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1 elective, with subnanomolar affinity for the 5-HT1A receptor.
2 ike effect of D1 and possible involvement of 5-HT1A receptor.
3 intrinsic activity (E max = 26 +/- 2.0%) on 5-HT1A receptor.
4 ceptor in recombinant cells expressing human 5-HT1A receptor.
5 at serotonin is primarily acting through the 5-HT1A receptor.
6 A, gamma-aminobutyric acid (GABA)B , BZ, and 5-HT1A receptors.
7 HT to a concentration sufficient to activate 5-HT1A receptors.
8 hypothalamus and hippocampus is mediated by 5-HT1A receptors.
9 ed with the known postmortem distribution of 5-HT1A receptors.
10 ylpiperazine ([(18)F]MPPF), an antagonist of 5-HT1A receptors.
11 rotonin transporter (SERT) and serotonin 1A (5-HT1A) receptor.
12 h potency and efficacy were increased at the 5-HT(1A) receptor.
13 ilar to the agonist-induced responses of the 5-HT(1A) receptor.
14 hether protection required activation of the 5-HT(1A) receptor.
15 use and human MC respond to 5-HT through the 5-HT(1A) receptor.
16 e on the expression of the gene encoding the 5-HT(1A) receptor.
17 hereby could provide a measure of functional 5-HT(1A) receptors.
18 a high affinity (0.1 nM) and selectivity for 5-HT(1A) receptors.
19 at its main pharmacology is mediated via the 5-HT(1A) receptors.
20 sitization rather than downregulation of DRN 5-HT(1A) receptors.
21 ow produce functional desensitization of DRN 5-HT(1A) receptors.
22 eptor domains and substitutes for endogenous 5-HT(1A) receptors.
23 e designed as "biased agonists" of serotonin 5-HT(1A) receptors.
24 10 specific binding in brain regions rich in 5-HT(1A) receptors.
25 selectivity for 5-HT(2A) versus 5-HT(2C) and 5-HT(1A) receptors.
26 e first promising agonist PET tracer for the 5-HT(1A) receptors.
27 ining NMDA receptor is the primary target of 5-HT(1A) receptors.
28 t inhibited by activation of the 5-HT(5A) or 5-HT(1A) receptors.
29 ng in CHO cells expressing the serotonin-1A (5-HT(1A)) receptor.
34 paring Smo with the 5-hydroxytryptamine(1A) (5-HT(1A)) receptor, a quintessential G(i)-coupled recept
35 the lipid dependence of the human serotonin 5-HT1A receptor, a GPCR that is central to neuronal func
37 to reveal the motivational mechanism whereby 5-HT(1A) receptor activation modulates drinking behavior
42 his study, we radiolabeled the high-affinity 5-HT(1A) receptor agonist (18)F-F13714 and investigated
43 n of caudal MR serotonergic neurons with the 5-HT(1A) receptor agonist (R)-(+)-8-hydroxy-2(di-n-propy
44 xetine attenuated hypothermia induced by the 5-HT(1A) receptor agonist 8-hydroxy-2-(di-n-propylamino)
45 thesis using bilateral microperfusion of the 5-HT(1A) receptor agonist 8-hydroxy-2-(di-n-propylamino)
47 results show that intra-mPFC infusion of the 5-HT(1A) receptor agonist 8-OH-DPAT induces rapid and lo
49 he effect of citalopram, whereas exposure to 5-HT(1A) receptor agonist only moderately influenced mal
50 s were used to test the possibility that the 5-HT(1A) receptor agonist, 8-hydroxy-2-(di-N-propylamino
52 receptor agonist, apomorphine (APO) and the 5-HT(1A) receptor agonist, 8-OHDPAT (8OH) in a low dose
54 tested for behavior under effective doses of 5-HT1A receptor agonist 8-hydroxy-N, N-dipropyl-2-aminot
55 ted following systemic administration of the 5-HT1A receptor agonist, 8-OH-DPAT, the D2 receptor anta
60 t years, new chemical entities targeting the 5-HT(1A) receptor (alone or in combination with other mo
62 h K(i) values of approximately 30 nM for the 5-HT(1A) receptor and K(i) values of 5 and 0.5 nM for th
63 series possessed high affinity for the human 5-HT(1A) receptor and many displayed potent antagonist a
64 mal binding) of ((3)H)-WAY 100635 binding to 5-HT(1A) receptors and ((3)H)-ketanserin binding to 5-HT
65 eir in vitro pharmacological profile at both 5-HT(1A) receptors and alpha(1)-adrenoceptor subtypes wa
66 er, curcumin treatment, via up-regulation of 5-HT(1A) receptors and BDNF, may reverse or protect hipp
68 ose dependent manner, while binding to D(3), 5-HT(1A) receptors and SERT was not detectable with the
70 Further investigation into the role of the 5-HT1A receptor and the potential of [11C]-WAY100635 PET
71 bited these cells directly via activation of 5-HT1A receptors and indirectly via enhanced GABA releas
72 measured in brain is dominated by binding to 5-HT1A receptors and to reveal the extent of defluorinat
73 receptors, direct or indirect stimulation of 5-HT(1A) receptors, and to a lesser extent, reduction in
75 profile of 5-HT(1A-1D) and 5-HT2 receptors, 5-HT1A receptors, and the serotonin (5-HT) transporter (
76 ing of pallidal neurons through postsynaptic 5-HT1A receptors; and (3) 5-HT postsynaptically excites
77 a and 4ccis emerged as novel and interesting 5-HT(1A) receptor antagonist (pK(i) = 8.70) and a 5-HT(1
78 n of fluoxetine (Prozac), others receiving a 5-HT(1A) receptor antagonist (WAY 100,635; Sigma, St. Lo
79 at the dosages used in this experiment, the 5-HT(1A) receptor antagonist WAY 100,635 may have positi
82 by pretreatment with WAY-100635, a serotonin 5-HT(1A) receptor antagonist, in DAT-KO mice, but the dr
84 nists (8-OH-DPAT, F13714 and F15599) and one 5-HT1A receptor antagonist (MPPF) were compared in terms
86 nduced increase in social behaviors, while a 5-HT1A receptor antagonist did not alter affiliative voc
87 infused with WAY100635 (400 to 2000 ng), the 5-HT1A receptor antagonist did not facilitate lordosis r
90 ntagonist SB 216641 (10 microM), but not the 5-HT1A receptor antagonist WAY 100635 (10 microM) or the
91 y 8-OH-DPAT persisted in the presence of the 5-HT1A receptor antagonist WAY-100635, was abolished by
92 antagonist), WAY-100635 (selective serotonin 5-HT1A receptor antagonist) as well as monoamine oxidase
94 contribute to propranolol's action since the 5-HT1A receptor antagonist, (S)-WAY 100135 (P = 0.2), an
95 n emission tomography imaging and a specific 5-HT1A receptor antagonist, [carbonyl-11C]WAY-100635.
96 5-HT2C receptor antagonist, SB242084, or the 5-HT1A receptor antagonist, WAY-100635, and were tested
98 tative differences in the mechanisms whereby 5-HT(1A) receptors are able to inhibit stimulation of ad
100 ypercapnia, but not to hypoxia, and that MRR 5-HT1A receptors are also involved in thermoregulation a
104 ally interesting to consider and justify the 5-HT(1A) receptor as a new attractive target for drug di
105 on in the mPFC, and provide evidence for the 5-HT(1A) receptor as a target for the treatment of MDD.
106 g and is a partial agonist for the serotonin 5-HT(1A) receptors as well as possessing low affinity an
107 hippocampus while increasing the efficacy of 5-HT1A receptors as measured by agonist-stimulated [35S]
108 pharmacology showed that focal activation of 5-HT1A receptors at the axon initial segment (AIS), but
111 MAO-A activity were associated with greater 5-HT(1A) receptor availability in women, but not in men.
112 we investigated the relationship between DRN 5-HT1A receptor availability and amygdala reactivity to
113 processing and the relationship between DRN 5-HT1A receptor availability and amygdala reactivity.
119 found between 5-HT neuron count or density, 5-HT(1A) receptor binding density, or 5-HTT receptor bin
120 HT neurons, there was a decrease with age in 5-HT(1A) receptor binding in the SIDS cases but no chang
122 as well as a significantly lower density of 5-HT(1A) receptor binding sites (P<or=.01 for all 9 nucl
127 exception of the hypoglossal nucleus, where 5-HT1A receptor binding increases while SERT binding rem
132 an age, 25.1 +/- 5.8 years).Intervention The 5-HT1A receptor binding was measured using positron emis
133 hey exhibit reduced 5-HT neuron activity and 5-HT1A receptor binding with varying changes in postsyna
136 gonism at trace amine receptor 1 (TAAR1) and 5-HT(1A) receptors but no appreciable action at dopamine
138 nsitivity, suggesting that Rh-CT(5-HT1A) and 5-HT(1A) receptors compete to interact with the same tra
139 A receptor protomer in the hippocampal FGFR1-5-HT1A receptor complex enhancing the FGFR1 signaling.
140 r receptor 1 (FGFR1)-5-hydroxytryptamine 1A (5-HT1A) receptor complexes have been demonstrated and th
147 ssion tomography (PET) for quantification of 5-HT(1A) receptor densities in the living brains of Alzh
148 compromises the accuracy of measurements of 5-HT1A receptor densities in adjacent areas of brain bec
150 esearch with PET for measuring serotonin 1A (5-HT1A) receptor densities in brain regions of human sub
154 TM4/TM5 can form an interaction interface in 5-HT(1A) receptor dimers and indicates that specific ami
155 inding in rats was consistent with the known 5-HT(1A) receptors distribution (hippocampus and cortica
156 ) F-Mefway therefore may be used to quantify 5-HT1A receptor distribution in brain regions for the st
157 G protein-coupled receptor that targets into 5-HT(1A) receptor domains and substitutes for endogenous
158 titive control of Gi/o pathway activation in 5-HT1A receptor domains in the dorsal raphe nucleus (DRN
159 ic alpha1 and alpha2 receptors; serotonergic 5-HT1A receptors; dopaminergic D1/5 receptors by using q
164 l polymorphism in the promoter region of the 5-HT(1A) receptor gene is associated with depression and
165 orphism in the promoter of the serotonin-1A (5-HT(1A)) receptor gene in increased susceptibility to d
167 activities at both the 5-HT transporter and 5-HT1A receptor, good selectivity over the alpha1-adrene
168 of the serotonin 1A (5-hydroxytryptamine 1A [5-HT(1A)]) receptor has been widely used in clinical stu
169 results reveal the broad dependence that the 5-HT1A receptor has on plasma membrane properties, demon
170 tonergic system, including the serotonin 1A (5-HT(1A)) receptor, has been implicated in the pathophys
171 5-HT1A receptors in line with evidence that 5-HT1A receptors have a role in mediating emotional proc
174 -HT1A autoreceptors by being part of a FGFR1-5-HT1A receptor heterocomplex in the midbrain raphe 5-HT
175 e cells, evidence for the existence of FGFR1-5-HT1A receptor heterocomplexes in the dorsal and median
176 that CaM binding and phosphorylation of the 5-HT(1A) receptor i3 loop peptides by protein kinase C a
177 (18) F-Mefway appears to be an effective 5-HT1A receptor imaging agent in all models, including h
178 uptake and, in turn, its spillover on brain 5-HT1A receptor imaging were assessed by PET with venous
179 gh the authors observed a greater density of 5-HT1A receptor immunoreactivity in H-Agg hamsters withi
180 2A), serotonin 2C (5-HT2C) and serotonin 1A (5-HT1A) receptors, implicated in the development of anxi
181 modulin (CaM) co-immunoprecipitates with the 5-HT(1A) receptor in Chinese hamster ovary fibroblasts.
182 tered serotonin transmission by means of the 5-HT(1A) receptor in dysfunction of prefrontal cortex py
183 onfirming the requirement for activating the 5-HT(1A) receptor in initiating this survival pathway.
184 also observed an increased expression of the 5-HT(1A) receptor in ipsapirone-treated control neurons.
185 transfer to show that CaM interacts with the 5-HT(1A) receptor in living cells, representing the firs
187 s of each receptor, Smo is equivalent to the 5-HT(1A) receptor in the assay as it relates to capacity
189 In particular, selective stimulation of the 5-HT(1A) receptor in the medial prefrontal cortex (mPFC)
190 sults indicate that selective stimulation of 5-HT(1A) receptor in the mPFC exerts rapid and sustained
191 tomography and [(11)C]WAY-100635 to quantify 5-HT(1A) receptors in a group of 31 healthy and unmedica
192 eased [(11)C]CUMI-101 BP(ND) at postsynaptic 5-HT(1A) receptors in several cortical regions, but ther
195 adiotracer for PET experiments examining the 5-HT1A receptor in neuropsychiatric disorders and drug i
196 rements show simultaneous trafficking of the 5-HT1A receptor in two distinct endosomal recycling path
200 rsive stimuli and that this is linked to DRN 5-HT1A receptors in line with evidence that 5-HT1A recep
201 of DA D2 receptors in mPFC or activation of 5-HT1A receptors in OFC increases impulsive choice in th
202 ial of 18F-FCWAY to act as a radioligand for 5-HT1A receptors in rat brain and also revealed extensiv
204 e as an effective platform for investigating 5-HT1A receptors in rodent models of neuropsychiatric co
205 e influence of pharmacological activation of 5-HT1A receptors in specific brain regions, this neuroim
206 Finally, we demonstrate that activation of 5-HT1A receptors in the dBNST is necessary for the anxio
207 r the results suggest that the activation of 5-HT1A receptors in the DRN results from the local relea
208 hat serotonin signaling through postsynaptic 5-HT1A receptors in the hippocampus is critical for the
211 hypothalamus of SERT knock-out mice restored 5-HT1A receptors in the medial hypothalamus; this effect
212 support earlier findings that activation of 5-HT1A receptors in the mediobasal hypothalamus inhibits
213 f research have implicated the serotonin 1A (5-HT1A) receptor in major depressive disorder (MDD).
214 ed decreased density of 5-hydroxytryptamine (5-HT1A) receptors in the hypothalamus, amygdala, and dor
215 or the serotonin 1A (5-hydroxytryptamine 1A [5-HT1A]) receptor in recombinant cells expressing human
216 etine persistently upregulated SERT, but not 5-HT1A receptors, in both the neocortex and the hippocam
221 Here we show that serotonin, by activating 5-HT(1A) receptors, inhibited NMDA receptor-mediated ion
222 e feedback onto receptor cells by activating 5-HT(1A) receptors, inhibiting taste-evoked Ca(2+) mobil
223 previous study has shown that activation of 5-HT(1A) receptors inhibits N-methyl-D-aspartate (NMDA)
226 further demonstrate that tonic activation of 5-HT1A receptors is not responsible for the absence of s
230 d chronic stimulant effects of cocaine using 5-HT1A receptor ligands in autoreceptor preferring doses
237 r 1 (TAAR1) and 5-hydroxytryptamine type 1A (5-HT(1A)) receptors, may represent a new class of psycho
240 sis that the 5-HT(7) but not the 5-HT(5A) or 5-HT(1A) receptors mediate serotonergic phase shifts.
241 ver, the detailed mechanisms underlying mPFC 5-HT(1A) receptor-mediated antidepressant-like effects a
242 m, we provide the first reported profile for 5-HT(1A) receptor-mediated ERK activation using a panel
243 e, but not controllable, tail shock impaired 5-HT(1A) receptor-mediated inhibition of DRN neuronal fi
244 potential significance of these findings to 5-HT(1A) receptor-mediated inhibition of female rat lord
247 ted depolarization and the appearance of the 5-HT1A receptor-mediated hyperpolarization appears to re
248 hesis in mouse DRN brain slices by recording 5-HT1A receptor-mediated inhibitory postsynaptic current
249 n slices evoked serotonin release produced a 5-HT1A receptor-mediated inhibitory postsynaptic current
250 Here we used computational modeling of the 5-HT(1A) receptor monomer and dimer to predict residues
252 ty, we investigated the impact of activating 5-HT1A receptors on post-C5 SCI respiratory dysfunction.
253 1A) receptor antagonist (pK(i) = 8.70) and a 5-HT(1A) receptor partial agonist (pK(i) = 9.25, pD(2) =
256 study provides class III evidence that both 5-HT(1A) receptor PET and CMRglc PET can contribute to t
257 a possible role for CaM in the regulation of 5-HT(1A) receptor phosphorylation and desensitization.
259 s demonstrate that serotonin, acting through 5-HT1A receptors, plays an excitatory role in forelimb m
260 ntributions of various pre- and postsynaptic 5-HT1A receptor populations to the behavioral effects of
261 lateral and medial parts of the CeA whereas 5-HT(1A) receptor positive neurones were located mainly
264 y, in part, be mediated by activation of the 5-HT1A receptor protomer in the hippocampal FGFR1-5-HT1A
266 results demonstrate that medial hypothalamic 5-HT1A receptors regulate stress responses and locomotor
271 ution of Rh-CT(5-HT1A) resembles that of the 5-HT(1A) receptor; Rh-CT(5-HT1A) localizes to somatodend
274 t 5-HTTLPR effect on receptor binding at the 5-HT(1A) receptor site has been reported in humans, sugg
275 ing, potassium channels, the HTR1A(serotonin 5-HT1A receptor), SLC6A4(serotonin reuptake transporter)
276 s-carriers) to examine the relation between 5-HT(1A) receptor-specific binding and 5-HTTLPR genotype
279 ists, further evidence for the importance of 5-HT(1A) receptor stimulation in the NOR deficit produce
280 e 5-HT(2A) receptor stimulation, relative to 5-HT(1A) receptor stimulation, both of which can increas
282 t have an agonist/antagonist activity at the 5-HT(1A) receptor subtype are known to greatly potentiat
284 pathway--as during motor exercise--activated 5-HT1A receptors that decreased motoneuronal excitabilit
285 Here, we define a mechanism downstream of 5-HT1A receptors that mediates antidepressant-like behav
286 pression-related research has focused on the 5-HT1A receptor, the 5-HT1B receptor has a lesser known
287 on expression and signaling activity of the 5-HT(1A) receptor to a ligand with an intrinsic agonist
288 To evaluate the contribution of hypothalamic 5-HT1A receptors to these phenotypes of SERT knock-out m
292 high affinity and selectivity for serotonin 5-HT(1A) receptors were obtained and tested in four func
294 m being protective led to desensitization of 5-HT(1A) receptors, whereas treatments that block the be
295 omography (PET) imaging studies of serotonin 5-HT1A receptors which are implicated in various brain f
296 with an antibody against the serotonin(1A) (5-HT(1A)) receptor, which also mediates inhibitory regul
297 ferent aspects of the depolarization, and of 5-HT1A receptors, which signal the late developing hyper
298 inds selectively to the 5-hydroxytryptamine (5-HT1A) receptor, which is expressed on pyramidal neuron
299 nergic modulation of 5-hydroxytryptamine 1A (5-HT1A) receptors, which hyperpolarizes the activation r
300 e electrophysiological effects of prefrontal 5-HT1A receptors with implications for neuropsychiatric