Cloning and Expression of a 5‐Hydroxytryptamine<sub>7</sub> Receptor Positively Coupled to Adenylyl Cyclase

Tsou, Ann-Ping; Kosaka, Alan; Bach, Chinh; Zuppan, Patti; Yee, Calvin; Tom, Leonard; Alvarez, Robert; Ramsey, Scott D.; Bonhaus, Douglas W.; Stefanich, Eric; Jakeman, Lyn B.; Eglen, Richard M.; Chan, Hardy

doi:10.1046/j.1471-4159.1994.63020456.x

Cited by 175 publications

(97 citation statements)

References 26 publications

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“…The structures of these compounds and/or their receptor coupling efficiencies might explain the different potencies (Leung et al, 1996). In addition, these agonists may affect other 5-HT receptors (Hensley and Cohen, 1992;Sebben et al, 1994;Tsou et al, 1994). However, because the agonist-induced facilitation of TRPV1 function was significantly reversed by SB204070, a selective 5-HT 4 receptor antagonist, we consider their effects to represent actions at the 5-HT 4 receptor.…”

Section: Discussionmentioning

confidence: 99%

TRPV1 Function in Mouse Colon Sensory Neurons Is Enhanced by Metabotropic 5-Hydroxytryptamine Receptor Activation

Sugiuar

Bielefeldt²,

Gebhart³

2004

J. Neurosci.

125

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Using whole-cell patch-clamp methods, we examined the hypothesis that serotonin [5-hydroxytryptamine (5-HT)] receptor activation enhances TRPV1 function in mouse colon sensory neurons in lumbosacral dorsal root ganglia, which were identified by retrograde labeling with DiI (1,1Ј-dioctadecyl-3,3,3Ј,3-tetramethlindocarbocyanine methanesulfonate) injected into multiple sites in the wall of the descending colon. 5-HT increased membrane excitability at a temperature below body temperature in response to thermal ramp stimuli in colon sensory neurons from wild-type mice, but not from TRPV1 knock-out mice. 5-HT significantly enhanced capsaicin-, heat-, and proton-evoked currents with an EC 50 value of 2.2 M. 5-HT (1 M) significantly increased capsaicin-evoked (100 nM) and proton-evoked (pH 5.5) currents 1.6-and 4.7-fold, respectively, and significantly decreased the threshold temperature for heat current activation from 42 to 38°C.

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Section: Discussionmentioning

confidence: 99%

TRPV1 Function in Mouse Colon Sensory Neurons Is Enhanced by Metabotropic 5-Hydroxytryptamine Receptor Activation

Sugiuar

Bielefeldt²,

Gebhart³

2004

J. Neurosci.

125

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“…cDNA clones of the mRNAs encoding this receptor have been isolated from several different species, including mouse, rat, guinea pig, and human. In all species, the 5-HT 7 receptor shows a consistent mRNA distribution pattern within the brain (1,3,4) and ligand binding profile (5)(6)(7)(8). The 5-HT 7 receptor is mainly localized to the hypothalamus, hippocampus, and frontal cortex.…”

mentioning

confidence: 90%

No hypothermic response to serotonin in 5-HT ₇ receptor knockout mice

Hedlund

Danielson

Thomas

et al. 2003

Proc. Natl. Acad. Sci. U.S.A.

167

125

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With data from recently available selective antagonists for the 5-HT7 receptor, it has been hypothesized that 5-hydroxytryptamine (5-HT)-induced hypothermia is mediated by the 5-HT7 receptor, an effect previously attributed to other receptor subtypes. It has been established that the biologically active lipid oleamide allosterically interacts with the 5-HT7 receptor to regulate its transmission. The most well characterized effects of oleamide administration are induction of sleep and hypothermia. Here, we demonstrate, by using mice lacking the 5-HT7 receptor, that 5-HTinduced hypothermia is mediated by the 5-HT7 receptor. Both 5-HT and 5-carboxamidotryptamine, a 5-HT1 and 5-HT7 receptor agonist, in physiological doses fail to induce hypothermia in 5-HT7 knockout mice. In contrast, oleamide was equally effective in inducing hypothermia in mice lacking the 5-HT7 receptors as in wild-type mice. When administered together, 5-HT and oleamide showed additive or greater than additive effects in reducing body temperature. Taken together, the results show that 5-HT-induced hypothermia is mediated by the 5-HT7 receptor, and that oleamide may act through an independent mechanism as well as at an allosteric 5-HT7 receptor site to regulate body temperature. The 5-HT 7 receptor is one of the most recently described members of the large family of serotonin [5-hydroxytryptamine (5-HT)] receptors (1, 2). cDNA clones of the mRNAs encoding this receptor have been isolated from several different species, including mouse, rat, guinea pig, and human. In all species, the 5-HT 7 receptor shows a consistent mRNA distribution pattern within the brain (1, 3, 4) and ligand binding profile (5-8). The 5-HT 7 receptor is mainly localized to the hypothalamus, hippocampus, and frontal cortex.Functionally, the 5-HT 7 receptor has been shown to stimulate cAMP formation (1, 2, 6, 7). This stimulation has been linked to the activation of a calmodulin-regulated adenylyl cyclase (9). The existence of several splice variants of the 5-HT 7 receptor mRNA has been clearly demonstrated (10-12). The variants encode receptors that have slightly different lengths of the C termini, but with no detectable difference in tissue distributions or functional couplings (13). The 5-HT 7 receptor has also been detected in the periphery, where it is found primarily in smooth muscle cells of blood vessels (2, 14), but also in the gastrointestinal tract (2).Early studies established a pharmacological profile that distinguished 5-HT 7 receptors from other 5-HT receptors. The 5-HT 7 receptor shows a high affinity for 5-HT, 5-carboxamidotryptamine (5-CT), and methiothepin, relatively high affinity for 8-hydroxy-[N-n-dipropyl-N-(3Ј-iodo-2Јpropenyl)amino]tetralin (8-OH-DPAT) and ritanserin, and low affinity for pindolol and buspirone (1, 15). Recently, more selective antagonists have been described (16)(17)(18)(19), developments that will facilitate the characterization of the 5-HT 7 receptor.The 5-HT 7 receptor has been linked to a number of physiological and pathophysiologi...

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“…In the present autoradiographic study, we took advantage of 5-HT 1A knockout and 5-HT 1A/1B double-knockout mice to revisit the pharmacological characterization and anatomical localization of 5-HT 7 binding sites in mouse brain using [ The 5-HT 7 receptor is the most recently identified member of the family of G protein-coupled 5-HT receptors (for review, see Vanhoenacker et al, 2000). The 5-HT 7 receptor has been cloned from rat Ruat et al, 1993;Shen et al, 1993), mouse (Plassat et al, 1993), human (Bard et al, 1993), and guinea pig (Tsou et al, 1994). The receptor is positively coupled to adenylate cyclase, preferentially via Gs.…”

Section: Introductionmentioning

confidence: 99%

“…The 5-HT 7 receptor has been cloned from rat Ruat et al, 1993;Shen et al, 1993), mouse (Plassat et al, 1993), human (Bard et al, 1993), and guinea pig (Tsou et al, 1994). The receptor is positively coupled to adenylate cyclase, preferentially via Gs.…”

mentioning

confidence: 99%

Reconsideration of 5-Hydroxytryptamine (5-HT)₇Receptor Distribution Using [³H]5-Carboxamidotryptamine and [³H]8-Hydroxy-2-(di-n-propylamino)tetraline: Analysis in Brain of 5-HT_1AKnockout and 5-HT_1A/1BDouble-Knockout Mice

Bonaventure

Nepomuceno²,

Kwok³

et al. 2002

J Pharmacol Exp Ther

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The characterization and anatomical distribution of 5-hydroxytryptamine (5-HT) 7 receptor binding sites in brain tissue has been hampered by the lack of a specific radioligand. In the present autoradiographic study, we took advantage of 5-HT 1A knockout and 5-HT 1A/1B double-knockout mice to revisit the pharmacological characterization and anatomical localization of 5-HT 7 binding sites in mouse brain using [ The 5-HT 7 receptor is the most recently identified member of the family of G protein-coupled 5-HT receptors (for review, see Vanhoenacker et al., 2000). The 5-HT 7 receptor has been cloned from rat Ruat et al., 1993;Shen et al., 1993), mouse (Plassat et al., 1993), human (Bard et al., 1993), and guinea pig (Tsou et al., 1994). The receptor is positively coupled to adenylate cyclase, preferentially via Gs. It exhibits a high degree of interspecies homology (approximately 95%) but a low sequence homology with other 5-HT receptors (Ͻ40%). In rat and human, three different splice variants have been described to date, which are thought to have similar pharmacology and function (Heidmann et al., 1997;Krobert et al., 2001). The pharmacological profile of the 5-HT 7 receptor is consistent across all tested species and is characterized by high affinity for the 5-HT 1 agonists 5-CT, 5-HT, and 8-OH-DPAT; and the 5-HT 2 antagonists ritanserin, metergoline, mesulergine, and risperidone. Possible physiological functions for this receptor have been suggested, including relaxation in several vascular preparations (Bard et al., 1993;Shen et al., 1993) and circadian rhythm control via the suprachiasmatic nucleus of the hypothalamus Gannon, 2001). Because 8-OH-DPAT has been shown to exhibit a relatively high affinity for the 5-HT 7 receptor, multiple functions formerly ABBREVIATIONS:

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Cloning and Expression of a 5‐Hydroxytryptamine₇ Receptor Positively Coupled to Adenylyl Cyclase

Cited by 175 publications

References 26 publications

TRPV1 Function in Mouse Colon Sensory Neurons Is Enhanced by Metabotropic 5-Hydroxytryptamine Receptor Activation

TRPV1 Function in Mouse Colon Sensory Neurons Is Enhanced by Metabotropic 5-Hydroxytryptamine Receptor Activation

No hypothermic response to serotonin in 5-HT ₇ receptor knockout mice

Reconsideration of 5-Hydroxytryptamine (5-HT)₇Receptor Distribution Using [³H]5-Carboxamidotryptamine and [³H]8-Hydroxy-2-(di-n-propylamino)tetraline: Analysis in Brain of 5-HT_1AKnockout and 5-HT_1A/1BDouble-Knockout Mice

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Cloning and Expression of a 5‐Hydroxytryptamine7 Receptor Positively Coupled to Adenylyl Cyclase

Cited by 175 publications

References 26 publications

TRPV1 Function in Mouse Colon Sensory Neurons Is Enhanced by Metabotropic 5-Hydroxytryptamine Receptor Activation

TRPV1 Function in Mouse Colon Sensory Neurons Is Enhanced by Metabotropic 5-Hydroxytryptamine Receptor Activation

No hypothermic response to serotonin in 5-HT 7 receptor knockout mice

Reconsideration of 5-Hydroxytryptamine (5-HT)7Receptor Distribution Using [3H]5-Carboxamidotryptamine and [3H]8-Hydroxy-2-(di-n-propylamino)tetraline: Analysis in Brain of 5-HT1AKnockout and 5-HT1A/1BDouble-Knockout Mice

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Cloning and Expression of a 5‐Hydroxytryptamine₇ Receptor Positively Coupled to Adenylyl Cyclase

No hypothermic response to serotonin in 5-HT ₇ receptor knockout mice

Reconsideration of 5-Hydroxytryptamine (5-HT)₇Receptor Distribution Using [³H]5-Carboxamidotryptamine and [³H]8-Hydroxy-2-(di-n-propylamino)tetraline: Analysis in Brain of 5-HT_1AKnockout and 5-HT_1A/1BDouble-Knockout Mice