ライフサイエンスコーパス: dantrolene

1 and [3H]ryanodine binding were unaffected by dantrolene.

2 ]i, ROS, and DDR signals are normalized with dantrolene.

3 th a novel formulation of the RyR inhibitor, dantrolene.

4 (+3) or GsMTx-4 and completely suppressed by dantrolene.

5 r of calcium-induced calcium release (CICR), dantrolene.

6 on response was reduced by ruthenium red and dantrolene.

7 after exposure to clinical concentrations of dantrolene.

8 Calpain expression was reduced by dantrolene.

9 doplasmic reticulum (ER) that was blocked by dantrolene.

10 + exchange and subsequent Na+-Ca2+ exchange; dantrolene (10 mg/kg, 30 mins, 6 and 22 hrs postburn) to

11 nhibition of the pig skeletal muscle RYR1 by dantrolene (10 microm) was associated with a 3-fold incr

12 + ionophore (A23187), nifedipine (1 microM), dantrolene (10 microM), thapsigargin (100 nM), or L-glut

13 ble by either wortmannin (1.5 micromol/l) or dantrolene (12.5 micromol/l).

14 RyR) antagonist ruthenium red (10 microM) or dantrolene (25 microM) inhibited the HP-induced calcium

15 Finally, FAT defects are prevented by dantrolene, a clinical compound that reduces Ca(2+) rele

16 l death of 58Q PC cultures was attenuated by dantrolene, a clinically relevant RyanR inhibitor and Ca

17 at feeding SCA3-YAC-84Q transgenic mice with dantrolene, a clinically relevant stabilizer of intracel

18 Dantrolene, a drug used to treat MH, binds to a region w

19 Isoflurane cytotoxicity was suppressed by dantrolene, a ryanodine receptor antagonist that inhibit

20 sepsis was blocked by treating the rats with dantrolene, a substance that inhibits the release of cal

21 The RYR inhibitor dantrolene abrogated the enhancement of trypsin and chym

22 Dantrolene abrogated the ethanol-induced acceleration of

23 +) from MgATP hydrolysis is required to make dantrolene administration effective in arresting an MH e

24 The inducibility of VF after dantrolene administration was documented.

25 In rats challenged with endotoxin, dantrolene affected neither survival nor circulating con

26 l rats were randomized to receive vehicle or dantrolene after intravenous injection of endotoxin.

27 that long-term feeding of SCA1-58Q mice with dantrolene alleviated age-dependent motor deficits (quan

28 Dantrolene also inhibited [3H]ryanodine binding to purif

29 Animal studies suggest that dantrolene also protects against heart failure and arrhy

30 However, dantrolene (an inhibitor of Ca(2+)-dependent Ca2+ releas

31 stores with thapsigargin and treatment with dantrolene, an inhibitor of calcium release from caffein

32 Here we show that azumolene, an equipotent dantrolene analog, inhibits a component of SOCE coupled

33 gin D, and the ryanodine receptor inhibitors dantrolene and 1,1'-diheptyl-4,4'-bipyridinium dibromide

34 or-alpha secretion by myocytes; in contrast, dantrolene and amiloride provided significantly greater

35 Dantrolene and BAPTA-AM prevented the increase in intrac

36 locked by the ryanodine receptor inhibitors, dantrolene and DHBP.

37 tions of these results for understanding how dantrolene and malignant hyperthermia mutations may affe

38 nced by caffeine, whereas it is inhibited by dantrolene and ruthenium red, two blockers of calcium-in

39 The calcium modulating compounds, dantrolene and sitagliptin, both prevent cytokine and ER

40 Dantrolene and thapsigargin, which decrease intracellula

41 n DA release was prevented by a RyR blocker, dantrolene, and by CPA.

42 erminus of the RyR is a molecular target for dantrolene, and suggest a regulatory role for both n-cal

43 HEK-293 cells was significantly inhibited by dantrolene, and the extent of RYR3 inhibition was simila

44 N2a cells was blocked by either ryanodine or dantrolene, antagonists of Ryrs and by Genz-161, a gluco

45 These activities were inhibited by dantrolene at 37 degrees C, yet required the presence of

46 significantly worse among rats that received dantrolene at a dose of 10 mg/kg, irrespective of whethe

47 This increase was reversed by dantrolene at both 37 and 22 degrees C and was unaffecte

48 inhibiting only RyR1 and RyR3 with 25 microM dantrolene attenuated these responses caused by high (>5

49 ected by the presence of dantrolene but that dantrolene becomes increasingly effective as cytoplasmic

50 in cleavage of the RyR does not affect [(3)H]dantrolene binding in the presence of AMP-PCP, but depre

51 [(3)H]Dantrolene binding to both the intact and the n-calpain-

52 d-binding conformation in vitro and that the dantrolene-binding site and the epitope for the monoclon

53 , the cardiac RYR2 isoform was unaffected by dantrolene, both in native cardiac SR vesicles and when

54 e of Mg(2+) is unaffected by the presence of dantrolene but that dantrolene becomes increasingly effe

55 This binding was displaced by caffeine and dantrolene, but not by ruthenium red, heparin or cyclic

56 gs (100 nM cytoplasmic [Ca(2+)] + 2 mM ATP), dantrolene caused inhibition of RyR1 (rabbit skeletal mu

57 calcium signalling stabilization, e.g. with dantrolene, could be a potential disease modifying thera

58 We conclude that dantrolene decreases survival in bacterial sepsis and ha

59 tretraacetic acid (acetoxymethyl) ester, and dantrolene, did not alter bortezomib cytotoxicity.

60 Importantly, dantrolene diminishes Abeta load, reduces Abeta-related

61 f action has remained controversial, because dantrolene does not inhibit single ryanodine receptor (R

62 membrane potential of -70 mV) tetracaine and dantrolene each blocked IP3-evoked Ca2+ increases.

63 rcoplasmic reticulum (SR) vesicles such that dantrolene effectively reversed the 3-fold decrease in t

64 AN while neurones pretreated with 100 microM dantrolene failed to show potentiation of DeltaVCAN when

65 Pretreatment with 40 microM dantrolene gave substantial protection against TG- or BH

66 Dantrolene, given with conventional cooling methods, off

67 of refibrillation episodes was lower in the dantrolene group (0 versus 1, P=0.04).

68 sure >/=60 mm Hg) was achieved in 85% of the dantrolene group in comparison with 39% of controls (P=0

69 0 s and 20 s, the generator potential of the dantrolene group is significantly greater than that of t

70 (group 1), conventional cooling methods and dantrolene (group 2), conventional cooling methods and d

71 In mouse cardiomyocytes, dantrolene had no effect on cardiac Ca(2+) release in th

72 (RYR) channels, the skeletal muscle relaxant dantrolene has proven to be both a valuable experimental

73 dodantrolene, a photoactivatable analogue of dantrolene, has identified a 160 kDa SR protein with imm

74 VF on calcium handling and its modulation by dantrolene, hearts from 14 New Zealand rabbits were Lang

75 Dantrolene improved function of livers preserved in Euro

76 We hypothesized that dantrolene improves survival after ventricular fibrillat

77 Treatment with dantrolene in 4L;C* mice starting at postnatal day 5 del

78 tors that are consistent with the actions of dantrolene in vivo and suggest a mechanism of action in

79 In media simulating resting myoplasm, dantrolene increased the half-time for 45Ca2+ release fr

80 Interestingly, dantrolene-induced lowering of RyR-mediated Ca(2)(+) rel

81 Dantrolene infusion during cardiopulmonary resuscitation

82 Dantrolene inhibited RyR2 with an IC50 of 0.16 +/- 0.03

83 e RYR3, but not the RYR2, may be targets for dantrolene inhibition in vivo.

84 oration into lipid bilayers, is required for dantrolene inhibition of RyR channels.

85 We conclude that CaM is essential for dantrolene inhibition of RyR1 and RyR2.

86 strated, there is little evidence for direct dantrolene inhibition of RyR1 channel function.

87 Its absence explains why dantrolene inhibition of single RyR channels has not bee

88 Dantrolene inhibition of the RYR1 was dependent on the p

89 Mutant N98S-CaM facilitated dantrolene inhibition with an IC50 = 5.9 +/- 0.3 nM.

90 ly attenuated by co-injecting BAPTA, heparin/dantrolene (inhibitors of intracellular Ca2+ release), a

91 Although dantrolene inhibits Ca(2+) release from the sarcoplasmic

92 Dantrolene inhibits the high potassium-induced release o

93 The skeletal muscle relaxant dantrolene inhibits the release of Ca2+ from the sarcopl

94 ults suggest that the mechanism of action of dantrolene involves stabilization of domain-domain inter

95 Dantrolene is a drug that suppresses intracellular Ca(2+

96 Dantrolene is a skeletal muscle relaxant which acts by i

97 Dantrolene is administered to alleviate MH symptoms, but

98 Dantrolene is neuroprotective in animal models and may a

99 Dantrolene is the drug of choice for the treatment of ma

100 Dantrolene is the first line therapy of malignant hypert

101 ively, and define the mechanism of action of dantrolene is to increase the Mg(2+) affinity of the RyR

102 feasibility and tolerability of intravenous dantrolene (IV-D) in patients with aSAH.

103 o and suggest a mechanism of action in which dantrolene may act directly at the skeletal muscle ryano

104 nd that Ca(2+) signaling stabilizers such as dantrolene may be considered as potential therapeutic dr

105 of a high-affinity, monophasic inhibition by dantrolene of ryanodine receptor Ca2+ channel function i

106 The inhibitory potency of dantrolene on ECCE found in wild-type and MH-susceptible

107 The effect of dantrolene on light adaptation of the photoreceptor was

108 plore its mechanism of action, the effect of dantrolene on MH-like channel activation by the syntheti

109 ular basis and specificity of the actions of dantrolene on RYR channels have remained in question.

110 ese results demonstrate selective effects of dantrolene on skeletal muscle ryanodine receptors that a

111 inding to further investigate the actions of dantrolene on the three mammalian RYR isoforms.

112 skeletal muscle function, but the effect of dantrolene on this pathway has not been examined.

113 Dantrolene or 1,2-bis(o-Aminophenoxy)ethane-N,N,N',N'-te

114 tation was then commenced for 3 minutes, and dantrolene or isotonic saline was infused at the onset o

115 (benzodiazepines, dopamine agonists, and/or dantrolene) or electroconvulsive therapy, if indicated.

116 ernal stores by perifusion with ryanodine or dantrolene, or direct diffusion of Ruthenium Red into ce

117 hould malignant hyperthermia occur, however, dantrolene permits the dependable reversal of skeletal m

118 entional cooling or conventional cooling and dantrolene provided significant improvement in cardiovas

119 ity analogue in order to identify a putative dantrolene receptor in skeletal muscle.

120 Thus, the putative dantrolene receptor may be related to the skeletal muscl

121 the putative, intracellular, skeletal muscle dantrolene receptor.

122 Dantrolene reduces the elevated myoplasmic Ca(2+) genera

123 king drugs such as ryanodine, tetracaine and dantrolene, reportedly specific inhibitors of RyRs.

124 ryanodine-sensitive stores (xestospongin and dantrolene, respectively) protected against the endanger

125 The current study examines the mechanisms of dantrolene's action on skeletal muscle and shows that on

126 ion on skeletal muscle and shows that one of dantrolene's mechanisms of action is to block excitation

127 (group 2), conventional cooling methods and dantrolene's vehicle mannitol (group 3), or no treatment

128 a; however, the molecular mechanism by which dantrolene selectively affects skeletal muscle Ca2+ regu

129 nhibiting Ca(2+)-dependent Ca2+ release from dantrolene-sensitive intracellular stores.

130 the apparently sequential activation of the dantrolene-sensitive, nonreceptor proline-rich tyrosine

131 ation of the site and mechanism of action of dantrolene should contribute to the understanding of the

132 ependent increase in capillary cell calcium, dantrolene significantly decreased hypoxia-induced capil

133 Administration of 20 mumol/L dantrolene significantly decreased spontaneous calcium e

134 Dantrolene significantly shortened the cooling time comp

135 Although dantrolene significantly shortened the cooling time, it

136 Dantrolene sodium is a medically important hydantoin der

137 eated intraperitoneal sepsis with the use of dantrolene sodium, a specific inhibitor of intracellular

138 we found that exposure to the RyR1 inhibitor dantrolene suppressed a similar component of charge move

139 Dantrolene suppressed the inhibitory effect of TNF on Bc

140 drugs that target ryanodine receptors (RyR1: dantrolene, tetracaine, S107) and L-type Ca(2+) channels

141 blocked by the RyR antagonists ryanodine and dantrolene, the calpain inhibitor calpastatin, and by a

142 Long-term feeding of the RyanR inhibitor dantrolene to amyloid precursor protein-presenilin-1 mic

143 up of nervous systems first was incubated in dantrolene to block release of calcium through the ryano

144 The effect of addition of dantrolene to preservation solutions on function of whol

145 Although specific binding of dantrolene to the type 1 ryanodine receptor (RyR1), the

146 he cortex and hippocampus is also reduced in dantrolene-treated AD mice.

147 in 83% of attempts in controls versus 41% in dantrolene-treated hearts (P=0.007).

148 ntaneous circulation was achieved earlier in dantrolene-treated pigs after successful defibrillation

149 Dantrolene treatment did not appear to affect virus prod

150 patch clamp recordings, we demonstrate that dantrolene treatment fully normalizes ER Ca(2+) signalin

151 Furthermore, dantrolene treatment increased residual mutant GCase act

152 Dantrolene treatment partially normalized Ryr expression

153 Compared to untreated 4L;C* mice, dantrolene treatment significantly improved gait, reduce

154 AD mice are restored to control levels with dantrolene treatment, as are synaptic transmission and s

155 a coli and allocated to control, vehicle, or dantrolene treatment.

156 n of RyR-evoked calcium release with chronic dantrolene treatment.

157 Preincubation with azumolene, an analog of dantrolene used for the treatment of malignant hyperther

158 ase channel in SR, as a molecular target for dantrolene using the photoaffinity analog [(3)H]azidodan

159 hibition of vesicle [3H]ryanodine binding by dantrolene was associated with a decrease in the extent

160 Importantly, the efficacy of dantrolene was enhanced in low [Ca(2+)](o), suggesting a

161 found in human muscle susceptible to MH that dantrolene was ineffective at reducing halothane-induced

162 These adaptations were prevented by dantrolene, which blocks Ca2+ release from the SR.

163 Dantrolene, which depresses charge movement and E-C coup

164 sphorylation of all NARPPs was eliminated by dantrolene, which inhibits release of calcium from intra

165 nt of RCASBP M2C (4070A)-infected cells with dantrolene, which inhibits the release of calcium from t

166 lpain activity and ATP in the interaction of dantrolene with the RyR in vivo.

167 Identification of the molecular target of dantrolene would greatly aid in understanding both the m