ライフサイエンスコーパス: P2X(1) receptor

1 TAC, in addition to the previously described P2X1 receptor.

2 can promote platelet activation through the P2X1 receptor.

3 cessibility of cysteine mutants at the human P2X1 receptor.

4 SP90 inhibitors consistent with an effect on P2X1 receptors.

5 effect on both recombinant and native human P2X1 receptors.

6 nerves, causes vasoconstriction largely via P2X1 receptors.

7 was reduced 50% by GsMTx-4, independently of P2X1 receptors.

8 striction through ATP-mediated activation of P2X1 receptors.

9 ist, through its effects on P2Y1, P2Y12, and P2X1 receptors.

10 onding 5-methylphosphonate was equipotent at P2X1 receptors.

11 much less sensitive to TNP-ATP than was the P2X(1) receptor.

12 noreactivity for both P2X2 and P2X3, but not P2X1, receptors.

13 id the profound desensitization exhibited by P2X(1) receptors.

14 in the binding of both suramin and NF449 to P2X(1) receptors.

15 , suggesting a common origin: ATP binding to P2X(1) receptors.

16 In cells expressing the homomeric P2X1 receptor, 30 microM alpha,beta-methylene ATP (alpha

17 These receptors co-exist with ligand-gated P2X1 receptors activated by ATP analogs and high levels

18 Ca(2+) response was predominantly because of P2X1 receptors activated by ATP release via a phospholip

19 that ATP-induced vasodilation is mediated by P2X(1) receptor activation on mesenteric arterial endoth

20 dase activity was required to fully preserve P2X1 receptor activation by ATP in vitro.

21 s study reveals a novel inhibitory effect of P2X1 receptor activation on subsequent increases in musc

22 In the ex vivo retina, the P2X1 receptor agonist alpha,beta-methylene ATP (300 nm)

23 and alpha, beta-methylene-ATP (40 microM), a P2X1 receptor agonist, had no effect on ADP-induced plat

24 P2X(1) receptors also participate in platelet shape chan

25 P2X1 receptors also enhanced Ca(2+) responses when costi

26 ATP acts on P2X1 receptors, although contributions from other P2X an

27 We conclude that Ca(2+) influx through P2X1 receptors amplifies Ca(2+) signaling through P2Y1 a

28 It has previously been reported that P2X1 receptors amplify P2Y1-evoked Ca(2+) responses in p

29 We looked at whether the P2X1 receptor, an ATP-gated cation channel present on pl

30 cal studies have indicated expression of the P2X1 receptor, an ATP-gated cation channel, in human and

31 X receptor that has the properties of cloned P2X1 receptors and is similar to native receptors in smo

32 The presence of P2X1 receptors and vanilloid receptor like 1 protein on

33 splayed an IC50 value of 9 nM at recombinant P2X1 receptors and was 1300-, 16-, and > 10,000-fold sel

34 er potency and efficacy of BzATP and Ap5A at P2X1 receptors) and antagonists.

35 selective antagonists in regulating platelet P2X1 receptors, and their potential effects on hemostasi

36 monstrate that HIV-1 infection is reduced by P2X1 receptor antagonism.

37 aneous depolarizations were abolished by the P2X(1) receptor antagonist NF449 (10 microm) (frequency

38 The purinergic P2X1 receptor antagonist NF449, the purinergic P2X7 rece

39 hat inhibition of HIV-1 fusion by a specific P2X1 receptor antagonist, NF279, is due to the blocking

40 P2X1 receptor antagonists could thus represent a new cla

41 Thus, P2X1 receptor antagonists inhibit, but do not abolish, t

42 nd suggest that the development of selective P2X1 receptor antagonists may provide an effective non-h

43 ent the first potent, non-acidic, allosteric P2X1 receptor antagonists reported to date.

44 We used P2X1 receptor antagonists to further characterize the pu

45 tent inhibition of HIV-1 fusion by selective P2X1 receptor antagonists, including NF279, and suggeste

46 , we characterize the inhibitory activity of P2X1 receptor antagonists, NF279 and NF449, in cell line

47 Knockout mice lacking the P2X(1) receptor appear normal, but fail to breed.

48 ithin the second transmembrane domain of the P2X1 receptor appeared to confer on the receptor the ina

49 P2X1 receptors are adenosine triphosphate (ATP)-gated ca

50 These results show that P2X1 receptors are essential for normal male reproductiv

51 P1, P2Y1, P2Y12, and P2X1 receptors are expressed on platelets, which mediate

52 /mobilization demonstrated that the platelet P2X1 receptors are pharmacologically distinct from the w

53 Although these findings suggest that P2X1 receptors are present in both blood leukocytes and

54 membranes with endoglycosidase-F causes the P2X1 receptor band to migrate as a 46-kD protein, verify

55 P2X(1) receptors belong to a family of cation channels g

56 danamycin almost abolished this movement for P2X1 receptors but had no effect on P2X2 receptor traffi

57 Platelet P2X1 receptor-, but not P2Y1 receptor-, mediated increas

58 toma cells stably transfected with the human P2X1 receptor by measuring inhibition of the ATP-induced

59 This study demonstrates that in neurons, the P2X1 receptor can contribute to the properties of hetero

60 he carboxyl terminus that slowed recovery of P2X1 receptor currents (7-fold less recovery at 30 secon

61 P2X1 receptor currents in HEK293 cells were reduced by a

62 P2X1 receptor deficiency also was associated with a mark

63 B neurones, but were absent in the MNTB from P2X(1) receptor-deficient mice demonstrating a functiona

64 a,beta-meATP) sensitive, and in neurons from P2X1 receptor-deficient mice the alpha,beta-meATP respon

65 In P2X1-receptor-deficient mice, contraction of the vas def

66 NF023 (50 mum), a potent antagonist of P2X1 receptors, dilated retinal arterioles by 32.1 +/- 2

67 tions in the extracellular loop of the human P2X1 receptor during not only agonist binding and desens

68 and blood platelets, the relative levels of P2X1 receptor expression and function in human blood leu

69 By contrast, P2X1 receptor expression is strongly maintained during m

70 platelets, we show that maximally activated P2X1 receptors failed to stimulate significant aggregati

71 latively selective pharmacological probes of P2X1 receptors, filling a long-standing need in the P2 r

72 P2X1 receptors for ATP are ligand-gated cation channels,

73 single mutation of residue 23 also protected P2X1 receptors from inhibition by EPAC activation.

74 trical field stimulation, suggesting altered P2X1 receptor function with a propensity to desensitize.

75 that NTPDase1 is required to maintain normal P2X1 receptor functionality in the vas deferens and that

76 receptors, suggesting the downregulation of P2X1 receptor gene expression during the differentiation

77 90% in mice with a targeted deletion of the P2X1 receptor gene.

78 Neither the P2TAC receptor nor the P2X1 receptor has any significant role in this response.

79 nother cAMP effector; however, its effect on P2X1 receptors has not yet been determined.

80 Mapping these data to a P2X1 receptor homology model identifies significant conf

81 nd characterized genomic clones of the human P2X1 receptor (hP2X1) gene in an effort to understand it

82 The potency of compound 3 at the recombinant P2X1 receptor (IC50 10.2 +/- 2.6 microM) was lower than

83 e observations establish a critical role for P2X(1) receptors in the ATP vasodilator pathway.

84 ent mice demonstrating a functional role for P2X(1) receptors in the CNS.

85 This study reveals a major role for the P2X1 receptor in LPS-induced lethal endotoxemia through

86 h-resolution cryo-EM structures of the human P2X1 receptor in the apo closed, ATP-bound desensitized,

87 Given the expression of P2X1 receptors in a range of neurons, it seems likely th

88 rted by the lack of detectable expression of P2X1 receptors in cells used in fusion experiments and b

89 port that there is significant expression of P2X1 receptors in human platelets, but not in neutrophil

90 Deletion of P2X1 receptors in KO mice significantly blunted autoregu

91 Emerging literature suggests a key role for P2X1 receptors in mediating this chronic inflammation, b

92 tions about the previously suggested role of P2X1 receptors in thymocyte apoptosis.

93 Incubation with the P2X(1) receptor inhibitor NF023 did not alter ATP-stimul

94 colocalized with somatostatin and purinergic P2X1 receptor-IR but not with tyrosine hydroxylase-IR.

95 periments conducted in this study imply that P2X1 receptor is not expressed in target cells or involv

96 icates that Schiff's base formation with the P2X1 receptor is not necessarily required for recognitio

97 The activity of P2X1 receptors is modulated by lipids and intracellular

98 ributed to the influx of cations through the P2X(1) receptor - is of larger amplitude for sAPs (2248

99 fine the molecular pharmacology of the human P2X1 receptor laying the foundation for structure-based

100 agents that potentiate the actions of ATP at P2X1 receptors may be useful in the treatment of male in

101 P2X1 receptors may therefore require interaction with an

102 This study tests the hypothesis that P2X1 receptors mediate pressure-induced afferent arterio

103 immunoblot analysis and functional assays of P2X1 receptor-mediated ionic fluxes, we report that ther

104 Geldanamycin also inhibited native P2X1 receptor-mediated responses.

105 unoblot analysis indicated that the platelet P2X1 receptor migrates as an approximately 60-kD protein

106 sulted in the up-regulation of P2Y2, but not P2X1, receptor mRNA.

107 Mutagenesis on P2X(1) receptors of conserved residues in mammalian P2X

108 mice, we demonstrate that the absence of the P2X1 receptor on neutrophils was responsible for this de

109 Homomeric P2X1 receptors open on binding ATP and then transition t

110 ps from wild type mice and mice deficient in P2X1 receptors (P2X1(-/-)) before and after pharmacologi

111 For VCF the P2X1 receptor (P2X1R) K190C mutant (adjacent to the agon

112 Platelet P2X1 receptors play an important role in hemostasis, con

113 production, ATP release, and stimulation of P2X1 receptors represent a standby purinergic signaling

114 Sensitivity to the P2X1 receptor-selective antagonist NF449 was reduced by

115 Electron microscopy of purified P2X1 receptors showed marked changes in structure on ATP

116 Although it is known that the P2X1 receptor subtype has increased sensitivity to ATP a

117 2X receptors with a phenotype resembling the P2X1 receptor subtype on cerebral resistance arterioles.

118 = 19) were detectably immunoreactive for the P2X1 receptor subunit.

119 express functionally significant numbers of P2X1 receptors, suggesting the downregulation of P2X1 re

120 tant Ca(2+) mobilization pathways, including P2X1 receptors, that may be particularly important durin

121 out affecting the percentage contribution of P2X1 receptors to collagen-evoked Ca(2+) responses, indi

122 n leads to rapid engagement of smooth muscle P2X1 receptors to increase action potentials (Ca(2+) fla

123 occur when sufficient cation influx through P2X(1) receptors triggers L-type Ca(2+) channels; the fi

124 expression for the ligand-gated ion channel P2X1 receptor was detected in rat, but not mouse, thymoc

125 Human and mouse P2X(1) receptors were expressed in human embryonic kidne

126 e cation channels from the rat vas deferens (P2X1 receptors) were stably expressed in HEK 293 cells,

127 tracellular ligand-binding loop of the human P2X1 receptor, which is inhibited by NF449, suramin, and

128 Healthy human eosinophils express functional P2X1 receptors whose activation leads to eosinophil alph

129 e potentiator of ATP-evoked responses at rat P2X1 receptors with an EC50 value of 5.9 +/- 1.8 microM,

130 Blockade of P2X1 receptors with NF279 blocked pressure-mediated vaso