ライフサイエンスコーパス: 5-HT(4) receptor

1 ta-arrestin-independent Erk1/2 activation by 5-HT4 receptor.

2 ng >5 h in slice recordings, mediated by the 5-HT4 receptor.

3 ng of the physiology and pharmacology of the 5-HT4 receptor.

4 ort-circuit current via submucosal 5-HT3 and 5-HT4 receptors.

5 ed that the effects of 5-HT were mediated by 5-HT4 receptors.

6 re evaluation as a PET radioligand for brain 5-HT(4) receptors.

7 3808 and thus involved 5-HT(7), 5-HT(2A) and 5-HT(4) receptors.

8 The serotonin 5-HT(4) receptor (5-HT(4)R) is coded by a complex gene t

9 w potential ligands for the brain imaging of 5-HT(4) receptors (5-HT(4)Rs) using single-photon emissi

10 Mucosal 5-HT(4) receptor activation can mediate the prokinetic a

11 genic effects of fluoxetine, indicating that 5-HT(4) receptor activation is necessary for these effec

12 activation stimulated DBS via muscarinic and 5-HT4 receptor activation.

13 induces HCO3(-) secretion via muscarinic and 5-HT4 receptor activation.

14 region that mediates the effect of enhanced 5-HT4 receptor activity and CK2 as modulator of 5-HT4 re

15 and benzimidazolone series possessed greater 5-HT4 receptor affinity than the corresponding indole an

16 ed for 5-HT(4) and 5-HT(3) receptor binding, 5-HT(4) receptor agonism in the rat tunica muscularis mu

17 we assessed whether chronic treatment with a 5-HT(4) receptor agonist (RS67333, 1.5 mg/kg/day) had ef

18 Furthermore, the 5-HT(4) receptor agonist prucalopride increases enteric

19 an NMDAR antagonist, and prucalopride (P), a 5-HT(4) receptor agonist, would have additional effects,

20 e serotonin (5-HT)2C receptor antagonists, a 5-HT4 receptor agonist, a 5-HT7 receptor antagonist, NMD

21 he 5-HT(1) (5-CT, 100 microg kg(-1), LA) and 5-HT(4) receptor agonists (SC53116, 100 microg kg(-1), L

22 Past work in naive rats showed that 5-HT(4) receptor agonists had rapid effects on depressio

23 Application of 5-HT(4) receptor agonists produced either an enhancement

24 5-HT(4) receptor agonists such as tegaserod have demonst

25 led to the development of several selective 5-HT4 receptor agonists and antagonists that may have th

26 In support, 5-HT2 and 5-HT4 receptor agonists mimicked the facilitating effect

27 ne moiety increased, the selectivity for the 5-HT4 receptor also increased.

28 We also assessed whether a 5-HT(4) receptor antagonist (GR125487, 1 mg/kg/day) coul

29 or antagonist granisetron (1 microM) and the 5-HT(4) receptor antagonist SB 204070 (100 nM) failed to

30 (SC-53606), which is a potent and selective 5-HT(4) receptor antagonist with a pA(2) value of 8.13 i

31 Therefore, the effects of a novel 5-HT(4) receptor antagonist, RS-100302, and the partial

32 e of forming hydrogen bonds showed increased 5-HT4 receptor antagonist activity.

33 5-HT4 receptor antagonist affinity was further increased

34 le-3- carboxamide) as a potent and selective 5-HT4 receptor antagonist with clinically suitable pharm

35 SB204070, a selective 5-HT4 receptor antagonist, dose-dependently reduced lumi

36 Also discovered were 5-HT(4) receptor antagonists, including imidazopyridine

37 nificantly attenuated by selective 5-HT2 and 5-HT4 receptor antagonists, but not by a 5-HT3 receptor

38 an acyclic aminoalkylene chain led to potent 5-HT4 receptor antagonists.

39 We tested the hypotheses that 5-HT(4) receptors are expressed in the colonic epitheliu

40 In humans and swine, 5-HT(4) receptors are present only in atrium.

41 teric neurogenesis; our results suggest that 5-HT(4) receptors are required postnatally for ENS growt

42 Serotonin 5-HT4 receptors are promising candidates in IBS pathophy

43 in inflamed tissue did not appear to involve 5-HT(4) receptors because the antagonist/inverse agonist

44 The 5-HT(4) receptor binding site can accommodate functional

45 DD, there was a correlation between cerebral 5-HT4 receptor binding and verbal memory (r = 0.29; P =

46 In addition, the association between 5-HT4 receptor binding and verbal memory performance in

47 outcome was the group difference in cerebral 5-HT4 receptor binding between patients with MDD and hea

48 current MDD had significantly lower cerebral 5-HT4 receptor binding than healthy controls (-7.0%; 95%

49 Results of this study show that cerebral 5-HT4 receptor binding was lower in patients with MDD th

50 th [11C]SB207145 for quantification of brain 5-HT4 receptor binding, but only the patients underwent

51 with MDD was associated with lower cerebral 5-HT4 receptor binding.

52 These results suggest that 5-HT(4) receptors can modulate GABAergic signalling bidi

53 al models that drugs acting at the serotonin 5-HT(4) receptor could finally achieve this goal.

54 , activation of 5-HT(7), but not 5-HT(2A) or 5-HT(4) receptors, elicited a robust inward current.

55 m (SNP) (rs201253747) c.*61 T > C within the 5-HT4 receptor gene HTR4 to be predominantly present in

56 MDD), and pharmacological stimulation of the 5-HT4 receptor has been associated with improved learnin

57 The 5-HT4 receptor has emerged as a new therapeutic target s

58 In the alimentary tract, stimulation of 5-HT4 receptors has a pronounced effect on smooth muscle

59 ne were studied to delineate the role of the 5-HT(4) receptor in modulating atrial electrophysiologic

60 evidence has implicated a potential role for 5-HT(4) receptors in cognition and anxiolysis.

61 ent as radioligands for the imaging of brain 5-HT(4) receptors in vivo with positron emission tomogra

62 Importantly, prolonged activation of 5-HT4 receptor in COS-7 cells or prolonged treatment of

63 rtantly, it is sufficient to overexpress the 5-HT4 receptor in the mPFC to generate mice with a simil

64 and evaluated for antagonist affinity at the 5-HT4 receptor in the rat esophagus.

65 dentifying the role of 5-hydroxytryptamine4 (5-HT4) receptors in the initiation of the peristaltic re

66 s were identified with high affinity for the 5-HT(4) receptor, including benzamide 12a (SC-53116), a

67 Stimulation of 5-HT(4) receptors increases atrial chronotropic and inot

68 The 5-HT4 receptor is a member of the seven transmembrane sp

69 The cerebral 5-HT4 receptor is a promising treatment target for memor

70 The 5-HT4 receptor is pharmacologically defined by selective

71 Here we show that the 5-HT4 receptor is regulated by CK2, at transcriptional a

72 The cerebral serotonin 4 (5-HT4) receptor is a promising novel target for treatmen

73 ons in wild-type (WT) mice and those lacking 5-HT(4) receptors [knock-out (KO)] was found to be simil

74 T4 receptor activity and CK2 as modulator of 5-HT4 receptor levels in this brain region that regulate

75 In the urinary bladder, activation of 5-HT4 receptors modulates cholinergic/purinergic transmi

76 eptor mRNA but frequently expressed 5-HT1 or 5-HT4 receptor mRNA.

77 One of the main target structures of 5-HT(4) receptors on 'cognitive and emotional' pathways

78 ing PFC functions, we examined the effect of 5-HT(4) receptors on GABA(A) receptor channels in PFC py

79 tion level, changing the enhancing effect of 5-HT(4) receptors on the amplitude of GABAergic inhibito

80 elopmentally regulated, and that 5-HT(7) and 5-HT(4) receptors play a previously unsuspected role in

81 In the heart, stimulation of atrial 5-HT4 receptors produces positive inotropy and tachycard

82 ested the hypothesis that stimulation of the 5-HT(4) receptor promotes enteric neuron survival and/or

83 ibition, whereas specific 5-HT3 (Y-25130) or 5-HT4 receptor (RS39604) antagonist failed to block the

84 In vivo, 5-HT4 receptor signaling is also upregulated since ERK a

85 5-HT4 receptor signaling is enhanced in vitro, as eviden

86 In the adrenal gland, agonism of 5-HT4 receptors stimulates release of cortisol, corticos

87 5-HT(4) receptor stimulation could represent an innovati

88 We decided to investigate whether 5-HT(4) receptor stimulation was necessary for the effec

89 -mediated pathways involving either 5-HT3 or 5-HT4 receptor subtype.

90 Short-term activation of a serotonin 5-HT4 receptor that is coupled to G alpha13 also increas

91 provides a unique and flexible mechanism for 5-HT(4) receptors to dynamically regulate synaptic trans

92 vel mode that activates epithelial serotonin 5-HT(4) receptors to modulate basal ion secretion and a

93 this regulation is region-specific, with the 5-HT4 receptor upregulated in prefrontal cortex (PFC) bu

94 The involvement of 5-HT4 receptors was examined with selective 5-HT4 agonis

95 In the distal colon, 5-HT(4) receptors were expressed by most epithelial cell

96 Mucosal 5-HT(4) receptors were present in the small and large in

97 igands were discovered for recombinant human 5-HT(4) receptors with amenability to labeling with a po