Results 181 to 190 of about 10,873 (200)

Histamine H3 Receptor Function and Ligands: Recent Developments

Mini-Reviews in Medicinal Chemistry, 2012
Histamine H3 receptors are found mostly in central nervous system involved in the regulation of release of various neurotransmitters in brain. They have been implicated in diverse potential therapeutic applications such as sleep-wake disorders, attention-deficient hyperactivity disorder, epilepsy, cognitive impairment and obesity.
Mahaveer, Singh, Hemant R, Jadhav
openaire   +2 more sources

Phencyclidine blocks histamine H3-receptors in rat brain

European Journal of Pharmacology, 1988
Phencyclidine (PCP) was examined for its ability to modulate histamine release from rat brain slices labeled with L-[3H]histidine. PCP failed to mimic but completely reversed the autoinhibitory effect of histamine at H3-receptors with an apparent Ki value of 13 +/- 3 microM.
J M, Arrang, N, Defontaine, J C, Schwartz   +2 more
openaire   +2 more sources

Histamine H3 receptors: an overview.

The Italian journal of gastroenterology, 1992
Histamine H3 receptors represent a new class of prejunctional receptors, which, first described as modulators of histamine synthesis and release in the central nervous system, were subsequently found to occur also in peripheral tissues. They may behave both as autoreceptors located in histaminergic neurons and as heteroreceptors localized in adrenergic,
G, Bertaccini, G, Coruzzi, M, Adami, C, Pozzoli, E, Gambarelli   +4 more
openaire   +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.
R, Wolin, M, Connolly, A, Afonso, J A, Hey, H, She, M A, Rivelli, S M, Willams, R E, West   +7 more
openaire   +2 more sources

Design of histamine H3-receptor agonists and antagonists

European Journal of Drug Metabolism and Pharmacokinetics, 1994
The development of highly potent and selective ligands for the characterization of histamine H3-receptors is reviewed. In the field of agonists stereoselectively methylated derivatives of the natural ligand are found to have the desired pharmacodynamic properties. Pharmacokinetic properties could be improved by forming bioreversible azomethine prodrugs
W, Schunack, H, Stark
openaire   +2 more sources

Rasagiline derivatives combined with histamine H3 receptor properties

Bioorganic & Medicinal Chemistry Letters, 2019
The irreversible monoamine oxidase B (MAO B) inhibitor rasagiline has been described with multiple disease modifying effects in vitro on models of Parkinson's disease. The combination of this established drug to recently developed histamine H3 receptor (H3R) antagonist elements gives new impetus to the design of multitargeting ligands.
K, Lutsenko, S, Hagenow, A, Affini, D, Reiner, H, Stark   +4 more
openaire   +2 more sources

Histamine homologues discriminating between two functional H3 receptor assays. Evidence for H3 receptor heterogeneity?.

The Journal of Pharmacology and Experimental Therapeutics, 1996
We studied several histamine homologues as potential ligands for the histamine H3 receptor in two binding assays ([125l]iodophenpropit and N alpha-[3H]methylhistamine binding to rat brain cortex membranes) and two functional H3 receptor models (inhibition of the neurogenic contraction in the guinea pig jejunum and of [3H]noradrenaline release in mouse ...
Leurs, R., Kathmann, M., Vollinga, R.C., Menge, W.M.P.B., Schlicker, E., Timmerman, H.   +5 more
openaire   +3 more sources

Histamine H3-Receptor Inverse Agonists as Novel Antipsychotics

Central Nervous System Agents in Medicinal Chemistry, 2009
Schizophrenia (SZ) that is resistant to treatment with dopamine (DA) D2 antagonists may involve changes other than those in the dopaminergic system. Recently, histamine (HA), which regulates arousal and cognitive functions, has been suggested to act as a neurotransmitter in the central nervous system.
openaire   +2 more sources

H3 Receptor Miniseries: The histamine H3 receptor and eating behavior

2011
Interest in the histaminergic system as a potential target for the treatment of feeding disorders is driven by the unsatisfactory history of the pharmacotherapy of obesity. Eating behavior is regulated by a complex interplay of central neurotransmitter systems, peripheral endocrine stimuli, the circadian rhythm, and environmental cues, all factors that
PASSANI, MARIA BEATRICE, BLANDINA, PATRIZIO, F. Torrealba   +2 more
openaire   +1 more source

Stress and brain H3-histamine receptors

Inflammation Research, 1995
P, Ghi, M, Blengio, C, Ferretti, P, Portaleone   +3 more
openaire   +2 more sources