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Agonistas e Antagonistas dos recetores H3: estado da arte e perspetivas de aplicação terapêutica
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A Histamina é uma amina biogénica que exerce um papel central como mediador em vários processos fisiopatológicos no nosso organismo. Para além de atuar como mediador inflamatório nos tecidos periféricos no qual interfere em processos de origem imunológica, esta amina também exerce sua ação a nível do sistema gastrointestinal e funciona como neurotransmissor no SNC.
O crescente conhecimento do sistema histaminérgico permitiu a sua categorização em quatro recetores distintos (H1, H2, H3 e H4), sendo que o constante aprofundamento das suas propriedades e funções constituiu a chave primordial para o desenvolvimento de novos compostos e para a descoberta de novas patologias a estes associados.
Os recetores H3 devido à sua localização e dupla funcionalidade no Sistema Nervoso Central (SNC), atuando como auto ou hetero-recetor, têm despoletado um interesse especial a nível terapêutico no mercado farmacêutico. O principal objetivo desta monografia é dar a conhecer as principais terapêuticas, mecanismos de ação associados aos fármacos com atividade agonista e antagonista H3R, principalmente a nível do SNC, e por último revelar as novas patologias a que este recetor tem sido associado.
Pode-se então concluir que os efeitos farmacológicos dos agonistas H3R foram evidenciados nas doenças gastrointestinais, nos processos inflamatórios (ex: enxaquecas, tosse, asma, alergias e rinites), nos distúrbios de sono (ex: insónia), na nocicepção, na isquemia do miocárdio. Em contrapartida a terapêutica com os antagonistas H3R abrangeu sobretudo patologias envolvidas no SNC nomeadamente, a doença de Alzheimer, a esquizofrenia, a epilepsia, a narcolepsia, o transtorno do défice de atenção na hiperatividade, a isquemia cerebral e por fim também doenças metabólicas (ex: obesidade).
No final desta monografia é descrito ainda em detalhe uma nova abordagem científica que veio propulsionar uma revolução no sector farmacêutico a nível farmacológico, denominando-se esta por polifarmacologia.
Histamine is one of the essential biogenic amines present in human body that has a crucial role as a mediator of a wide variety of physiological and pathological processes. Although histamine mediates inflammatory processes in peripheral tissues, this amine is also functionally involved in gastrointestinal system and works as a neurotransmitter in the brain. The increasing knowledge of histaminergic system allowed their classification in four different receptors (H1, H2, H3 e H4), and the steady improvement of its properties and functions constitute the primary key for developing new compounds and also for the discovery of new diseases. Due to the localization and the possibility of acting like an auto-receptor or hetero-receptor in the Central Nervous System (CNS), the H3 receptor has triggered a special interest in the pharmaceutical market, mainly in the pharmacology issue. Therefore, the main goal of this monography is try to describe and inform the major therapeutics and mechanisms of action associated to each agonists and antagonists H3R, especially in CNS, and finally reveal which new pathologies are under investigation. We can conclude that the pharmacological effects of agonists H3R has been focused on gastrointestinal diseases, on inflammatory processes (eg. headache, asthma, cough, allergies and rhinitis), on sleep disorders (eg. insomnia), on nociception and also on myocardial ischemia. On the other hand, the antagonists H3R therapy has been associated to CNS disorders such as Alzheimer’s disease, schizophrenia, epilepsy, narcolepsy, attention-deficit hyperactivity disease, cerebral ischemia and also to metabolic pathologies like obesity. At the end of this monography is also described in further detail a new scientific approach called polipharmacology, which in a recent future will lead to a pharmacological revolution on the pharmaceutical market.
Histamine is one of the essential biogenic amines present in human body that has a crucial role as a mediator of a wide variety of physiological and pathological processes. Although histamine mediates inflammatory processes in peripheral tissues, this amine is also functionally involved in gastrointestinal system and works as a neurotransmitter in the brain. The increasing knowledge of histaminergic system allowed their classification in four different receptors (H1, H2, H3 e H4), and the steady improvement of its properties and functions constitute the primary key for developing new compounds and also for the discovery of new diseases. Due to the localization and the possibility of acting like an auto-receptor or hetero-receptor in the Central Nervous System (CNS), the H3 receptor has triggered a special interest in the pharmaceutical market, mainly in the pharmacology issue. Therefore, the main goal of this monography is try to describe and inform the major therapeutics and mechanisms of action associated to each agonists and antagonists H3R, especially in CNS, and finally reveal which new pathologies are under investigation. We can conclude that the pharmacological effects of agonists H3R has been focused on gastrointestinal diseases, on inflammatory processes (eg. headache, asthma, cough, allergies and rhinitis), on sleep disorders (eg. insomnia), on nociception and also on myocardial ischemia. On the other hand, the antagonists H3R therapy has been associated to CNS disorders such as Alzheimer’s disease, schizophrenia, epilepsy, narcolepsy, attention-deficit hyperactivity disease, cerebral ischemia and also to metabolic pathologies like obesity. At the end of this monography is also described in further detail a new scientific approach called polipharmacology, which in a recent future will lead to a pharmacological revolution on the pharmaceutical market.
Descrição
Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, Universidade de Lisboa, Faculdade de Farmácia, 2016
Palavras-chave
Agonistas H3R Antagonistas H3R Neurotransmissores Terapêutica Sistema Nervoso Central (SNC) Polifarmacologia Mestrado Integrado - 2016