ライフサイエンスコーパス: cytisine

1 cerebral cortex, and hippocampus, using [3H]cytisine.

2 ChRs with relatively low affinity to ACh and cytisine.

3 decreased the antidepressant-like effect of cytisine.

4 behavioral responses to spinal nicotine and cytisine.

5 s serotonin depletion blocked the effects of cytisine.

6 ansmitter ACh and the smoking cessation drug cytisine.

7 ited differential activation by nicotine and cytisine.

8 similar agonist activity profile to that of cytisine.

9 a4beta2 nAChR subtype in binding assays than cytisine.

10 y of binding was measured in the presence of cytisine.

11 approximately 4-fold the number of sites for cytisine.

12 (-)-Cytisine (0.8 and 1.0 mg/kg) displaced 70% and 72% of th

13 paradigm with subcutaneous injection of (-)-cytisine (0.8 and 1.0 mg/kg).

14 l ATP release while alpha3* stimulation with cytisine (1-100 muM) caused a concentration-dependent, b

15 ditional agonists (acetylcholine, anabasine, cytisine, 1, 1-dimethyl-4-phenylpiperazinium, lobeline,

16 e and other activator ligands, including (-)-cytisine, 1,1-dimethyl-4-phenylpiperazinium, (S)-3-methy

17 Cytisine (100 microM), an agonist of nAChRs that contain

18 bladder reflexes in response to intravesical cytisine (100 muM) is blocked by systemic administration

19 ation and radioligand binding studies ([(3)H]cytisine, (125)I-alpha-bungarotoxin, and (125)I-alpha-co

20 s reported for 40% of participants receiving cytisine (264 of 655) and 31% of participants receiving

21 nd the cytisine-derivative 3-(pyridin-3'-yl)-cytisine (3-pyr-Cyt) on brain reward function in nicotin

22 Subcutaneous injection of 1 mg/kg cytisine 45 min after injection of the radiotracer reduc

23 Moreover, unlike epibatidine and cytisine, 5-[(125)I]iodo-A-85380 shows no binding in any

24 receptor agonists nicotine (5-100 microM) or cytisine (50-75 microM) and the P2X receptor agonists AT

25 receive behavioural support plus either oral cytisine (9 mg on day 0, which was gradually reduced to

26 Cytisine, a ligand formerly believed to be beta4-selecti

27 Placebo-controlled trials indicate that cytisine, a partial agonist that binds the nicotinic ace

28 Cytisine, a partial agonist that binds with high affinit

29 pibatidine binding sites with relatively low cytisine affinity ("cytisine-resistant" sites), resolvin

30 e, nicotine, dimethylphenylpiperazinium, and cytisine all produced a conductance increase.

31 Both cytisine and 1,1-dimethyl-4-phenylpiperazinium behaved a

32 [3H]Cytisine and 125I-alpha-bungarotoxin binding sites were

33 Cytisine and 5-halogenated cytisines had moderate effica

34 The pharmacokinetic characteristics of [(3)H]cytisine and [(125)I]alpha-bungarotoxin binding in the f

35 These results indicate that [(3)H]cytisine and [(125)I]alpha-bungarotoxin identify distinc

36 adiography, we examined the binding of [(3)H]cytisine and [(125)I]alpha-bungarotoxin in the laminated

37 d binding assay on rat cortex against [(3)H]-cytisine and [(3)H]-methyllycaconitine to measure their

38 tisine and placebo NRT (group 3), or placebo cytisine and active NRT (group 4).

39 sitive to the beta4-containing nAChR agonist cytisine and antagonist mecamylamine (MEC).

40 Cytisine and DMPP seemed to be partial agonists.

41 Cytisine and lobeline serve as full agonists at alpha4be

42 Cytisine and nicotine bound to specific sites in homogen

43 Binding of tritiated cytisine and nicotine to cell homogenates revealed the p

44 varenicline and active NRT (group 2), active cytisine and placebo NRT (group 3), or placebo cytisine

45 rchloroepibatidine, [3H](-)-nicotine and [3H]cytisine and that of nAChR densities determined in postm

46 y-metanicotine (TC-2559), cytisine, and 3-Br-cytisine and the antagonists dihydro-beta-erythroidine a

47 alpha4beta2* nAChR partial agonist and like cytisine and varenicline has antidepressant-like effects

48 Here we present the co-crystal structures of cytisine and varenicline in complex with Aplysia califor

49 ta2 receptors by the smoking-cessation drugs cytisine and varenicline is strongly limited by desensit

50 essation therapy (nicotine, varenicline, and cytisine) and by sazetidine.

51 +/-)-epibatidine, 2S-(-)-nicotine, 7R,9S-(-)-cytisine, and 1,1-dimethyl-4-phenylpiperazinium in a cel

52 ses to the agonists acetylcholine, nicotine, cytisine, and 1,1-dimethyl-4-phenylpiperazinium, suggest

53 eptors from SH-SY5Y cells for acetylcholine, cytisine, and 1,1-dimethyl-4-phenylpiperazinium.

54 oline, 24 nM for (+)-epibatidine, 6.6 microM cytisine, and 15 microM 1,1-dimethyl-4-phenylpiperaziniu

55 trast, inhibition experiments with nicotine, cytisine, and 3-(2(S)-azetidinylmethoxy)pyridine-2HCl (A

56 (A-85380), 5-ethoxy-metanicotine (TC-2559), cytisine, and 3-Br-cytisine and the antagonists dihydro-

57 riatum have similar affinities for nicotine, cytisine, and A85380, that alpha-conotoxin MII discrimin

58 In this study, we used ACh, cytisine, and nicotine (which bind at both the a4:a4 and

59 In this study, we used ACh, cytisine, and nicotine (which bind at both the alpha4:al

60 cacy for 1,1-dimethyl-4-phenyl-piperazinium, cytisine, and suberyldicholine; competitive antagonism b

61 ies investigated the effects of varenicline, cytisine, and the cytisine-derivative 3-(pyridin-3'-yl)-

62 r the nicotinic partial agonists dianicline, cytisine, and two cytisine derivatives - 10-fluorocytisi

63 es the decay kinetics ("desensitization") of cytisine- and nicotine-evoked currents (pK(a) approximat

64 with a rank order of epibatidine >> A85380 > cytisine approximately 1,1-dimethyl-4-phenyl-piperaziniu

65 The novel compound NS3861 and cytisine are agonists of nicotinic acetylcholine recepto

66 ne receptor (nAChR) agonists varenicline and cytisine are widely used as smoking cessation treatments

67 is study assessed the efficacy and safety of cytisine as compared with placebo.

68 The lower price of cytisine as compared with that of other pharmacotherapie

69 te the extent to which this model applies to cytisine at the alpha4beta2 nAChR, which is a subtype th

70 ine (IC50, 1.3 microM), but had no effect on cytisine binding at a concentration of 30 microM.

71 ine and nicotine (IC50, 2.5 nM), and reduced cytisine binding in a competitive manner (Ki 20 nM).

72 Similarly, 3H-cytisine binding in cortex of SAM-R/1 mice was higher at

73 the optic nerve for 6 weeks decreased [(3)H]cytisine binding in layers 8/9 by 70+/-1%, whereas 6-mon

74 le to published values for the high affinity cytisine binding site in rat brain (alpha4beta2), demons

75 id not seem to influence the number of [(3)H]cytisine binding sites across mouse strains.

76 s ca.50 pM affinity for rat brain [(3)H]-(-)-cytisine binding sites and 163% efficacy compared to nic

77 horbol-12-myristate-13-acetate increased [3H]cytisine binding sites and nAChR function and enhanced t

78 secutive coronal sections the density of [3H]cytisine binding sites was decreased in pre-hypertensive

79 ecutive coronal sections, the density of [3H]cytisine binding sites was decreased in SHR by up to 25%

80 The increase in [3H]cytisine binding sites was initiated by low concentratio

81 However, the number of [(3)H]cytisine binding sites was not correlated with nicotine-

82 isplayed moderate to high affinity for [(3)H]cytisine binding sites, while three (17b, 18b,c) and six

83 within each strain with the number of [(3)H]cytisine binding sites.

84 vatives were measured by inhibition of [(3)H]cytisine binding to rat brain tissue.

85 [(3)H]Cytisine binding was significantly higher in the tecta o

86 cotine-stimulated (86)Rb(+) efflux and [(3)H]cytisine binding were found to vary across brain regions

87 cotine-stimulated (86)Rb(+) efflux and [(3)H]cytisine binding, both of which seem to measure the nico

88 Nicotine fully blocked cytisine binding, but cytisine only partially blocked ni

89 nicotine was a full competitive inhibitor of cytisine binding.

90 These data indicate that cytisine binds only to surface receptors on intact cells

91 N in the brain was evaluated in baseline and cytisine-blocking studies of 4 male Papio anubis baboons

92 Varenicline and cytisine, but not 3-pyr-Cyt, diminished the nicotine wit

93 Acetylcholine, (-)-nicotine, cytisine, carbachol, and (+/-)-epibatidine all stimulate

94 -dimethyl-4-phenylpiperzinium iodide (DMPP), cytisine (CYT) and epibatidine (EPI) were investigated o

95 [(3)H]Cytisine demonstrated high specific binding in adult fro

96 The dose-dependent blocking experiments with cytisine demonstrated that (18)F-AZAN binds specifically

97 he effects of varenicline, cytisine, and the cytisine-derivative 3-(pyridin-3'-yl)-cytisine (3-pyr-Cy

98 The cytisine-derivative 3-pyr-Cyt is a very weak alpha4beta2

99 rtial agonists dianicline, cytisine, and two cytisine derivatives - 10-fluorocytisine and 9-bromo-10-

100 The results suggest a model for how cytisine derivatives substituted at C(10) (as well as C(

101 We also use a panel of C(10)-substituted cytisine derivatives to probe the effects of subtle chan

102 also evaluated a series of C(10)-substituted cytisine derivatives, using two-electrode voltage-clamp

103 is and pharmacological properties of several cytisine derivatives.

104 e = 3-(azetidinylmethoxy)pyridine (A-85380), cytisine, dimethylphenylpiperazinium (DMPP).

105 these studies indicate that varenicline and cytisine diminish the dysphoric-like state associated wi

106 Application of agonists (nicotine, cytisine, epibatidine) activated a large (100-200 pA/pF)

107 randomly assigned in a 1:1 ratio to receive cytisine for 25 days or nicotine-replacement therapy for

108 The effectiveness of cytisine for continuous abstinence was superior to that

109 The apparent affinity of cytisine for surface receptors (K(d)=0.8 nM) was not sig

110 ver 6 months occurred more frequently in the cytisine group (288 events among 204 participants) than

111 verse events occurred less frequently in the cytisine group (997 events among 482 participants) compa

112 events were reported more frequently in the cytisine group (difference, 5.7 percentage points; 95% C

113 ntinuous abstinence rates were 11.7% for the cytisine group and 13.3% for the varenicline group (risk

114 At 6 months, 401 (32.4%) participants in the cytisine group and 366 (29.7%) participants in the place

115 group), which included 91 deaths (49 in the cytisine group and 42 in the placebo group).

116 53 (4.3%) of 1239 participants in the cytisine group and 46 (3.7%) of 1233 participants in the

117 ted serious adverse events (94 events in the cytisine group and 90 events in the placebo group), whic

118 abstinence was 8.4% (31 participants) in the cytisine group as compared with 2.4% (9 participants) in

119 e at the 12-month follow-up was 13.2% in the cytisine group versus 7.3% in the placebo group (P=0.01)

120 1-dimethyl-4-phenylpiperazinium>(-)nicotine>cytisine>carbamylch oli ne> /=d-tubocurarine).

121 In contrast, cytisine had no effect on DMV neurones previously expose

122 Cytisine and 5-halogenated cytisines had moderate efficacy at LS receptors but had

123 However, cytisine has not been tested against the most effective

124 w nicotinic ligand based on the structure of cytisine, has recently been approved by the U.S. Food an

125 fluoxetine and the nicotinic partial agonist cytisine have synergistic effects in a mouse model of an

126 Rapid application of nicotine and cytisine indicated EC50 values of congruent with22 and c

127 Cytisine is a partial agonist of some nAChRs and has bee

128 The blocking of nAChRs with cytisine is dose-dependent and it showed that (18)F-AZAN

129 Cytisine is more effective than placebo and nicotine rep

130 the United States for smoking cessation and cytisine is used in Eastern European countries.

131 Cytisinicline (cytisine) is a plant-based alkaloid that, like varenicli

132 gands, determined in competition assays, was cytisine < nicotine < acetylcholine < carbachol < curare

133 raction and two hydrogen bonds, we find that cytisine makes a second cation-pai interaction at the ag

134 with the manufacturers' recommended dosage: cytisine (n = 725), 1.5-mg capsules taken 6 times daily

135 re enrolled and randomly assigned to receive cytisine (n=1239) or placebo (n=1233).

136 2 nAChRs when measured with [3H]epibatidine, cytisine, nicotine, and acetylcholine.

137 Nicotine fully blocked cytisine binding, but cytisine only partially blocked nicotine binding to inta

138 in displacing (+/-)-[3H]epibatidine, (-)-[3H]cytisine or (-)-[3H]nicotine binding to spinal nicotinic

139 Unlike (-)-[3H]cytisine or (-)-[3H]nicotine, (+/-)-[3H]epibatidine reve

140 Acute administration of cytisine or 3-pyr-Cyt did not affect ICSS thresholds.

141 ) and more than twice that measured with [3H]cytisine or [3H](-)nicotine.

142 However, no changes in hippocampal cytisine or alpha-bungarotoxin binding were found.

143 Relative sensitivity to inhibition by cytisine or alpha-bungarotoxin was used to evaluate phar

144 rticipants were randomly assigned to receive cytisine or matching placebo for 25 days; participants i

145 ent therapies or partial nAChR agonists like cytisine or varenicline.

146 -related alterations in either nicotinic (3H-cytisine) or muscarinic (3H-QNB) cholinergic receptor bi

147 e full agonist nicotine, the partial agonist cytisine, or the competitive antagonist dihydro-beta-ery

148 beta4 Gene deletion partially reduced cytisine-resistant and alpha-bungarotoxin-resistant site

149 Comparison of the cytisine-resistant population's distribution with that o

150 inhibition by cytisine were eliminated, and cytisine-resistant sites were reduced.

151 ites with relatively low cytisine affinity ("cytisine-resistant" sites), resolving [(3)H]epibatidine

152 s nicotine and cytisine with high affinity ("cytisine-sensitive" sites).

153 eled epibatidine, (-)-nicotine, lobeline and cytisine significantly inhibited [18F]FPH binding in tha

154 tine-treated and NGF-treated cells; however, cytisine-stimulated [3H]norepinephrine release indicated

155 creased EC(50) values for both nicotine- and cytisine-stimulated alpha-CtxMII-sensitive dopamine rele

156 tentiated the antidepressant-like effects of cytisine, suggesting that this subtype might mediate the

157 essation compounds varenicline (Chantix) and cytisine (Tabex), have been evaluated at both the 2:3 an

158 ations in hydrogen bonding interactions with cytisine that provide a rationalization for the stoichio

159 Our findings do not support the addition of cytisine to brief behavioural support for the treatment

160 Among daily smokers willing to quit, cytisine treatment for 25 days, compared with vareniclin

161 malaria (mefloquine) and nicotine addiction (cytisine, varenicline).

162 ber of sites for cytisine was increased, and cytisine was able to fully block nicotine binding.

163 Cytisine was about 3 times more potent than ACh (low-con

164 e ligand-binding domain, whereas efficacy of cytisine was additionally affected by the nature of the

165 We investigated whether cytisine was at least as effective as nicotine-replaceme

166 When combined with brief behavioral support, cytisine was found to be superior to nicotine-replacemen

167 was unchanged, while the number of sites for cytisine was increased, and cytisine was able to fully b

168 In this single-center study, cytisine was more effective than placebo for smoking ces

169 In addition, cytisine was more efficacious at the alpha-CtxMII-sensit

170 Cytisine was provided by mail, free of charge, and nicot

171 ed subgroup analysis of the primary outcome, cytisine was superior to nicotine-replacement therapy am

172 agonists (such as epibatidine, anatoxin, or cytisine) was also powerfully antagonized by bisindolylm

173 differential effects of ACh, TC-2559 and 5-I-cytisine we evaluated the effects of long-term exposure

174 for the agonists epibatidine, nicotine, and cytisine were consistent with reported values, indicatin

175 er-affinity sites sensitive to inhibition by cytisine were eliminated, and cytisine-resistant sites w

176 risky drinking and smoking, varenicline and cytisine were not more efficacious than NRT to treat ris

177 Compared with cytisine, which selectively activates receptors containi

178 The alpha4beta2 receptor bound [3H]cytisine with a Kdapp of 0.74 +/- 0.14 nM.

179 correspond to that which binds nicotine and cytisine with high affinity ("cytisine-sensitive" sites)