ライフサイエンスコーパス: sigma-1 receptor

1 e receptors but have nMolar affinity for the sigma 1 receptor.

2 haracterized their binding affinities to the sigma-1 receptor.

3 d is known to interact functionally with the sigma-1 receptor.

4 te that DMT is an endogenous agonist for the sigma-1 receptor.

5 least in part, a ligand binding site of the sigma-1 receptor.

6 lated with the affinity of the compounds for sigma 1 receptors.

7 be useful in further characterization of the sigma(1) receptor.

8 ent to the O-atom were well tolerated by the sigma(1) receptor.

9 ndicated that pituitary tumors overexpressed sigma-1 receptors.

10 myocytes and heterologous cells that express sigma-1 receptors.

11 tion between L-type calcium channels and the sigma-1 receptors.

12 e mitigated by blocking its interaction with sigma-1 receptors.

13 gma-2 ligand with an 11-fold preference over sigma-1 receptors.

14 resent in part the neuroprotective effect of sigma-1 receptors.

15 riphosphate ([(35)S]GTP gamma S) binding, by sigma(1) receptors.

16 ) but were essentially equipotent at DAT and sigma(1) receptors (10; K(i) = 77 and 124 nM, respective

17 125)I]IAF), which covalently derivatized the sigma-1 receptor (25.3 kDa) in both the rat liver and gu

18 d covalently derivatized the pure guinea pig sigma-1 receptor (26.1 kDa).

19 These results suggest that sigma-1 receptor activation can regulate calcium homeost

20 death involved activation of caspase-3, and sigma-1 receptor activation prevented an increase in cas

21 We synthesized and investigated the NMDA and sigma(1) receptor affinity of enantiomerically pure 2-(2

22 in this in vitro cell assay, the prototypic sigma 1 receptor agonist (+)-pentazocine was found not t

23 ium imaging was used to assess the effect of sigma-1 receptor agonist (+)-N-allylnormetazocine ((+)-S

24 The sigma-1 receptor agonist (+)-SKF10047 inhibited potassiu

25 We determined the effect of sigma(1) receptor agonists on immune responses in a syng

26 In vivo, sigma(1) receptor agonists promoted tumor growth and ind

27 Sigma(1) receptor agonists, including cocaine, up-regula

28 nt study was undertaken to determine whether sigma-1 receptor agonists provide neuroprotection by dec

29 at D2-like receptors but varying affinity at sigma 1 receptor and b) two benzyl phenylacetamides sigm

30 a halogen resulted in a similar affinity for sigma(1) receptors and a significantly increased affinit

31 high to moderate affinities for both DAT and sigma(1) receptors and failed to show cocaine-like discr

32 the detection of the interaction between the sigma-1 receptor and hERG within the plane of the plasma

33 te the nature of the interaction between the sigma-1 receptor and hERG.

34 itation assessed the interaction between the sigma-1 receptor and the L-type voltage-gated calcium ch

35 ychotic drug haloperidol is an antagonist of Sigma-1 receptors and in this study it potently protects

36 DMT bound to sigma-1 receptors and inhibited voltage-gated sodium ion

37 y correlate with their affinity for a cloned Sigma-1 receptor, and the protection is mimicked by a Si

38 is mediated by agonism or antagonism of the Sigma-1 receptor, and whether drugs already in use for o

39 Rimcazole, a sigma(1) receptor antagonist that binds to the DAT (K(i)

40 The sigma-1 receptor antagonist, BD1047, reversed the inhibi

41 BD1047, a sigma-1 receptor antagonist, blocked the protective effe

42 novel prodrug of haloperidol metabolite II (sigma-1 receptor antagonist/sigma-2 receptor agonist lig

43 Both dopamine uptake inhibitors and sigma(1) receptor antagonists have been implicated as po

44 bs to IL-10 or by administration of specific sigma(1) receptor antagonists.

45 The sigma-1 receptor belongs to a recently discovered family

46 repinephrine transporter (NET/DAT = 63), and sigma(1) receptor binding (sigma(1)/DAT = 44).

47 ant determinant of binding to the guinea pig sigma-1 receptor binding site may be the development of

48 at an electron-rich source is present in the sigma-1 receptor binding site, such as the pi system of

49 mischaracterized as an opioid receptor, the sigma-1 receptor binds a vast number of synthetic compou

50 The distribution of angles between pairs of sigma-1 receptors bound to hERG tetramers had two peaks,

51 in the SBDLII region of a mutant guinea pig sigma-1 receptor (C94A,V190C), both in a sigma-ligand (h

52 antinociceptive effects of opioid drugs, so sigma-1 receptors constitute a biological brake to opioi

53 In conclusion, sigma-1 receptors curtail immune-driven peripheral opioi

54 the SBDLI region of the wild type guinea pig sigma-1 receptor (Cys94) and at position 190 in the SBDL

55 ccumulation of (18)F-FTC-146 was observed in sigma-1 receptor-dense organs such as the pancreas and s

56 ide cleavage of the [125I]IACoc photolabeled sigma-1 receptor followed by radiosequencing identified

57 s became both singly and doubly decorated by sigma-1 receptors; however, hERG monomers were only sing

58 To determine the roles of both DAT and sigma(1) receptors in the behavioral actions of rimcazol

59 eaving the specific [(125)I]IAF-photolabeled sigma-1 receptor in guinea pig and rat liver membranes a

60 The overexpression of sigma-1 receptors in spontaneous pituitary tumors is det

61 ticle that small molecule antagonists of the sigma-1 receptor inhibit tumor cell survival to reveal c

62 io of approximately 2:1, indicating that the sigma-1 receptor interacts with hERG with 4-fold symmetr

63 The sigma-1 receptor is an endoplasmic reticulum chaperone p

64 The sigma-1 receptor is widely distributed in the central ne

65 evidence suggests that Sigma1 (also known as sigma-1 receptor) is a unique chaperone or scaffolding p

66 d hypermobility in wild-type mice but not in sigma-1 receptor knockout mice.

67 ization than did normal RGC-5 cells, and the sigma-1 receptor ligand (+)-SKF10047 reduced the glutama

68 comprises, at least in part, regions of the sigma-1 receptor ligand binding site(s).

69 An additional photoprobe based on the sigma-1 receptor ligand fenpropimorph, 1- N-(2-3-[ (125)

70 We report that sigma(1) receptor ligands, including cocaine, augment tu

71 Regulation of calcium influx in RGCs by sigma-1 receptor ligands may represent in part the neuro

72 this study was to investigate the effect of sigma-1 receptor ligands on calcium homeostasis in a ret

73 sigma-1 Receptor ligands prevent neuronal death associat

74 he putative "nitrogen interacting region" of sigma-1 receptor ligands.

75 (S1R) is a mammalian member of the ERG2 and sigma-1 receptor-like protein family (pfam04622).

76 ues with varying affinities for both DAT and sigma(1) receptors may provide a novel approach toward d

77 We suggest that the sigma-1 receptor may bind to hERG in the endoplasmic ret

78 other indications and that interact with the Sigma-1 receptor might also prevent oxidative damage due

79 sigma-1 Receptor-overexpressing RGC-5 (RGC-5-S1R) cells

80 dosimetry in humans for the highly selective sigma-1 receptor PET agent (18)F-6-(3-fluoropropyl)-3-(2

81 The sigma-1 receptor pharmacophore includes an alkylamine co

82 sigma(1) Receptors physically associate with mu opioid r

83 xplore the hydrophobic binding region of the sigma(1) receptor protein, regioisomeric spirocyclic thi

84 The results suggest that sigma-1 receptors regulate intracellular calcium levels

85 sigma-1 receptors represent unique binding sites that ar

86 3E-10), and its effect on BDNF secretion was sigma 1 receptor (S1R) dependent.

87 The sigma-1 receptor (S1R) is a 223 amino acid two transmemb

88 The sigma-1 receptor (S1R) is a ligand-regulated membrane pr

89 Sigma-1 receptor (S1R) is a mammalian member of the ERG2

90 The Sigma-1 receptor (S1R) is known to play a protective rol

91 sigma-1 receptor (S1R) radioligands have the potential t

92 The non-opioid sigma-1 receptor (S1R) was identified as a novel effecto

93 To exploit RGC-protective sigma-1 receptor (S1R), we loaded unimNPs with an endoge

94 The noninvasive imaging of sigma-1 receptors (S1Rs) could provide insight into thei

95 These results also demonstrate that sigma 1 receptor selective benzyl phenylacetamides are c

96 These studies provide further evidence that sigma 1 receptor selective compounds can provide neuropr

97 receptor and b) two benzyl phenylacetamides sigma 1 receptor selective compounds which bind with low

98 eceptor, and the protection is mimicked by a Sigma-1 receptor-selective antagonist (BD1063), but not

99 Sigma 1 receptor (Sig-1R), a MAM chaperone affecting cal

100 lodynia (MA) induced by direct activation of sigma-1 receptor (Sig-1).

101 The sigma-1 receptor (Sig-1R) chaperone at the endoplasmic r

102 the present study, we demonstrated that the sigma-1 receptor (Sig-1R) chaperone, the mammalian homol

103 The sigma-1 receptor (Sig-1R) is an endoplasmic reticulum ch

104 The sigma-1 receptor (Sig-1R), an endoplasmic reticulum (ER)

105 We found here that the ER protein sigma-1 receptor (Sig-1R), which is implicated in neurop

106 The present study found that sigma-1 receptors (Sig-1R), unique endoplasmic reticulum

107 Sigma-1 receptors (Sig-1Rs) are endoplasmic reticulum (E

108 s aimed at determining whether antagonism of Sigma-1 receptors (Sig-1Rs) blocked compulsive-like bing

109 Sigma-1 receptors (Sig-1Rs) have been implicated in many

110 Sigma-1 receptors (Sig-1Rs) that bind diverse synthetic

111 Sigma-1 receptors (Sig-1Rs), shown by us to exist in det

112 The sigma 1 receptor (Sig1R) is a stress-activated chaperone

113 explored the activation of a unique protein, sigma 1 receptor (Sig1R), in the treatment of PRC loss b

114 The sigma-1 receptor (Sig1R) is up-regulated in many human t

115 The sigma-1 receptor (Sig1R) is widely expressed in the CNS,

116 of a new series of 1-arylpyrazoles as potent sigma(1) receptor (sigma(1)R) antagonists are reported.

117 Sigma(1) receptors (sigma(1)Rs) are intracellularly mobi

118 growth and survival signaling cascades, the sigma(1) receptors (sigma(1)Rs) represent a novel target

119 Sigma-1 receptor (sigma-1R) agonists enhance inositol 1,

120 The sigma-1 receptor (sigma-1R) is an endoplasmic reticulum

121 Sigma-1 receptors (sigma-1Rs) are endoplasmic reticulum

122 r arises from R-CIT activation of the orphan sigma-1 receptor(sigma1, Oprs1).

123 The sigma-1 receptor (sigma1R) is a molecular chaperone, and

124 Methamphetamine also interacts with the sigma-1 receptor (sigma1R), an inter-organelle signaling

125 (11)C-Me-NB1 binding was independent of the sigma-1 receptor (Sigma1R), and the Sigma1R agonist (+)-

126 mers of 2a-c showed greater affinity for the sigma(1) receptor than the (1S, 5S,9S)-isomers.

127 protein confirmed the direct binding of the sigma-1 receptor to hERG monomers, dimers, and tetramers

128 Cleavage of the photolabeled sigma-1 receptor using Endo Lys C and cyanogen bromide (

129 0.992) for [(125)I]IAF interaction with the sigma-1 receptor was identified by (+)-[(3)H]pentazocine

130 ]IACoc derivatization site in the guinea pig sigma-1 receptor was identified using chemical cleavage

131 npropimorph has high-binding affinity to the sigma-1 receptor, we have synthesized a series of fenpro

132 CoMFA studies at both DAT and sigma(1) receptors were performed to examine structural

133 cocaine derivatives to the guinea pig liver sigma-1 receptor were determined.

134 erminus and SBDLI-containing peptides of the sigma-1 receptor, while [ (125)I]IAC44 was found in pept

135 4-azidococaine ([ (125)I]IACoc) binds to the sigma-1 receptor with 2-3 orders of magnitude higher aff

136 do-4-azidococaine ([125I]IACoc) binds to the sigma-1 receptor with an affinity that is 2-3 orders of

137 rat liver membranes and the pure guinea pig sigma-1 receptor with EndoLys-C and cyanogen bromide, th