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Electrophysiological, biochemical, neurohormonal and behavioural studies with WAY-100635, a potent, selective and silent 5-HT1A receptor antagonist
In vitro electrophysiological studies demonstrated that WAY-100635 had no 5-HT1A receptor agonist actions, but dose-dependently blocked the effects of agonists at both the postsynaptic5-HT 1A receptor in the CA1 region of the hippocampus, and the somatodendritic 5-ht1A receptors located on dorsal raphe 5- HT neurones.
Serotonin transporter overexpression is responsible for pulmonary artery smooth muscle hyperplasia in primary pulmonary hypertension.
It is concluded that 5-HTT activity plays a key role in the pathogenesis of PA-SMC proliferation in PPH and that a 5HTT polymorphism confers susceptibility to PPH.
Cloning of a functional vesicular GABA and glycine transporter by screening of genome databases
Hydropathy plot analysis identifies a candidate vesicular GABA transporter in genomic sequences derived from a region of the physical map comprising unc‐47 of Caenorhabditis elegans and demonstrates that the mouse clone encodes a vesicle inhibitory amino acid transporter.
International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors.
The peptide cholecystokinin has been shown to mediate pancreatic secretion and contraction of gallbladder and was described in the mammalian central nervous system (CNS) as a gastrin-like peptide.
International Union of Pharmacology. XII. Classification of opioid receptors.
The results show that data from published knowledge can be used to provide reliable, patient level, automated risk assessment, potentially reducing the cognitive burden on physicians and helping policy makers better prepare for future needs.
Somatodendritic localization of 5‐HT1A and preterminal axonal localization of 5‐HT1B serotonin receptors in adult rat brain
The localization of 5‐HT1B receptors to the membrane of preterminal axons suggests that they control transmitter release from nonserotonin as well as serotonin neurons by mediating serotonin effects on axonal conduction.
Neurotransmitter transporters in the central nervous system.
Intercellular communication in the central nervous system (CNS)2 requires the precise control of the duration and the intensity of neurotransmitter action at specific molecular targets. After they
Disruption of the nonneuronal tph1 gene demonstrates the importance of peripheral serotonin in cardiac function
It is established that the neuronal tph2 is expressed in neurons of the raphe nuclei and of the myenteric plexus, whereas the nonneuronal tph1, as detected by β-galactosidase expression, is in the pineal gland and the enterochromaffin cells.
Epigenetic regulation of the BDNF gene: implications for psychiatric disorders
An overview of the current literature on epigenetic modifications at the BDNF locus in psychiatric disorders and related animal models is presented and drugs that modify epigenetic regulation at specific BDNF exons represents a promising strategy for the treatment of psychiatric disorders.
The selective 5-HT1A antagonist radioligand [3H]WAY 100635 labels both G-protein-coupled and free 5-HT1A receptors in rat brain membranes.
The tritiated derivative of the novel silent 5-HT1A receptor antagonist WAY 100635 [N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl) cyclohexane carboxamide] was tested as a potential