TY - JOUR
T1 - Histamine H3 receptor as a potential target for cognitive symptoms in neuropsychiatric diseases
AU - Sadek, Bassem
AU - Saad, Ali
AU - Sadeq, Adel
AU - Jalal, Fakhreya
AU - Stark, Holger
N1 - Publisher Copyright:
© 2016 Elsevier B.V.
PY - 2016/10/1
Y1 - 2016/10/1
N2 - The potential contributions of the brain histaminergic system in neurodegenerative diseases, and the possiblity of histamine-targeting treatments is attracting considerable interests. The histamine H3 receptor (H3R) is expressed mainly in the central nervous system, and is, consequently, an attractive pharmacological target. Although recently described clinical trials have been disappointing in attention deficit hyperactivity disorder (ADHD) and schizophrenia (SCH), numerous H3R antagonists, including pitolisant, demonstrate potential in the treatment of narcolepsy, excessive daytime sleepiness associated with cognitive impairment, epilepsy, and Alzheimer's disease (AD). This review focuses on the recent preclinical as well as clinical results that support the relevance of H3R antagonists for the treatment of cognitive symptoms in neuropsychiatric diseases, namely AD, epilepsy and SCH. The review summarizes the role of histaminergic neurotransmission with focus on these brain disorders, as well as the effects of numerous H3R antagonists on animal models and humans.
AB - The potential contributions of the brain histaminergic system in neurodegenerative diseases, and the possiblity of histamine-targeting treatments is attracting considerable interests. The histamine H3 receptor (H3R) is expressed mainly in the central nervous system, and is, consequently, an attractive pharmacological target. Although recently described clinical trials have been disappointing in attention deficit hyperactivity disorder (ADHD) and schizophrenia (SCH), numerous H3R antagonists, including pitolisant, demonstrate potential in the treatment of narcolepsy, excessive daytime sleepiness associated with cognitive impairment, epilepsy, and Alzheimer's disease (AD). This review focuses on the recent preclinical as well as clinical results that support the relevance of H3R antagonists for the treatment of cognitive symptoms in neuropsychiatric diseases, namely AD, epilepsy and SCH. The review summarizes the role of histaminergic neurotransmission with focus on these brain disorders, as well as the effects of numerous H3R antagonists on animal models and humans.
KW - Brain histamine receptors
KW - Cognitive symptoms
KW - H3R Antagonists
KW - Histamine
KW - Neuropsychiatric diseases
UR - http://www.scopus.com/inward/record.url?scp=84978737339&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84978737339&partnerID=8YFLogxK
U2 - 10.1016/j.bbr.2016.06.051
DO - 10.1016/j.bbr.2016.06.051
M3 - Review article
C2 - 27363923
AN - SCOPUS:84978737339
SN - 0166-4328
VL - 312
SP - 415
EP - 430
JO - Behavioural Brain Research
JF - Behavioural Brain Research
ER -