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Identification of serotonin 5-HT1A receptor partial agonists in ginger

open access: yesBioorganic & Medicinal Chemistry, 2010
Animal studies suggest that ginger (Zingiber officinale Roscoe) reduces anxiety. In this study, bioactivity-guided fractionation of a ginger extract identified nine compounds that interact with the human serotonin 5-HT(1A) receptor with significant to moderate binding affinities (K(i)=3-20 microM).
Nievergelt, Andreas   +4 more
openaire   +5 more sources
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Serotonin and psychostimulant addiction: Focus on 5-HT1A-receptors

Progress in Neurobiology, 2007
Serotonin(1A)-receptors (5-HT(1A)-Rs) are important components of the 5-HT system in the brain. As somatodendritic autoreceptors they control the activity of 5-HT neurons, and, as postsynaptic receptors, the activity in terminal areas. Cocaine (COC), amphetamine (AMPH), methamphetamine (METH) and 3,4-methylenedioxymethamphetamine ("Ecstasy", MDMA) are ...
Christian P, Müller   +3 more
openaire   +2 more sources

Serotonin-induced 5-HT1A receptor desensitization in C6BU-1 glioma cells transfected with 5-HT1A receptor gene

Neuroscience Letters, 1995
In this study, it has been clearly demonstrated that a selective 5-hydroxytryptamine (5-HT)1A agonist, 8-OH-2-(di-n-propylamino)-tetraline (8-OH-DPAT, 1 microM) significantly inhibited forskolin (10 microM)-stimulated cyclic AMP (cAMP) accumulation in the C6BU-1 cells transfected with 5-HT1A receptor gene.
K, Saitoh   +5 more
openaire   +2 more sources

Clozapine is a partial agonist at cloned, human serotonin 5-HT1A receptors

Neuropharmacology, 1996
Clozapine exhibited 10-fold higher affinity than haloperidol for human 5-HT1A receptors expressed in Chinese Hamster Ovary cells (CHO-h5-HT1A) (Kis = 160 and 1910 nM respectively). Whereas haloperidol did not alter the basal binding of [35S]GTP gama S to CHO-h5HT1A membranes, clozapine stimulated it with an EC50 of 2320 nM and an efficacy of 49 ...
A, Newman-Tancredi   +3 more
openaire   +2 more sources

Visualisation of serotonin-1A (5-HT1A) receptors in the central nervous system

European Journal of Nuclear Medicine, 2000
The 5-HT1A subtype of receptors for the neurotransmitter serotonin is predominantly located in the limbic forebrain and is involved in the modulation of emotion and the function of the hypothalamus. Since 5-HT1A receptors are implicated in the pathogenesis of anxiety, depression, hallucinogenic behaviour, motion sickness and eating disorders, they are ...
J, Passchier, A, van Waarde
openaire   +2 more sources

Modification of serotonin neuron properties in mice lacking 5-HT1A receptors

European Journal of Pharmacology, 2002
Using null mutant mice for the 5-HT1A receptor (5-HT1A-/-), extracellular electrophysiological recordings were first conducted to evaluate the impact of its genetic deletion on the firing rate of dorsal raphe 5-hydroxytryptamine (5-HT) neurons. Experiments were also done using brain slices to assess whether any compensation phenomenon had taken place ...
Maxime, Richer   +2 more
openaire   +2 more sources

Diurnal rhythm in the levels of the serotonin 5-HT1A receptors in the crayfish eyestalk

Synapse, 2006
The crayfish eyestalk (ES) has been postulated as a possible circadian clock. 5-Hydroxytryptamine (5-HT) has been shown to play the role of a neurotransmitter or a modulator in the ES. However, little is known about the 5-HT receptors in the ES. The purpose of this work is to determine the specific binding sites using [(3)H]8-hydroxy-2(di-n-propylamino)
Gabina, Calderón-Rosete   +2 more
openaire   +2 more sources

Corticosterone regulation of serotonin transporter and 5‐HT1A receptor expression in the aging brain

Synapse, 1999
Hypercortisolemia is often observed in patients suffering from major depression. As the serotonergic (5-hydroxytryptamine; 5-HT) system plays a major role in the etiology of depression, a loss of endocrine and neurotransmitter system interactions, including corticosterone regulation of 5-HT transporter (5-HTT) and 5-HT receptor expression, may underlie
L W, Maines   +3 more
openaire   +2 more sources

Localization of 5-HT1A serotonin receptors in the cerebellum of young rats

Neurochemistry International, 1991
Abstract Previous studies have shown that functional 5-HT 1A receptors are present in the cerebellum only for the early postnatal period in rats. In order to investigate further the possible physiological significance of such a transient expression of 5-HT 1A receptors during maturation of the cerebellum, anatomical studies were performed for ...
Daniel Verge   +5 more
openaire   +1 more source

Neuroticism and serotonin 5-HT1A receptors in healthy subjects

Psychiatry Research: Neuroimaging, 2015
Neuroticism is a personality trait associated with vulnerability for mood and anxiety disorders. Serotonergic mechanisms likely contribute to neuroticism. Serotonin 5-HT1A receptors are altered in mood and anxiety disorders, but whether 5-HT1A receptors are associated with neuroticism in healthy subjects is unclear.
Hirvonen, Jussi   +3 more
openaire   +5 more sources

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