Cloning and characterisation of the human 5‐HT<sub>5A</sub> serotonin receptor

Rees, Stephen Edward; Daas, Izaak den; Foord, Steven M.; Goodson, Susannah J.; Bull, David A.; Kilpatrick, Gavin J.; Lee, Melanie

doi:10.1016/0014-5793(94)01209-1

Cited by 117 publications

(84 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Radioligand binding studies for the serotonin subtypes 5-HT 1A and 5-HT 5A were performed according to procedures described by Rees and colleagues (Rees et al, 1994) with the purpose of determining the binding activity of ethanol extracts compared to [³H]5-carboxamidotryptamine (5-CT). For the 5-HT 7 receptor binding studies, [³H] LSD was used to measure the binding ability of ethanol extracts.…”

Section: In Vitro Serotonin Receptor (5-ht 1a5a7 ) Binding Assaymentioning

confidence: 99%

Medical potential of plants used by the Q’eqchi Maya of Livingston, Guatemala for the treatment of women's health complaints

Michel

Duarte

Bolton

et al. 2007

Journal of Ethnopharmacology

View full text Add to dashboard Cite

Investigation on the medical ethnobotany of the Q'eqchi Maya of Livingston, Izabal, Guatemala, was undertaken in order to explore Q'eqchi perceptions, attitudes, and treatment choices related to women's health. Through participant observation and interviews a total of 48 medicinal plants used to treat conditions related to pregnancy, childbirth, menstruation, and menopause were collected and identified followed by the evaluation of 20 species in bioassays relevant to women's health. Results of field interviews indicate that Q'eqchi cultural perceptions affect women's health experiences while laboratory results (estrogen receptor and serotonin receptor binding assays) provide a scientific correlation between empirical medicinal plant use among the Q'eqchi and the pharmacological basis for their administration. These data can contribute to Guatemala's national effort to promote a complementary relationship between traditional Maya medicine and public health services and can serve as a basis for further pharmacology and phytochemistry on Q'eqchi medicinal plants for the treatment of women's health conditions.

show abstract

Section: In Vitro Serotonin Receptor (5-ht 1a5a7 ) Binding Assaymentioning

confidence: 99%

Medical potential of plants used by the Q’eqchi Maya of Livingston, Guatemala for the treatment of women's health complaints

Michel

Duarte

Bolton

et al. 2007

Journal of Ethnopharmacology

View full text Add to dashboard Cite

show abstract

“…Initial radioligand binding studies were performed by MDS Pharma Services (Bothell, WA) as previously described for serotonin receptor subtypes 1A, 1B, 2B, 2C, 3, 5A, 6, 7, serotonin transporter [5,6,8,23,31,32,[37][38][39][40][41][43][44][45]47]. Significant binding affinity was only observed at the 5-HT 5a receptor (>50%) for the PE and DCM extracts at a concentration of 50 μg/ml [12].…”

Section: Serotonin Receptor Binding Assaysmentioning

confidence: 99%

Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro

Dietz

Mahady

Pauli

et al. 2005

Molecular Brain Research

125

View full text Add to dashboard Cite

Insomnia is the most frequently encountered sleep complaint worldwide. While many prescription drugs are used to treat insomnia, extracts of valerian (Valeriana officinalis L., Valerianaceae) are also used for the treatment of insomnia and restlessness. To determine novel mechanisms of action, radioligand binding studies were performed with valerian extracts (100% methanol, 50% methanol, dichloromethane [DCM], and petroleum ether [PE]) at the melatonin, glutamate, and GABA A receptors, and 8 serotonin receptor subtypes. Both DCM and PE extracts had strong binding affinity to the 5-HT 5a receptor, but only weak binding affinity to the 5-HT 2b and the serotonin transporter. Subsequent binding studies focused on the 5-HT 5a receptor due to the distribution of this receptor in the suprachiasmatic nucleus of the brain, which is implicated in the sleep-wake cycle. The PE extract inhibited [ 3 H]lysergic acid diethylamide (LSD) binding to the human 5-HT 5a receptor (86% at 50 μg/ml) and the DCM extract inhibited LSD binding by 51%. Generation of an IC 50 curve for the PE extract produced a biphasic curve, thus GTP shift experiments were also performed. In the absence of GTP, the competition curve was biphasic (two affinity sites) with an IC 50 of 15.7 ng/ml for the high-affinity state and 27.7 μg/ml for the lowaffinity state. The addition of GTP (100 AM) resulted in a right-hand shift of the binding curve with an IC 50 of 11.4 μg/ml. Valerenic acid, the active constituent of both extracts, had an IC 50 of 17.2 AM. These results indicate that valerian and valerenic acid are new partial agonists of the 5-HT 5a receptor.

show abstract

“…Finally, with regards to the last three 5-HT receptor families, only moderate-to-low concentrations of both receptor proteins and mRNA have been found in the SN and the GP of rat and human brain for the 5-HT 5A (Rees et al, 1994;Oliver et al, 2000), 5-HT 6 (Kohen et al, 1996;430 Gerard et al, 1997;Hamon et al, 1999;Roberts et al, 2002;Hirst et al, 2003) and 5-HT 7 (Ruat et al, 1993b;Martin-Cora and Pazos, 2004;Varnas et al, 2004) receptor subtypes.…”

Section: Substantia Nigra and Globus Pallidusmentioning

confidence: 99%

“…Only moderate-to-low expression of 5-HT 5A receptor protein and mRNA has been found in the striatum of mouse, rat and human brain (Boess and Martin, 1994;Rees et al, 1994;Wesolowska, 2002). In particular, 5-HT 5A immunoreactivity was detectable at low levels in MSNs of rat caudate-putamen (Oliver et al, 2000).…”

Section: Striatummentioning

confidence: 99%

Serotonin modulation of the basal ganglia circuitry: therapeutic implication for Parkinson's disease and other motor disorders

Matteo

Pierucci

Esposito

et al. 2008

Progress in Brain Research

133

View full text Add to dashboard Cite

Several recent studies have emphasized a crucial role for the interactions between serotonergic and dopaminergic systems in movement control and the pathophysiology of basal ganglia. These observations are supported by anatomical evidence demonstrating large serotonergic innervation of all the basal ganglia nuclei. In fact, serotonergic terminals have been reported to make synaptic contacts with both substantia nigra dopamine-containing neurons and their terminal areas such as the striatum, the globus pallidus and the subthalamus. These brain areas contain a high concentration of serotonin (5-HT), with the substantia nigra pars reticulata receiving the greatest input. In this chapter, the distribution of different 5-HT receptor subtypes in the basal ganglia nuclei will be described. Furthermore, evidence demonstrating the serotonergic control of basal ganglia activity will be reviewed and the contribution of the different 5-HT receptor subtypes examined. The new avenues that the increasing knowledge of 5-HT in motor control has opened for exploring the pathophysiology and pharmacology of Parkinson's disease and other movement disorders will be discussed. It is clear that these avenues will be fruitful, despite the disappointing results so far obtained by clinical studies with selective 5-HT ligands. Nevertheless, these studies have led to a great increase in the attention given to the neurotransmitters of the basal ganglia and their connections.

show abstract

Cloning and characterisation of the human 5‐HT_5A serotonin receptor

Cited by 117 publications

References 8 publications

Medical potential of plants used by the Q’eqchi Maya of Livingston, Guatemala for the treatment of women's health complaints

Medical potential of plants used by the Q’eqchi Maya of Livingston, Guatemala for the treatment of women's health complaints

Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro

Serotonin modulation of the basal ganglia circuitry: therapeutic implication for Parkinson's disease and other motor disorders

Contact Info

Product

Resources

About

Cloning and characterisation of the human 5‐HT5A serotonin receptor

Cited by 117 publications

References 8 publications

Medical potential of plants used by the Q’eqchi Maya of Livingston, Guatemala for the treatment of women's health complaints

Medical potential of plants used by the Q’eqchi Maya of Livingston, Guatemala for the treatment of women's health complaints

Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro

Serotonin modulation of the basal ganglia circuitry: therapeutic implication for Parkinson's disease and other motor disorders

Contact Info

Product

Resources

About

Cloning and characterisation of the human 5‐HT_5A serotonin receptor