RESUMEN
We designed and synthesized novel δ opioid receptor (DOR) agonists 3a-i with an azatricyclodecane skeleton, which was a novel structural class of DOR agonists. Among them, 3b exhibited high values of binding affinity and potent agonistic activity for the DOR that were approximately equivalent to those of 2 which bore an oxazatricyclodecane skeleton. In vitro assays using the blood-brain barrier (BBB) permeability test kit supported the idea that 3b achieved an excellent BBB permeability by converting an oxygen atom of 2 to a carbon atom (methylene group) in the core skeleton. As a result, 3b showed potent antinociceptive effects.
Asunto(s)
Analgésicos Opioides/farmacología , Analgésicos Opioides/farmacocinética , Barrera Hematoencefálica/metabolismo , Ciclodecanos/farmacología , Ciclodecanos/farmacocinética , Receptores Opioides delta/agonistas , Administración Cutánea , Analgésicos Opioides/síntesis química , Analgésicos Opioides/química , Animales , Ciclodecanos/síntesis química , Ciclodecanos/química , Diseño de Fármacos , Humanos , Ratones , Receptores Opioides delta/metabolismoRESUMEN
A toxicologic and dermatologic review of tricyclo[5.2.1.02,6]dec-4-en-8-yl acetate when used as a fragrance ingredient is presented.
Asunto(s)
Acetatos/química , Ciclodecanos/química , Perfumes/química , Acetatos/farmacocinética , Ciclodecanos/farmacocinética , Humanos , Perfumes/farmacocinética , Piel/efectos de los fármacos , Piel/metabolismoRESUMEN
A toxicologic and dermatologic review of 1,7,7-trimethylbicyclo[4.4.0]dec-3-yl acetate when used as a fragrance ingredient is presented.
Asunto(s)
Acetatos/química , Acetatos/toxicidad , Perfumes/química , Perfumes/toxicidad , Acetatos/farmacocinética , Animales , Compuestos Bicíclicos con Puentes/química , Compuestos Bicíclicos con Puentes/farmacocinética , Compuestos Bicíclicos con Puentes/toxicidad , Ciclodecanos/química , Ciclodecanos/farmacocinética , Ciclodecanos/toxicidad , Humanos , Perfumes/farmacocinéticaRESUMEN
A toxicologic and dermatologic review of tricyclodecanyl acetate when used as a fragrance ingredient is presented.
Asunto(s)
Acetatos/química , Acetatos/toxicidad , Perfumes/química , Perfumes/toxicidad , Acetatos/farmacocinética , Animales , Ciclodecanos/química , Ciclodecanos/farmacocinética , Ciclodecanos/toxicidad , Humanos , Perfumes/farmacocinética , Piel/efectos de los fármacos , Piel/metabolismoRESUMEN
A toxicologic and dermatologic review of tricyclodecenyl acetate when used as a fragrance ingredient is presented.