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 e, and fitted a 2-site binding model for the sigma-1 receptor.

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

4 ium (K(i) 9 nM) showed high affinity for the sigma-1 receptor.

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

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

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

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

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

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

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

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

13 ndicated that pituitary tumors overexpressed sigma-1 receptors.

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

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

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

17 AT, as well as the serotonin transporter and sigma(1) receptors.

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

19 targeting of either GluN2B-carrying NMDA or sigma(1)-receptors.

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

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

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

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

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

25 tructure-activity relationships studies, the sigma(1) receptor affinity and sigma(1):sigma(2) selecti

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

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

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

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

30 Fluvoxamine (an SSRI and sigma-1 receptor agonist) was initially identified to po

31 icacy and safety of pridopidine, a selective Sigma-1 receptor agonist, in HD.

32 ion) is an oral NMDA receptor antagonist and sigma-1 receptor agonist, which utilizes inhibition of C

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

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

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

36 Two potent sigma(1) receptor agonists, TC1 and SA4503, showed dose-

37 Cheap, simple ammonium salts act as sigma-1 receptor agonists and antagonists in vivo and re

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

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

40 emerging structural and genetic data on the sigma(1) receptor and discuss the recent cloning of the

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

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

43 Further, we noted activation of the sigma-1 receptor and enhanced intracellular Ca(2+) conce

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

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

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

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

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

49 philicity efficiency (LLE), selectivity over sigma(1) receptors, and metabolic stability, beta-amino

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

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

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

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

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

55 inding can be used to biochemically define a sigma-1 receptor antagonist.

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

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

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

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

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

61 n autoradiograms and predominantly exhibited sigma(1)-receptor binding.

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

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

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

65 in the presence or absence of pharmacologic sigma(1) receptor blockade with FTC146.

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

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

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

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

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

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

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

73 Antagonists at sigma(1) receptors have great potential for the treatmen

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

90 sigma-1 Receptor ligands prevent neuronal death associat

91 In search of new dual-acting histamine H(3)/sigma-1 receptor ligands, we designed a series of compou

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

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

94 studies, suggested off-target binding to the sigma-1 receptor, likely due to limited selectivity over

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

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

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

98 olo[1,5-d][1,4]oxazine derivatives as potent sigma-1 receptor (o(1)R) ligands are reported.

99 thyl anisamide (AEAA, a targeting ligand for sigma-1 receptor overexpressing on CRC and HCC).

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

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

102 The sigma-1 receptor pharmacophore includes an alkylamine co

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

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

105 ntly reported X-ray crystal structure of the sigma(1) receptor protein.

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

107 sigma-1 receptors represent unique binding sites that ar

108 3E-10), and its effect on BDNF secretion was sigma 1 receptor (S1R) dependent.

109 Sigma 1 receptor (S1R) is a 223-amino-acid-long transmem

110 The sigma 1 receptor (S1R) is a molecular chaperone protein

111 The sigma 1 receptor (S1R) is an enigmatic ligand-operated c

112 of the endoplasmic reticulum stress marker, sigma 1 receptor (S1R), using [(11)C]SA4503 positron emi

113 ANAVEX2-73 (blarcamesine) is a sigma-1 receptor (S1R) agonist with a strong safety reco

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

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

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

117 Sigma-1 receptor (S1R) is a multimodal chaperone protein

118 The Sigma-1 receptor (S1R) is a transmembrane protein with i

119 Sigma-1 receptor (S1R) is an endoplasmic reticulum (ER)

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

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

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

123 this study, we found that activation of the sigma-1 receptor (S1R), an ER-resident protein involved

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

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

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

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

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

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

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

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

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

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

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

135 Here, we found that the sigma-1 receptor (Sig-1R), a molecular chaperone, revers

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

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

138 e via interaction with the chaperone protein sigma-1 receptor (Sig-1R).

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

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

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

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

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

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

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

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

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

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

149 e derivatives as potent dual ligands for the sigma(1) receptor (sigma(1)R) and the mu-opioid receptor

150 )piperazin-1-yl)ethanone (9k, EST64454) as a sigma(1) receptor (sigma(1)R) antagonist clinical candid

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

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

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

154 e derivatives as potent dual ligands for the sigma-1 receptor (sigma(1)R) and the mu-opioid receptor

155 Sigma-1 receptor (sigma(1)R) is an intracellular protein

156 eno[2,3-d]pyrimidin-4(3H)-one derivatives as sigma-1 receptor (sigma(1)R) ligands are reported.

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

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

159 showed a significantly different affinity at sigma-1 receptors (sigma(1)Rs).

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

161 found that cocaine binding to intracellular sigma-1 receptor (sigma1) initiates this mechanism.

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

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

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

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

166 Sigma 1 receptor (Sigmar1) is a widely expressed, multit

167 NA-binding proteins as bait, we identify the sigma-1 receptor (SigmaR1) as an ER sheet-shaping factor

168 rline the tightrope walk between GluN2B- and sigma(1)-receptor-targeted imaging, illustrated by the e

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

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

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

172 0.992) for [(125)I]IAF interaction with the sigma-1 receptor was identified by (+)-[(3)H]pentazocine

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

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

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

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

177 nt clinical deterioration by stimulating the sigma-1 receptor, which regulates cytokine production.

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

179 4-azidococaine ([ (125)I]IACoc) binds to the sigma-1 receptor with 2-3 orders of magnitude higher aff

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

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