{"id":29389,"date":"2018-03-09T09:22:29","date_gmt":"2018-03-09T09:22:29","guid":{"rendered":"https:\/\/www.deberes.net\/tesis\/sin-categoria\/investigacion-y-desarrollo-de-abaperidona-nuevo-antipsicotico-5ht2a-d2-y-alfa1-adrenergico-modelos-in-vitro-e-in-vivo-predictivos-de-eficacia-y-efectos-adversos\/"},"modified":"2018-03-09T09:22:29","modified_gmt":"2018-03-09T09:22:29","slug":"investigacion-y-desarrollo-de-abaperidona-nuevo-antipsicotico-5ht2a-d2-y-alfa1-adrenergico-modelos-in-vitro-e-in-vivo-predictivos-de-eficacia-y-efectos-adversos","status":"publish","type":"post","link":"https:\/\/www.deberes.net\/tesis\/farmacos-psicotropicos\/investigacion-y-desarrollo-de-abaperidona-nuevo-antipsicotico-5ht2a-d2-y-alfa1-adrenergico-modelos-in-vitro-e-in-vivo-predictivos-de-eficacia-y-efectos-adversos\/","title":{"rendered":"Investigaci\u00f3n y desarrollo de abaperidona, nuevo antipsic\u00f3tico 5ht2a\/d2 y alfa1-adren\u00e9rgico. modelos in vitro e in vivo predictivos de eficacia y efectos adversos"},"content":{"rendered":"<h2>Tesis doctoral de <strong> Marta Princep Mota <\/strong><\/h2>\n<p>Abaperidona, es una entidad qu\u00edmica investigada y desarrollada como potencial antipsic\u00f3tico at\u00edpico, con favorable perfil 5ht2\/d2 y elevada afinidad por el receptor alfa1-adren\u00e9rgico. Abaperidona tambi\u00e9n mostr\u00f3 afinidad en rango nm por otros receptores centrales (d3, d1,5ht2c, 5ht1a y h1) y escasa afinidad (superior a 100 nm) por los receptores muscar\u00ednicos. Este compuesto se evalu\u00f3 mediante pruebas predictivas tanto de eficacia antipsic\u00f3tica como de efectos extrapiramidales (eps).  abaperidona inhibi\u00f3 de manera dosis dependiente las hiperactividades inducidas por agonistas dopamin\u00e9rgicos en rat\u00f3n y revirti\u00f3 los d\u00e9ficits sensorimotores (ppi) inducidos por apomorfina en ratas. Adem\u00e1s, abaperidona demostr\u00f3 elevada afinidad por el receptor 5ht2a en el c\u00f3rtex y bloque\u00f3 potentemente las sacudidas de cabeza inducidas por doi [1-(2,5-dimetoxi-4-iodofenil)-2-aminopropano, agonista preferente 5ht2a] en rat\u00f3n, as\u00ed como tendencia a revertir de manera dosis dependiente la hipolocomoci\u00f3n inducida por mcpp (1-(3-clorofenil)piperazina, agonista 5ht2c). Su potente antagonismo alfa1-adren\u00e9rgico se demostr\u00f3 en estudios funcionales en rata anestesiada y desmedulada y en la protecci\u00f3n a la letalidad inducida por noradrenalina, a dosis 5 veces inferiores a las necesarias para inducir el bloqueo de los receptores d2. Sin embargo, abaperidona \u00fanicamente induje eps a dosis entre 21 (estereotipias inducidas por agonista dopamin\u00e9rgicos) y 35 (catalepsia) veces superiores a las dosis predictivas de actividad antipsic\u00f3tica precl\u00ednica, y demostr\u00f3 menor regulaci\u00f3n ascendente del receptor d2 en el estriado que haloperidol y risperidona tras administraci\u00f3n prolongada. Adem\u00e1s, la inducci\u00f3n de prolactina debida a la administraci\u00f3n del compuesto fue significativamente menor que la inducida por haloperidol o risperidona. Abaperidona tambi\u00e9n demostr\u00f3 una potente acci\u00f3n moduladora del receptor nmda al inhibir la hiperactividad inducida por<\/p>\n<p>&nbsp;<\/p>\n<h3>Datos acad\u00e9micos de la tesis doctoral \u00ab<strong>Investigaci\u00f3n y desarrollo de abaperidona, nuevo antipsic\u00f3tico 5ht2a\/d2 y alfa1-adren\u00e9rgico. modelos in vitro e in vivo predictivos de eficacia y efectos adversos<\/strong>\u00ab<\/h3>\n<ul>\n<li><strong>T\u00edtulo de la tesis:<\/strong>\u00a0 Investigaci\u00f3n y desarrollo de abaperidona, nuevo antipsic\u00f3tico 5ht2a\/d2 y alfa1-adren\u00e9rgico. modelos in vitro e in vivo predictivos de eficacia y efectos adversos <\/li>\n<li><strong>Autor:<\/strong>\u00a0 Marta Princep Mota <\/li>\n<li><strong>Universidad:<\/strong>\u00a0 Barcelona<\/li>\n<li><strong>Fecha de lectura de la tesis:<\/strong>\u00a0 26\/03\/2004<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n<h3>Direcci\u00f3n y tribunal<\/h3>\n<ul>\n<li><strong>Director de la tesis<\/strong>\n<ul>\n<li>Antonio Guglietta<\/li>\n<\/ul>\n<\/li>\n<li><strong>Tribunal<\/strong>\n<ul>\n<li>Presidente del tribunal: miquel Llobera sande <\/li>\n<li>joaquin del Rio zambrana (vocal)<\/li>\n<li>Rafael Maldonado l\u00f3pez (vocal)<\/li>\n<li>daniel Palop palop (vocal)<\/li>\n<\/ul>\n<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Tesis doctoral de Marta Princep Mota Abaperidona, es una entidad qu\u00edmica investigada y desarrollada como potencial antipsic\u00f3tico at\u00edpico, con favorable [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"site-sidebar-layout":"default","site-content-layout":"","ast-site-content-layout":"","site-content-style":"default","site-sidebar-style":"default","ast-global-header-display":"","ast-banner-title-visibility":"","ast-main-header-display":"","ast-hfb-above-header-display":"","ast-hfb-below-header-display":"","ast-hfb-mobile-header-display":"","site-post-title":"","ast-breadcrumbs-content":"","ast-featured-img":"","footer-sml-layout":"","theme-transparent-header-meta":"","adv-header-id-meta":"","stick-header-meta":"","header-above-stick-meta":"","header-main-stick-meta":"","header-below-stick-meta":"","astra-migrate-meta-layouts":"default","ast-page-background-enabled":"default","ast-page-background-meta":{"desktop":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center 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