46 research outputs found
Panspermia, Past and Present: Astrophysical and Biophysical Conditions for the Dissemination of Life in Space
Astronomically, there are viable mechanisms for distributing organic material
throughout the Milky Way. Biologically, the destructive effects of ultraviolet
light and cosmic rays means that the majority of organisms arrive broken and
dead on a new world. The likelihood of conventional forms of panspermia must
therefore be considered low. However, the information content of dam-aged
biological molecules might serve to seed new life (necropanspermia).Comment: Accepted for publication in Space Science Review
Twenty-six years of HIV science: an overview of anti-HIV drugs metabolism
From the identification of HIV as the agent causing AIDS, to the development of effective antiretroviral drugs, the scientific achievements in HIV research over the past twenty-six years have been formidable. Currently, there are twenty-five anti-HIV compounds which have been formally approved for clinical use in the treatment of AIDS. These compounds fall into six categories: nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), cell entry inhibitors or fusion inhibitors (FIs), co-receptor inhibitors (CRIs), and integrase inhibitors (INIs). Metabolism by the host organism is one of the most important determinants of the pharmacokinetic profile of a drug. Formation of active or toxic metabolites will also have an impact on the pharmacological and toxicological outcomes. Therefore, it is widely recognized that metabolism studies of a new chemical entity need to be addressed early in the drug discovery process. This paper describes an overview of the metabolism of currently available anti-HIV drugs.Da identificação do HIV como o agente causador da AIDS, ao desenvolvimento de fĂĄrmacos antirretrovirais eficazes, os avanços cientĂficos na pesquisa sobre o HIV nos Ășltimos vinte e seis anos foram marcantes. Atualmente, existem vinte e cinco fĂĄrmacos anti-HIV formalmente aprovados pelo FDA para utilização clĂnica no tratamento da AIDS. Estes compostos sĂŁo divididos em seis classes: inibidores nucleosĂdeos de transcriptase reversa (INTR), inibidores nucleotĂdeos de transcriptase reversa (INtTR), inibidores nĂŁo-nucleosĂdeos de transcriptase reversa (INNTR), inibidores de protease (IP), inibidores da entrada celular ou inibidores de fusĂŁo (IF), inibidores de co-receptores (ICR) e inibidores de integrase (INI). O metabolismo consiste em um dos maiores determinantes do perfil farmacocinĂ©tico de um fĂĄrmaco. A formação de metabĂłlitos ativos ou tĂłxicos terĂĄ impacto nas respostas farmacolĂłgicas ou toxicolĂłgicas do fĂĄrmaco. Portanto, Ă© amplamente reconhecido que estudos do metabolismo de uma nova entidade quĂmica devem ser realizados durante as fases iniciais do processo de desenvolvimento de fĂĄrmacos. Este artigo descreve uma abordagem do metabolismo dos fĂĄrmacos anti-HIV atualmente disponĂveis na terapĂȘutica
Modifications de lâactivitĂ© Ă©lectrique cĂ©rĂ©brale spontanĂ©e et Ă©voquĂ©e chez le lapin adulte soumis Ă une irradiation Îł globale
Lâirradiation Îł globale comprise entre 150 et 850 rads (dĂ©bit de 14 rad.min-1) entraĂźne chez le lapin adulte muni dâĂ©lectrodes chroniquement implantĂ©es des modifications immĂ©diates et retardĂ©es du comportement, de la vigilance et des activitĂ©s Ă©lectriques cĂ©rĂ©brales spontanĂ©es et Ă©voquĂ©es. Les techniques electrophysiologiques dâenregistrement polygraphique et les mĂ©thodes de traitement du signal permettent dâĂ©tablir que ces altĂ©rations sont reliĂ©es Ă la dose absorbĂ©e. La dose-seuil sâaccompagnant de modifications transitoires de la vigilance serait comprise entre 50 et 100 rads ; au-dessous de cette gamme de dose, lâirradiation agirait, Ă lâexclusion dâĂ©ventuelles modifications du comportement, comme une stimulation, qui ne deviendrait nociceptive que pour des doses plus Ă©levĂ©es