya que hay mayor expresión de estos receptores a nivel de la retina. El objetivo es conseguir dilucidar la estructura de agonistas CB1, con elevada biodisponibilidad, gran afinidad y selectividad, así como crear una síntesis adecuada para su obtención.
Glaucoma is one of the leading causes of blindness worldwide. The observation that smokers of Cannabis sativa (Δ 9 -THC) developed a reduction in intraocular pressure (IOP), suggested the isolation of cannabinoids as a therapeutic possibility in the treatment of glaucoma. The endogenous cannabinoid system (SEC), allowed us to know the endogenous ligands (CB), and the receptors (CB1 and CB2) that activate to mediate their actions. Thus, the need arose to obtain synthetic cannabinomimetic ligands, in particular with greater CB1 affinity, since there is a greater expression of these receptors at the level of the retina. The objective is to obtain CB1 agonists, with high bioavailability, high affinity and selectivity, create a useful pathway to get them synthesized.
Glaucoma is one of the leading causes of blindness worldwide. The observation that smokers of Cannabis sativa (Δ 9 -THC) developed a reduction in intraocular pressure (IOP), suggested the isolation of cannabinoids as a therapeutic possibility in the treatment of glaucoma. The endogenous cannabinoid system (SEC), allowed us to know the endogenous ligands (CB), and the receptors (CB1 and CB2) that activate to mediate their actions. Thus, the need arose to obtain synthetic cannabinomimetic ligands, in particular with greater CB1 affinity, since there is a greater expression of these receptors at the level of the retina. The objective is to obtain CB1 agonists, with high bioavailability, high affinity and selectivity, create a useful pathway to get them synthesized.