Tsegay Etsay Weldekidan, Demise Desalegn Getnet, Hailu Nigus Alemu, Gufue Zenawi Hagos
Department of Pharmacy, College of Medicine and Health Sciences, Adigrat University, Adigrat, Tigray, Ethiopia.
Department of Biomedical Science, College of Medicine and Health Sciences, Adigrat University, Adigrat, Tigray, Ethiopia.
Neuropsychiatr Dis Treat. 2020 Oct 28;16:2499-2509. doi: 10.2147/NDT.S263424. eCollection 2020.
Schizophrenia is a serious disease of the central nervous system that affects a person's ability to think, feel and behave clearly. Even though the pathophysiological hypothesis of the disease is not clearly understood, dysfunction of dopamine, glutamate, serotonin and other neurotransmitters is widely believed to be involved. Serotonin within the synaptic vesicles functions as neurotransmitter and neurohormone in regulation of emotion, learning, memory, hormone release, cognition and motor function. Dysfunction of normal brain activity of serotonin is associated with schizophrenia. The role of serotonin 6 and 7 receptors in schizophrenia, interaction with neurotransmitters and the effect of drugs on those receptors in schizophrenia are the goal of this review. The aim of this review was to provide information for researchers and other scholars to identify the possible intervention points in the management of schizophrenia. The serotonin 6 and 7 receptors are associated with schizophrenia via modulating cyclic adenosine monophosphate, regulation of Fyn kinase and induction of structural plasticity. The above modulatory effects affect cholinergic, dopaminergic, glutamatergic, adrenergic and GABAergic systems. Recently, diverse numbers of selective agonist and antagonist ligands were developed for both receptors. SGS-518, ABT-354, Lu AE58054, SB-742,457, S-518, AVN-211, AVN-322, SYN-114 and SYN-120 are serotonin 6 receptor antagonists and aripiprazole-controlled release serotonin 7 receptor agonists under clinical trial for schizophrenia. Thus, research on novel drugs that act on serotonin 6 and 7 receptors likely facilitates the intervention into schizophrenia patients seeking better quality of life in the future.
精神分裂症是一种严重的中枢神经系统疾病,会影响人的清晰思考、感受和行为能力。尽管该疾病的病理生理假说尚未完全明确,但人们普遍认为多巴胺、谷氨酸、血清素和其他神经递质的功能失调与之有关。突触小泡内的血清素作为神经递质和神经激素,参与调节情绪、学习、记忆、激素释放、认知和运动功能。血清素正常脑活动的功能失调与精神分裂症有关。本文综述的目的是探讨血清素6和7受体在精神分裂症中的作用、与神经递质的相互作用以及药物对这些受体的影响。本综述旨在为研究人员和其他学者提供信息,以确定精神分裂症治疗中可能的干预点。血清素6和7受体通过调节环磷酸腺苷、Fyn激酶的调节和诱导结构可塑性与精神分裂症相关。上述调节作用影响胆碱能、多巴胺能、谷氨酸能、肾上腺素能和GABA能系统。最近,针对这两种受体开发了多种选择性激动剂和拮抗剂配体。SGS-518、ABT-354、Lu AE58054、SB-742,457、S-518、AVN-211、AVN-322、SYN-114和SYN-120是血清素6受体拮抗剂,阿立哌唑控释血清素7受体激动剂正在进行精神分裂症的临床试验。因此,对作用于血清素6和7受体的新型药物的研究可能有助于未来对寻求更好生活质量的精神分裂症患者进行干预。