This letter describes the discovery and synthesis of a series of octahydropyrrolo[3,4-c]pyrrole based selective histamine hH4 receptor antagonists. The amidine compound 20 was found to be a potent and selective histamine H4 receptor antagonist with moderate clearance and a high volume of distribution.
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| http://dx.doi.org/10.1016/j.bmcl.2011.11.098 | DOI Listing |
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Cancer Med
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Medical Data Analytics Centre, The Chinese University of Hong Kong, Hong Kong SAR, China.
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J Prev Med Public Health
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Department of Preventive Medicine, Seoul National University College of Medicine, Seoul, Korea.
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Department of Pharmacology and Department of Pharmacy of the Second Affiliated Hospital, Key Laboratory of Medical Neurobiology of the Ministry of Health of China, School of Basic Medical Sciences, Zhejiang University School of Medicine, Hangzhou 310058, China. Electronic address:
Attention deficit hyperactivity disorder (ADHD), affecting 4% of the population, is characterized by inattention, hyperactivity, and impulsivity; however, its neurophysiological mechanisms remain unclear. Here, we discovered that deficiency of histamine H receptor (HR) in parvalbumin-positive neurons in substantia nigra pars recticulata (PV) attenuates PV neuronal activity and induces hyperactivity, impulsivity, and inattention in mice. Moreover, decreased HR expression was observed in PV in patients with ADHD symptoms and dopamine-transporter-deficient mice, whose behavioral phenotypes were alleviated by HR agonist treatment.
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View Article and Find Full Text PDFComparative analysis of adenosine 1 receptor expression and function in hippocampal and hypothalamic neurons.
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Medical Faculty and University Hospital, Institute of Neural and Sensory Physiology, Heinrich Heine University Düsseldorf, 40225, Düsseldorf, Germany.
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