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1 5-HT increased frequency of sIPSCs without affecting pos
2 5-HT increased vesicular GABA release in naive and depen
3 5-HT(2A) activation gave rise to stress fibers in these
4 5-HT(2A)R agonist-induced head-twitch behavior was also
5 5-HT(2A,) a G-protein coupled receptor, is widely expres
6 5-HT(3) receptors are pentameric ligand-gated ion channe
7 5-HT(7) drives the acquisition of profibrotic and anti-i
8 5-HT(7) receptors in their inactive state associate with
9 5-HT-ir neurons were also observed within the vocal moto
11 r 1 (TAAR1) and 5-hydroxytryptamine type 1A (5-HT(1A)) receptors, may represent a new class of psycho
12 01854944) was to assess D(2)/D(3), 5-HT(1A), 5-HT(2A) and serotonin transporter (SERT) occupancies of
14 ata and indicating the involvement of MT(2) /5-HT(2C) heteromers. The antidepressant agomelatine had
16 ose dependent manner, while binding to D(3), 5-HT(1A) receptors and SERT was not detectable with the
17 study (NCT01854944) was to assess D(2)/D(3), 5-HT(1A), 5-HT(2A) and serotonin transporter (SERT) occu
18 ons of the homomeric 5-hydroxytryptamine 3A (5-HT(3A)) serotonin receptor for 15 to 20 mus to demonst
20 that antagonizing serotonin (5-HT) type 3AB (5-HT(3AB)) receptors in brain areas involved in mood reg
22 Compound 12 (CTW0415) was discovered as a 5-HT(2C)R PAM with improved pharmacokinetics and reduced
23 stimulation of beta-cells were blocked by a 5-HT(3)R antagonist and were enhanced by increasing sero
25 lthy volunteers were randomly allocated to a 5-HT depletion (N = 24), DA depletion (N = 24), or place
29 havioral and neural responses observed after 5-HT depletion in the current study closely resemble our
30 lowing the formation of conventional agonist-5-HT(7)-G(s) ternary complexes and subsequent G(s) activ
33 nist SB-243213, and were absent in MT(2) and 5-HT(2C) knockout mice, fully recapitulating previous in
35 (2A)-, mGlu(2)/Gqo5-, 5-HT(2A)/mGlu(2)-, and 5-HT(2A)/mGlu(2)/Gqo5-expressing HEK293 cells using a Ca
37 on of serotonin receptors, with 5-HT(2B) and 5-HT(7) expression restricted to M-CSF-primed monocyte-d
40 l-emotion processing and brain dynamics, and 5-HT abnormalities have been consistently implicated in
41 that mostly colocalized PDF, FMRFamide, and 5-HT immunoreactivities, and with terminals of ipsi- and
42 These results suggest that glutamate and 5-HT, released by NTS afferent terminals, trigger Ca(2+)
43 tor pathways regenerated into the graft, and 5-HT(+) neurons within graft and host brainstem neurons
48 trated in vivo binding to D(2) receptors and 5-HT(2A) receptors at steady state after 10 days of dail
50 gonism at trace amine receptor 1 (TAAR1) and 5-HT(1A) receptors but no appreciable action at dopamine
51 namic range of agonist-induced signaling, as 5-HT(7) receptors spontaneously activate G(s) variants t
52 ed 5-HT staining in SK-N-SH cells as well as 5-HT concentrations in the culture media and cell lysate
60 -ICD is required for the interaction between 5-HT(3A) and the chaperone protein resistance to inhibit
61 responses in 5-HT(2A)/mGlu(2) cells and both 5-HT- and Glu-induced responses in 5-HT(2A)/mGlu(2)/Gqo5
62 mulation results of apo- and serotonin-bound 5-HT(3A)R, the study reveals a distinct interaction fing
63 tion regarding the orthosteric activation by 5-HT and by the partial agonist tryptamine, and the allo
65 osteric regulation of ion gating elements by 5-HT binding is indicative of a preactive state, which p
66 lease was attenuated, suggesting blunted CeA 5-HT sensitivity, which partially recovered in protracte
67 Here, we examined neuroadaptations of CeA 5-HT signaling in adult, male Sprague Dawley rats using
68 em and unravels the vulnerability of the CeA 5-HT system to chronic alcohol and protracted withdrawal
69 of firing rate of DRN 5-HT neurons, cerebral 5-HT depletion, and optogenetic activation and silencing
70 n addition, we comprehensively characterized 5-HT-immunoreactive (-ir) innervation throughout the bra
72 ll vocal midbrain nuclei showed considerable 5-HT-ir innervation, as did thalamic and hindbrain audit
74 impairment, but not increased frontal cortex 5-HT(2A)R density or psychedelic-induced head-twitch beh
77 and ERICH3 knock-out dramatically decreased 5-HT staining in SK-N-SH cells as well as 5-HT concentra
80 These changes presumably lead to decreased 5-HT synthesis and/or increased 5-HT reuptake, thereby r
81 tional knockout male mice supports deficient 5-HT transmission underlying depression-related phenotyp
85 it, in vivo recordings of firing rate of DRN 5-HT neurons, cerebral 5-HT depletion, and optogenetic a
88 )R) allosteric site to potentiate endogenous 5-HT tone may provide novel therapeutics to alleviate th
89 ve panel of pruritogens (C48/80, endothelin, 5-HT, chloroquine, histamine, lysophosphatidic acid, try
90 (5-HT) in the mammalian brain, and excessive 5-HT signaling is critically implicated in the etiology
91 eus, the major source of 5-HT, and expresses 5-HT receptor subtypes (e.g., 5-HT2C and 5-HT1A) critica
92 CE) using chitosan as cross-linked agent for 5-HT sensing studies; conducted through cyclic voltammet
94 ancy; Cohort 2 received [(11)C]MDL100907 for 5-HT(2A) occupancy and [(11)C]DASB for SERT occupancy; C
95 of 63 +/- 11 nM for DA and 40 +/- 17 nM for 5-HT through a wide concentration range (40 nM-200 muM).
96 anomolar detection limit of 63 +/- 11 nM for 5-HT through a wide concentration range (63 nM-200 muM)
100 ts demonstrate the existence of a functional 5-HT/5-HT(2B)/AhR axis in human macrophages and indicate
101 nteraction, we developed different MBP-fused 5-HT(3A)-ICD constructs by deleting large segments of it
102 e characterized in 5-HT(2A)-, mGlu(2)/Gqo5-, 5-HT(2A)/mGlu(2)-, and 5-HT(2A)/mGlu(2)/Gqo5-expressing
103 on mouse homomeric 5-HT(3A) and heteromeric 5-HT(3AB) receptors expressed in Xenopus laevis oocytes
104 hibited 5-HT-induced currents in heteromeric 5-HT type 3AB receptors (5-HT(3AB)Rs) (IC(50) = 840 and
106 effects that bupropion exerts on heteromeric 5-HT(3AB) receptors, in particular when constantly prese
107 t ligands targeting the putative heteromeric 5-HT(2A)/mGlu(2) receptor complex, based on the 5-HT(2A)
113 bupropion and hydroxybupropion for homomeric 5-HT(3A)Rs were 10- and 5-fold lower, respectively (87 a
114 tabolite hydroxybupropion on mouse homomeric 5-HT(3A) and heteromeric 5-HT(3AB) receptors expressed i
116 To date, however, no one has examined how 5-HT influences the dynamics of facial-emotion processin
118 By constructing a high-conductance human 5-HT(3)A receptor, we here revealed mechanistic informat
119 e of the vestibule binding site to the human 5-HT(3) receptor, suggesting a common mechanism of modul
120 g the activation and modulation of the human 5-HT(3) type A receptor has been based only on macroscop
121 ot only extend our knowledge about the human 5-HT(3)A molecular function but also provide novel insig
122 inding and unbinding of 5-hydroxytryptamine (5-HT) (i.e., serotonin) to the binding pocket located on
123 hown that the selective 5-hydroxytryptamine (5-HT) (serotonin) reuptake inhibitor (SSRI) fluoxetine (
126 smitters, estimation of 5-hydroxytryptamine (5-HT; Serotonin) release has proved to be challenging.
130 heterobivalent ligands were characterized in 5-HT(2A)-, mGlu(2)/Gqo5-, 5-HT(2A)/mGlu(2)-, and 5-HT(2A
131 ing affinities exhibited by the compounds in 5-HT(2A), 5-HT(2A)/mGlu(2), and 5-HT(2A)/mGlu(2)/Gqo5 ce
134 ligands inhibited 5-HT-induced responses in 5-HT(2A)/mGlu(2) cells and both 5-HT- and Glu-induced re
138 propion with 5-HT dose dependently inhibited 5-HT-induced currents in heteromeric 5-HT type 3AB recep
139 lities, the seven bivalent ligands inhibited 5-HT-induced responses in 5-HT(2A)/mGlu(2) cells and bot
140 mimics therapeutic drug conditions inhibits 5-HT-induced currents in 5-HT(3A) and 5-HT(3AB) receptor
141 ructs that are unable to form the interclass 5-HT(2A)R-mGluR2 complex, we demonstrated that heteromer
142 gions in the superior raphe, an intermediate 5-HT-ir cell cluster, and an extensive inferior raphe po
144 ug intake, genetically predisposed irregular 5-HT receptor density, or change in sensory bombardment
145 that the 5-HT-mediated activation of AhR is 5-HT(2B) dependent because it is abrogated by the 5-HT(2
147 ata show that in addition to (R,S)-ketamine, 5-HT(4)R agonists are also effective prophylactics again
148 resolution cryo-EM structures of full-length 5-HT(3A)R in complex with palonosetron, ondansetron, and
151 ptor occupancy and [(11)C]CUMI101 to measure 5-HT(1A) occupancy; Cohort 2 received [(11)C]MDL100907 f
153 ver, the detailed mechanisms underlying mPFC 5-HT(1A) receptor-mediated antidepressant-like effects a
154 d arise by either the expression of multiple 5-HT receptors (5-HTRs) on the same cells or by populati
155 ong enough to observe complete activation of 5-HT(3A), the allosteric regulation of ion gating elemen
156 Our findings reveal that the activity of 5-HT(DR->VTA) neurons may be an essential factor in dete
159 racellular compartments, and coexpression of 5-HT(2A)R with mGluR2 increased the intracellular distri
162 etermine the transcriptional consequences of 5-HT(2B) engagement in human macrophages, for which 5-HT
163 using Ni(3)HHTP(2) MOFs for the detection of 5-HT with a nanomolar detection limit of 63 +/- 11 nM fo
169 Therefore, we compared the influence of 5-HT on the responsivity of brain dynamics during facial
170 nt increase in adhesion, while inhibition of 5-HT(2A) by antipsychotics, such as risperidone, olanzap
172 d that citalopram (which increases levels of 5-HT) caused sustained activation in key limbic regions
173 portantly, the bidirectional manipulation of 5-HT(DR->VTA) neurons could modulate susceptibility to s
174 offers new insights into the organization of 5-HT nuclei in teleosts and provides neuroanatomical evi
176 to long-duration clusters in the presence of 5-HT and even longer in the presence of terpenoids, wher
178 downregulated with a concurrent reduction of 5-HT-immunoreactivity in the DRN and its two major proje
181 itude longer than any previous simulation of 5-HT(3A), allow us to observe the dynamic binding and un
182 he dorsal raphe nucleus, the major source of 5-HT, and expresses 5-HT receptor subtypes (e.g., 5-HT2C
183 sults indicate that selective stimulation of 5-HT(1A) receptor in the mPFC exerts rapid and sustained
184 udies, we present an argument for the use of 5-HT(1A) agonists in the treatment of Dup15q epilepsy.
185 ur results indicate that adiponectin acts on 5-HT neurons through AdipoR1 receptors to regulate depre
186 iological function of TSPAN5 with a focus on 5-HT and kynurenine concentrations in the tryptophan pat
187 r, they add to an emerging view that NAC, or 5-HT(1B/1D/1F) receptor agonist treatment, may be a prom
188 nal secretagogues, drugs acting on opioid or 5-HT receptors, or minimally absorbed antibiotics (all o
189 eaches the AL via the diffusion of paracrine 5-HT through the fly hemolymph [8] and by activation of
191 by which it might be associated with plasma 5-HT concentrations and SSRI clinical response remained
194 ET) using [(11)C]CUMI-101 (CUMI) to quantify 5-HT(1A) binding in midbrain raphe nuclei and functional
195 investigated the relationship between raphe 5-HT(1A) binding and brain-wide network dynamics of nega
198 , expression and stimulation of human or rat 5-HT(2A) receptor by agonists such as serotonin or 2,5-d
201 frontal cortex serotonin 5-HT(2A) receptor (5-HT(2A)R) density in the adult offspring, a phenotype p
202 addition to the serotonin 5-HT(2A) receptor (5-HT(2A)R), the dopamine D(2) receptor (D(2)R) is a key
203 ting the serotonin (5-HT) 5-HT(2C) receptor (5-HT(2C)R) allosteric site to potentiate endogenous 5-HT
206 effects of specific serotoninergic receptor (5-HT(2A)R) stimulation with psilocybin in healthy humans
207 at the class A serotonin 5-HT(2A) receptors (5-HT(2A)Rs) affected the localization and trafficking of
209 ents in heteromeric 5-HT type 3AB receptors (5-HT(3AB)Rs) (IC(50) = 840 and 526 muM, respectively).
210 vation of serotonin (5-HT) type 4 receptors (5-HT(4)Rs) has been shown to have anxiolytic effects in
213 ecause 5-HT(2B) mediates clinically relevant 5-HT-related pathologies (valvular heart disease, pulmon
214 12 to potentiate the effects of a selective 5-HT(2C)R agonist was established in a drug discriminati
215 ed to obtain PZ-1361, a potent and selective 5-HT(7) receptor antagonist, with antidepressant propert
216 of hemodynamics, we implanted serotonergic (5-HT(+)) neuron-enriched embryonic raphe nucleus-derived
217 Here, we showed that the class A serotonin 5-HT(2A) receptors (5-HT(2A)Rs) affected the localizatio
218 ed up-regulation of frontal cortex serotonin 5-HT(2A) receptor (5-HT(2A)R) density in the adult offsp
219 MT(2) receptors and G(q) -coupled serotonin 5-HT(2C) receptors, in which melatonin transactivates ph
220 high affinity and selectivity for serotonin 5-HT(1A) receptors were obtained and tested in four func
226 ed with altered dopamine (DA) and serotonin (5-HT) functioning, the current study aimed to elucidate
229 gnaling-such as dopamine (DA) and serotonin (5-HT)-have been independently detected in psychiatric di
230 tudies indicate that antagonizing serotonin (5-HT) type 3AB (5-HT(3AB)) receptors in brain areas invo
231 eroendocrine signalling compound, serotonin (5-HT), is important for regulating peristaltic motion, f
232 ransmitters, i.e., dopamine (DA), serotonin (5-HT), epinephrine (Epn), and norepinephrine (Norepn), u
235 translate environmental cues into serotonin (5-HT) production, contributing to intestinal physiology.
237 e binding of the neurotransmitter serotonin (5-HT) into a transient cation current that mediates fast
238 raphe nucleus, the main source of serotonin (5-HT) in the mammalian brain, and excessive 5-HT signali
240 recordings, and iontophoresis of serotonin (5-HT) receptor antagonists in the mouse visual cortex.
242 cantly increased plasma levels of serotonin (5-HT), and serotonin molecule and SCA plasma induced neu
244 zone, markedly reduced placental serotonin (5-HT) concentrations, and lowered 5-HT GC immunoreactivi
245 SPAN5 were associated with plasma serotonin (5-HT) concentrations which were themselves associated wi
246 nificantly associated with plasma serotonin (5-HT) concentrations, which were themselves associated w
248 grees of conformational change in the setron-5-HT(3A)R structures, throughout the channel and particu
251 tal cortex (mPFC), as opposed to the somatic 5-HT(1A) autoreceptor, has been shown to play a critical
259 axis in human macrophages and indicate that 5-HT potentiates the activity of a transcription factor
260 l modeling-based fMRI analyses revealed that 5-HT depletion altered social reward prediction signals
261 ecific agonists and antagonist revealed that 5-HT(2B) engagement modifies the cytokine and gene signa
263 on modulator N-acetyl cysteine (NAC) and the 5-HT(1B/1D/1F) receptor agonist eletriptan to normalise
265 ights into modulation of CeA activity by the 5-HT system and unravels the vulnerability of the CeA 5-
268 on in the mPFC, and provide evidence for the 5-HT(1A) receptor as a target for the treatment of MDD.
269 that heteromerization was necessary for the 5-HT(2A)R-dependent effects on mGluR2 subcellular distri
272 results show that intra-mPFC infusion of the 5-HT(1A) receptor agonist 8-OH-DPAT induces rapid and lo
273 In particular, selective stimulation of the 5-HT(1A) receptor in the medial prefrontal cortex (mPFC)
275 with spatial gene expression patterns of the 5-HT(2A) (5-hydroxytryptamine 2A) and 5-HT(1A) (5-hydrox
278 Using a simplified model of the pore of the 5-HT(3) receptor (5HT3R) which restrains the backbone st
279 identify a 24-amino-acid-long segment of the 5-HT(3A)-ICD as a molecular determinant for the interact
280 T(2A)/mGlu(2) receptor complex, based on the 5-HT(2A) antagonist MDL-100,907 and the mGlu(2) ago-PAM
281 synthesized monovalent ligands retained the 5-HT(2A) antagonist and mGlu(2) ago-PAM functionalities,
282 Previously, we have demonstrated that the 5-HT(3A)-ICD is required for the interaction between 5-H
283 ylactics against stress, suggesting that the 5-HT(4)R may be a novel target for prophylactic drug dev
284 ion of AhR target genes in M-MO and that the 5-HT-mediated activation of AhR is 5-HT(2B) dependent be
286 eritoneally) or intra-mPFC infusion with the 5-HT(4)R agonist, RS67333 (0.5 mug/side), were examined
291 odes exhibit higher sensing activity towards 5-HT in accordance to its higher surface area, lower par
294 the predominance of SMN-SN activity, whereas 5-HT signaling favors the predominance of DMN activity,
295 anti-inflammatory functions in M-MO, whereas 5-HT(2B) prevents the degeneration of spinal cord mononu
298 uorescence showed ERICH3 colocalization with 5-HT in vesicle-like structures, and ERICH3 knock-out dr
299 cation of bupropion or hydroxybupropion with 5-HT dose dependently inhibited 5-HT-induced currents in
300 the expression of serotonin receptors, with 5-HT(2B) and 5-HT(7) expression restricted to M-CSF-prim