Results 51 to 60 of about 13,967 (254)
Histamine H3 Receptor Antagonists Go to Clinics
Biological and Pharmaceutical Bulletin, 2008 Within the recent years novel lead optimisations for histamine H(3) receptor antagonists made their way from bench to bedside. Structure-activity relationships, cross-affinities and side effects as well as pharmacokinetic profiling will be discussed on selected promising compound series.
Kerstin, Sander +2 more
openaire +3 more sources
Therapeutic Approach of Histamine H3 Receptors in Obesity [PDF]
Recent Patents on CNS Drug Discovery, 2007 Obesity is considered one of the risk factors for metabolic disorders. There is increasing evidence that obesity is under control of several cytokines and hormone in the brain. Brain histamine and H3 receptors are important factors for regulating obesity.
Takayuki, Masaki, Hironobu, Yoshimatsu
openaire +2 more sources
Transient changes in the limbic histaminergic system after systemic kainic acid-induced seizures
Neurobiology of Disease, 2005 Increased brain histamine is reported to protect against convulsions. We used systemic kainic acid (KA) administration to study possible changes of the histaminergic system in rat brain in status epilepticus (SE).
Minnamaija Lintunen +3 more
doaj +1 more source
Novel H3 receptor antagonists. Sulfonamide homologs of histamine
Bioorganic & Medicinal Chemistry Letters, 1998 Sulfonamides derived from 4(5)-(omega-aminoalkyl)-1H-imidazoles containing chain lengths of three- to five-carbons were synthesized. Good to moderate H3 receptor binding affinities were observed for several butyl and pentyl homologs, whereas binding affinities were considerably weaker in the propyl series.
Ronald Wolin +7 more
openalex +3 more sources
The Histamine H3 Receptor: Structure, Pharmacology, and Function [PDF]
Molecular Pharmacology, 2016 Among the four G protein-coupled receptors (H1-H4) identified as mediators of the biologic effects of histamine, the H3 receptor (H3R) is distinguished for its almost exclusive expression in the nervous system and the large variety of isoforms generated by alternative splicing of the corresponding mRNA.
Gustavo, Nieto-Alamilla +4 more
openaire +2 more sources
Journal of Pharmacological Sciences, 2008 The aim of this study was to investigate the effects of histamine H1 and H3 antagonists on learning and mnemonic dysfunction in mice. Two H1 antagonists, pyrilamine and clozapine, and the prototypic H3 antagonist thioperamide were used to study the role ...
Feiyong Jia +9 more
doaj +1 more source
Acta Psychiatrica Scandinavica, EarlyView.ABSTRACT Background Schizophrenia is characterized by positive, negative, and cognitive symptoms. Current pharmacological treatments often fail to address cognitive deficits. In this review of clinical trials, we aim to identify studies that explore neurobiological (non‐psychological) strategies to address Cognitive Impairment Associated with ...
Bahareh Peyrovian +3 more
wiley +1 more source
Frontiers in Neural Circuits, 2017 Histamine H3 receptors are autoreceptors that regulate histamine release from histaminergic neuronal terminals. The cerebral cortex, including the insular cortex (IC), expresses abundant H3 receptors; however, the functions and mechanisms of H3 receptors
Hiroki Takei +8 more
doaj +1 more source
Evaluation of preclinical antipsychotic models used to support first‐in‐human clinical trials
British Journal of Pharmacology, EarlyView.Abstract Schizophrenia is regarded as a complex and heterogeneous psychiatric disorder, characterised by diverse symptoms and comorbidities, which complicate both clinical management and drug development. Current pharmacological treatment, primarily based on dopamine D2 receptor antagonism or partial agonism, which has not markedly progressed since the
Thi Viet Ha Nguyen +2 more
wiley +1 more source
Drug design for CNS diseases: polypharmacological profiling of compounds using cheminformatic, 3D-QSAR and virtual screening methodologies [PDF]
, 2016 Support was kindly provided by the EU COST Action CM1103. DA, KN, and JV kindly acknowledge national project number 172033 and OI1612039 supported by the Ministry of the Republic of Serbia.
Agbaba, Danica +7 more
core +3 more sources