ライフサイエンスコーパス: 5-HT3 receptor

1 ory responses through ligand-gated channels (5-HT3 receptors).

2 ding preferentially to the open state of the 5-HT3 receptor.

3 em acts by causing open-channel block of the 5-HT3 receptor.

4 sis (CoMFA) is applied to antagonists of the 5-HT3 receptor.

5 of agonists to the desensitized form of the 5-HT3 receptor.

6 species variation in the pharmacology of the 5-HT3 receptor.

7 brane and carboxyl-terminal domains from the 5-HT3 receptor.

8 r is the best-characterized heteropentameric 5-HT3 receptor.

9 loop and the critical role of Pro 8* in the 5-HT3 receptor.

10 nd 31 units, respectively, by activating the 5-HT3 receptors.

11 and is an antagonist of serotonin 5-HT2 and 5-HT3 receptors.

12 receptor subunit (5-HT3A) yields functional 5-HT3 receptors.

13 e nerve responses apparently by blocking the 5-HT3 receptors.

14 se and differential expression of 5-HT1A and 5-HT3 receptors.

15 neuronal activation in the DVC by activating 5-HT3 receptors.

16 Extrinsic nerves are activated by 5-HT3 receptors.

17 ediated by 5-HT in the colonic mucosa and by 5-HT3 receptors.

18 ction is not clear and may involve hindbrain 5-HT3 receptors.

19 ze a 5-HT-containing pathway which activates 5-HT3 receptors.

20 alterations in the neuronal distribution of 5-HT3 receptors.

21 holecystokinin A receptors and serotonin via 5-HT3 receptors.

22 s high-affinity CCK-A receptors also express 5-HT3 receptors.

23 nly high- or low-affinity CCK-A receptors or 5-HT3 receptors.

24 may also be responsive to serotonin through 5-HT3 receptors.

25 ch activates an inhibitory pathway involving 5-HT3 receptors.

26 f 5-HT receptors, including the 5-HT type-3 (5-HT3) receptors.

27 d at 20 degrees or when an antagonist of the 5-HT3 receptor, [3H]granisetron, was used as the radioli

28 The 5-HT3 receptor (5-HT3R) antagonist Alosetron (Alos) redu

29 permeability seen in native and recombinant 5-HT3 receptor (5-HT3R) channels, we reported previously

30 The kinetics of desensitization of the 5-HT3 receptor (5-HT3R)-gated ion channel were investiga

31 spinal dorsal horn via activation of spinal 5-HT3 receptors (5-HT3Rs).

32 ave the capacity to synthesize two different 5-HT3 receptors, 5-HT3A+/3B- and 5-HT3A+/3B+ receptors.

33 of the 5-HT3A receptor subunit rendered the 5-HT3 receptor 70-fold more sensitive to serotonin and p

34 st channel conductance displayed by neuronal 5-HT3 receptors (9-17 pS).

35 ond messenger pathways, or to the ionotropic 5-HT3 receptor, a non-selective cation channel that medi

36 bout PKC modulation of the serotonin type 3 (5-HT3) receptor, a ligand-gated membrane ion channel tha

37 I cells activates gustatory nerve fibers via 5-HT3 receptors, accounting for a significant proportion

38 m, these results suggest that stimulation of 5-HT3 receptors activates an intracellular signalling ca

39 ate in the inhibition of aggression, whereas 5-HT3 receptor activation facilitates aggression, the au

40 This excitatory response to 5-HT3 receptor activation may be partly a direct postsyn

41 tamine (5-HT)1A receptors and facilitated by 5-HT3 receptor activation.

42 of descending serotonergic pathways or tonic 5-HT3 receptor activity in maintaining hypersensitivity

43 Pretreatment of ganglia with the 5-HT3 receptor agonist 1-m-(chlorophenyl) biguanide (m-C

44 ione (DNQX) on the excitatory actions of the 5-HT3 receptor agonist 1-phenylbiguanide (PBG) were stud

45 Only the 5-HT3 receptor agonist altered the quality of the lordos

46 A 5-HT3 receptor agonist CPBG (1 microM), mimicked the unm

47 that phenyldiguanide (later recognized as a 5-HT3 receptor agonist) stimulated the firing of C-fibre

48 This initial response was mimicked by the 5-HT3 receptor agonist, 2-methyl-5-HT, whereas 5-methoxy

49 sed with the 5-HT1A receptor agonist and the 5-HT3 receptor agonist, m-chlorophenyl-biguanide (mCPBG;

50 The 5-HT3 receptor agonist, m-chlorophenylbiguanide (mCPBG),

51 retic application of PBG, a highly selective 5-HT3 receptor agonist, significantly increased activity

52 2-methylserotonin (100 microg kg-1, i.a.), a 5-HT3 receptor agonist, stimulated eleven of twelve affe

53 data are consistent with the hypothesis that 5-HT3 receptor agonists activate DVMN neurones partly by

54 urrent by low concentrations of bath-applied 5-HT3 receptor agonists is compatible with the cyclic mo

55 The effects of 5-HT3 receptor agonists on cortical circuit response pro

56 The rank order of potency of all the 5-HT3 receptor agonists tested in the PI assay as compar

57 The effect was mimicked by two other 5-HT3 receptor agonists, 2-methyl-5-HT and m-chloropheny

58 by white matter stimulation were reduced by 5-HT3 receptor agonists, whereas the frequency of sponta

59 With the exception of the 5-HT3 receptor, all of the cloned serotonin receptors be

60 Neuronal 5-HT3 receptors also display a permeability to calcium i

61 n the basis of its ability to inactivate the 5-HT3 receptor, an excitatory serotonin-gated ion channe

62 sion of the functional 5-HT3A subunit of the 5-HT3 receptor and the central CB1 cannabinoid receptor

63 erents, mainly through direct stimulation of 5-HT3 receptors and that the action of 5-HT on these aff

64 allosteric regulation of agonist binding to 5-HT3 receptors and the first example of a ligandgated i

65 ether gustatory afferents express functional 5-HT3 receptors and, if so, whether these receptors play

66 -application of 5-HT (300 microM), acting at 5-HT3 receptors, and ACh (3 mM) or ATP (1 mM) were addit

67 ors, 5-hydroxytryptamine (serotonin) type 3 (5-HT3) receptors, and a chimeric receptor constructed fr

68 Aprepitant, a 5-HT3 receptor antagonist (5HT3-RA), and dexamethasone a

69 Similar pretreatment with the 5-HT3 receptor antagonist 3-tropanyl-3,5-dichlorobenzoat

70 kg-1, i.v.), or treatment with the selective 5-HT3 receptor antagonist alosetron (30 microg kg-1, i.v

71 Although tropisetron is a 5-HT3 receptor antagonist and an alpha7nAChR partial ago

72 1) receptor antagonist in conjunction with a 5-HT3 receptor antagonist and corticosteroid in patients

73 Rolapitant in combination with a 5-HT3 receptor antagonist and dexamethasone is well tole

74 Rolapitant in combination with a 5-HT3 receptor antagonist and dexamethasone is well-tole

75 isetron; 500 ng), or were coinfused with the 5-HT3 receptor antagonist and the 5-HT2A/2C receptor ago

76 o 3.8 +/- 1.1 spikes s(-1)) by the selective 5-HT3 receptor antagonist granisetron.

77 coefficient = 1.8) that were blocked by the 5-HT3 receptor antagonist ondansetron (IC50 = 103 pM) an

78 led to do so in Tph1(-/-) colon; and (9) the 5-HT3 receptor antagonist ondansetron, which reduced CMM

79 ivity effect of intrathecal injection of the 5-HT3 receptor antagonist ondansetron.

80 otetralin (DPAT; 0.1 mg/kg and 0.3 mg/kg) or 5-HT3 receptor antagonist tropisetron (0.3 mg/kg) treatm

81 d Fos-LI in the DVC of ondansetron (1 mg/kg; 5-HT3 receptor antagonist) and vehicle-treated rats foll

82 Rats were infused with the 5-HT3 receptor antagonist, 3-tropanyl-indole-3 carbonyla

83 A combination of aprepitant, a 5-HT3 receptor antagonist, and dexamethasone is recommen

84 combination of an NK1 receptor antagonist, a 5-HT3 receptor antagonist, and dexamethasone.

85 ICS205-930 (1 microM), a 5-HT3 receptor antagonist, completely blocked the 5-HT-i

86 -HT response was completely abolished by the 5-HT3 receptor antagonist, granisetron (0.5 mg kg-1).

87 njection of tropisetron (200 microg kg-1), a 5-HT3 receptor antagonist, significantly attenuated the

88 fusions with 100 ng, 250 ng or 500 ng of the 5-HT3 receptor antagonist, tropisetron.

89 was less affected by VMN infusions with the 5-HT3 receptor antagonist.

90 and 5-HT4 receptor antagonists, but not by a 5-HT3 receptor antagonist.

91 urthermore, this mutation also converted the 5-HT3 receptor antagonist/very weak partial agonist, apo

92 rolapitant, in combination with a serotonin (5-HT3) receptor antagonist and dexamethasone, for the pr

93 f ondansetron, a selective serotonin type-3 (5-HT3) receptor antagonist, attenuates cholecystokinin (

94 rotonin and this effect was blocked with the 5-HT3-receptor antagonist ondansetron.

95 ) and palonosetron (a 5-hydroxytryptamine-3 [5-HT3] receptor antagonist) for the prevention of acute

96 wide dynamic range neurons are inhibited by 5-HT3 receptor antagonists in rats following spinal nerv

97 whisking frequencies, and selective 5-HT2 or 5-HT3 receptor antagonists suppress this rhythmic firing

98 Unilateral infusion of selective 5-HT2 or 5-HT3 receptor antagonists suppresses ipsilateral whiski

99 by DPPIV inhibition or by cholecystokinin or 5-HT3 receptor antagonists, but was inhibited by atropin

100 nged efficacy, and acts synergistically with 5-HT3 receptor antagonists.

101 The 5-HT3 receptor "antagonists' (+)-tubocurarine and quipaz

102 The 5-HT3 receptors are serotonin-gated ion channels that ph

103 5-hydroxytryptamine type 3 (5-HT3) receptors are cation-selective transmitter-gated

104 5-hydroxytryptamine type 3 (5-HT3) receptors are members of the Cys-loop receptor su

105 Serotonin type 3 (5-HT3) receptors are members of the pentameric Cys-loop

106 t likely to be due to a direct action on the 5-HT3 receptor as it could be recorded using intracellul

107 yonic kidney 293 cells stably expressing the 5-HT3 receptor As subunit, (+)-verapamil, (-)-verapamil,

108 o membranes from Sf9 cells infected with the 5-HT3 receptor As subunit, [3H]mCPBG and [3H]granisetron

109 yonic kidney 293 cells stably expressing the 5-HT3 receptor As subunit, similar concentrations of the

110 be the role of two residues in loop A of the 5-HT3 receptor: Asn128 and Glu129.

111 gle-channel conductance of human recombinant 5-HT3 receptors assembled as homomers of 5-HT3A subunits

112 us, the data support a modified model of the 5-HT3 receptor binding site and show that loop A plays a

113 143, Tyr153, and Tyr234), which dominate the 5-HT3 receptor binding site.

114 We report that recombinantly expressed 5-HT3 receptor binding sites are reduced by chronic expo

115 hese physiologic data, the effects of spinal 5-HT3 receptor blockade on behavioral hypersensitivity a

116 Second, we examined the effects of hindbrain 5-HT3 receptor blockade on suppression of intake by syst

117 The efficacy of a new 5-HT3 receptor blocking drug in the treatment of the dia

118 of the SCG of the rat requires activation of 5-HT3 receptors both for induction and maintenance.

119 work not only unveils the mechanism by which 5-HT3 receptors can reach their axonal localization requ

120 Thus, presynaptic 5-HT3 receptors containing the 5-HT3B subunit might be p

121 Activation of the 5-HT3 receptor decreased the amplitude and lateral exten

122 Also, 5-HT3 receptor density was greater in H-Agg hamsters wit

123 el lining, but may play an important role in 5-HT3 receptor desensitization.

124 n-selective 5-HT agonist devoid of action at 5-HT3 receptors, did not (n = 18).

125 y and selectivity for peripheral and central 5-HT3 receptors) dose-dependently stimulated PI turnover

126 However, pre-blockade of 5-HT3 receptors eliminated the influence of the antibody

127 udy the mechanism of alcohol potentiation of 5-HT3 receptor function and to analyse effects of alcoho

128 m the site through which nimodipine inhibits 5-HT3 receptor function.

129 A human recombinant homo-oligomeric 5-HT3 receptor (h5-HT3A) expressed in a human embryonic

130 alter the density of serotonergic fibers or 5-HT3 receptor immunoreactivity or spinal tissue content

131 rons in human intestine and 5-HT4/5-HT1P and 5-HT3 receptors in guinea pig colon.

132 anaesthetized rats investigated the role of 5-HT3 receptors in modulating vagal afferent evoked acti

133 tribution consistent with the involvement of 5-HT3 receptors in modulation of both presynaptic releas

134 current experiment, a potential role for VMN 5-HT3 receptors in the control of lordosis behavior was

135 vations emphasize the potential role for VMN 5-HT3 receptors in the control of lordosis behavior.

136 s, that 5-HT2A receptors are segregated from 5-HT3 receptors in the macaque cerebral cortex.

137 Unlike its action on the 5-HT3 receptors in the periphery or cultured cell lines,

138 ventromedial medulla and the contribution of 5-HT3 receptors in the trigeminal nucleus caudalis (Vc),

139 Pharmacological blockade of 5-HT3 receptors in vivo or genetic deletion of the 5-HT3

140 amine2A receptors and the ion-channel gating 5-HT3 receptors, in cortical neuron types, which control

141 receptor were limited, the broad effects of 5-HT3 receptor included repetitive and impulsive element

142 This is confirmed for 5-HT3 receptor-induced contractions in the guinea pig il

143 d butanol (ButOH) had similar effects on the 5-HT3 receptor-induced current.

144 ugh serotonin, acting on facilitatory spinal 5-HT3 receptors, influences the final expression of DNIC

145 tivity because the endogenous ligand for the 5-HT3 receptor is a hydroxylated derivative of tryptopha

146 The 5-HT3 receptor is a member of the Cys-loop ligand-gated

147 The 5-HT3 receptor is a transmitter-gated ion channel of the

148 The type 3 serotonin (5-HT3) receptor is the only ligand-gated ion channel rec

149 Antagonism of 5-HT3 receptors known to promote learning significantly

150 combined with a new model of the nonliganded 5-HT3 receptor, lead to a mechanistic explanation of the

151 These data demonstrate that 5-HT3 receptors located in the medial NTS participate in

152 partmentalized structural composition of the 5-HT3 receptor may be the basis of functional diversity

153 ents through a serotonin receptor (subtype 3,5-HT3 receptor) mechanism, before treatment with the ant

154 Therefore, we hypothesized that 5-HT3 receptors mediate CCK-induced Fos-LI in the dorsal

155 The inhibition of the 5-HT3 receptor mediated inward current by low concentrat

156 To determine the relevant sites for 5-HT3 receptor mediated transmission in this region, we

157 This study suggests that alcohols potentiate 5-HT3 receptor-mediated current by both increasing the r

158 Here, we show that PKC potentiated 5-HT3 receptor-mediated current in Xenopus oocytes expre

159 Ca2+, and Mg2+ concentrations on 5-HT2- and 5-HT3 receptor-mediated depolarizations of the resting m

160 5-HT3 receptor-mediated ion current was recorded from NC

161 In contrast, ethanol potentiated 5-HT3 receptor-mediated responses at low agonist concent

162 The magnitude of the ethanol potentiation of 5-HT3 receptor-mediated responses decreased with increas

163 The exact location of 5-HT3 receptors mediating this action is not clear and m

164 iously, we have shown that serotonin type-3 (5-HT3) receptor mediation of suppression of food intake

165 the mid-to-caudal regions of the NTS and AP, 5-HT3 receptors most significantly mediate neuronal acti

166 ung-specific jugular neurons did not express 5-HT3 receptor mRNA but frequently expressed 5-HT1 or 5-

167 trogradely labelled from the lung, expressed 5-HT3 receptor mRNA.

168 T to inappropriate sites in IBS may activate 5-HT3 receptors on extrinsic afferent fibers and motor n

169 lucose regulates the density and function of 5-HT3 receptors on gastric vagal afferent neurones.

170 th the antibody in another group, we blocked 5-HT3 receptors on sensory nerve endings with tropisetro

171 ine have been defined as partial agonists of 5-HT3 receptors on the basis of macroscopic measurements

172 c) tastants and this released 5-HT activates 5-HT3 receptors on the gustatory nerves.

173 intestinal enterochromaffin cells activates 5-HT3 receptors on vagal afferent fibres to mediate lumi

174 al enterochromaffin cells, which acts on the 5-HT3 receptors on vagal afferent fibres to stimulate va

175 rt latency, transient excitation mediated by 5-HT3 receptors, or a delayed onset, more prolonged effe

176 This raises the possibility that 5-HT3 receptors participating in sympathetic, parasympat

177 The pharmacological characterisation of 5-HT3 receptor recognition sites in homogenates of pig c

178 receptors in vivo or genetic deletion of the 5-HT3 receptors reduces taste nerve responses to acids a

179 nic acetylcholine receptor and the serotonin 5-HT3 receptor, respectively.

180 In cells exhibiting a 5-HT3 receptor response, 5-HT and 2-methyl-5-HT produced

181 s to recommend the two-drug combination of a 5-HT3 receptor serotonin antagonist and dexamethasone.

182 The three-drug combination of a 5-HT3 receptor serotonin antagonist, dexamethasone, and

183 s of muscarinic, AMPA, NMDA, GABAA, ATP, and 5-HT3 receptors, spontaneous and evoked postsynaptic cur

184 Here we describe a new class of 5-HT3-receptor subunit (5-HT3B).

185 Uniquely, 5-HT3 receptor subunits (5-HT3A and 5-HT3B) possess a po

186 Two 5-HT3 receptor subunits have been cloned, subunit A (5-H

187 Thus, the prevalent form of 5-HT3 receptor synthesized within the CNS lacks the 5-HT

188 s mesenteric afferents by a direct action on 5-HT3 receptors that are present on vagal mucosal affere

189 final sigma-Conotoxin inactivates the 5-HT3 receptor through competitive antagonism and is a h

190 is a specific competitive antagonist of the 5-HT3 receptor; thus, alphaS-RVIIIA defines a novel fami

191 egulate directly the function and binding of 5-HT3 receptors to ondansetron.

192 d that the interaction of diltiazem with the 5-HT3 receptor was well described by a bimolecular react

193 sponses were reduced, and that the remaining 5-HT3 receptors were hypersensitive.

194 nts is activated directly via stimulation of 5-HT3 receptors, while another population responds to 5-

195 action of L-type Ca2+ channel antagonists on 5-HT3 receptors, whole-cell voltage clamp electrophysiol

196 fibers, serotonin content and the levels of 5-HT3 receptors within the spinal cord at this time poin