ライフサイエンスコーパス: opioid antagonist

1 hine (a partial agonist), and naltrexone (an opioid antagonist).

2 I), are derived from naltrexone, a universal opioid antagonist.

3 ed by Portoghese as a highly selective delta-opioid antagonist.

4 whether these effects can be blocked via an opioid antagonist.

5 blocked by pretreatment with naloxone, a mu-opioid antagonist.

6 ethyl-4-(3-hydroxyphenyl)piperidine class of opioid antagonist.

7 whether these effects could be blocked by an opioid antagonist.

8 erapeutic benefit in schizophrenia for 4 pan-opioid antagonists.

9 stemic and central administration of general opioid antagonists.

10 by pretreatment with general or mu-selective opioid antagonists.

11 administration of appropriately low doses of opioid antagonists.

12 reatment with either general or mu-selective opioid antagonists.

13 lective opioid agonists and highly-selective opioid antagonists.

14 platform on which to build a novel series of opioid antagonists.

15 atory or neuropathic pain can be reversed by opioid antagonists.

16 by central but not peripheral application of opioid antagonists.

17 planning and evaluation of experiments with opioid antagonists.

18 l)piperazines (8a,b) gives (4a,b), which are opioid antagonists.

19 nduced constipation with peripherally acting opioid antagonists.

20 ethyl-4-(3-hydroxyphenyl)piperidine class of opioid antagonists.

21 distribution in vivo of the selective delta-opioid antagonist 11C-methylnaltrindole (11C-MeNTI) and

22 opyl substituted compounds were nonselective opioid antagonists (2) all N-phenylpropyl analogues were

23 However, infusion of the opioid antagonist 24 hr postpartum had no effect on the

24 Using the non-selective opioid antagonist, [3H]-naloxone, opioid binding sites w

25 The present study used the opioid antagonist 6 beta-[125iodo]-3,14-dihydroxy-17-cyc

26 ind that in a rat model of human depression, opioid antagonists abolish the ability of ketamine to re

27 ptor affinity (K(i) = 0.62 nM) and potent mu-opioid antagonist activity (IC(50) = 0.54 nM).

28 5'-regioisomer (GNTI) possessed potent kappa-opioid antagonist activity and high affinity at kappa-re

29 group has resulted in far more robust kappa opioid antagonist activity than seen in the standard orv

30 analgesia in the amygdala was unaffected by opioid antagonists administered into control misplacemen

31 Yet, opioid antagonists administered into misplaced amygdala

32 In contrast, opioid antagonists administered into misplaced mesenceph

33 ine) and delta2 (naltrindole isothiocyanate) opioid antagonists administered into the PAG significant

34 s the struggle of traditional pharmaceutical opioid antagonists against BNO substances.

35 or guinea pig brain membranes and for their opioid antagonist and agonist activities in vitro on the

36 date the potential for the use of a combined opioid antagonist and agonist therapy for the treatment

37 We tested the effects of an opioid antagonist and dopamine agonist on the ability of

38 Opioid antagonists and mixed agonist/antagonists appear

39 -line oral treatments recommended include an opioid-antagonist and opiate analgesics.

40 lus + 0.15 mg/kg/hour maintenance) naloxone (opioid antagonist) and placebo-saline infusion.

41 Extended-release naltrexone (XR-NTX), an opioid antagonist, and sublingual buprenorphine-naloxone

42 either general, mu, mu(1), kappa(1) or delta opioid antagonists, and through central administration o

43 Non-selective opioid antagonists applied to the PAG block the expressi

44 d that the variations in binding affinity of opioid antagonists are dominated by steric rather than e

45 of the opioid receptor blockade achieved by opioid antagonists are missing.

46 us treatment of slices with the irreversible opioid antagonist beta-chlornaltrexamine (beta-CNA) but

47 Moreover, the selective mu opioid antagonist, beta-funaltrexamine (betaFNA: 2-20 mu

48 Opioid antagonists block the positive hedonic response t

49 n to decrease pain in a manner reversible by opioid antagonists, but little is known about the centra

50 dogenous opioid-receptor interfacing with an opioid antagonist can facilitate the process of wound he

51 formation provides very strong evidence that opioid antagonists can interact with opioid receptors in

52 Importantly, opioid antagonists can readily reverse their effects in

53 s challenging to teach, whereas naloxone, an opioid antagonist, can be administered by emergency medi

54 This study used an opioid antagonist challenge procedure to evaluate the re

55 ioid receptor (DORS177L), in which classical opioid antagonists could inhibit forskolin-stimulated ad

56 ubjects received injections of either the mu opioid antagonist CTAP (6.6 nMol), the kappa opioid anta

57 This effect was reversed by the neutral mu-opioid antagonist CTAP.

58 ns of these neuropeptides with the selective opioid antagonists, CTAP (mu) and nor-BNI (kappa) and th

59 The mu-opioid antagonist D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH

60 by a hedonic mechanism because naloxone, an opioid antagonist, decreased intake in rats infused with

61 be the sum of two independent drug effects (opioid antagonists decreasing and baclofen increasing fo

62 one (5 mg/kg, sc), a peripherally restricted opioid antagonist, did not affect the hypothermia caused

63 acterised and are important to understand as opioid antagonists do not help everyone with AD.

64 activators, a serotonin 2C receptor agonist, opioid antagonist, dopamine-norepinephrine reuptake inhi

65 xamine the role of OPRM1 A118G variation for opioid antagonist effects on alcohol responses.

66 ervations of selective and receptor-specific opioid antagonist effects upon corresponding agonist-ind

67 The use of opioid antagonists (eg, naloxone) during respiratory or

68 tment of either general, mu, kappa, or delta-opioid antagonists even though OFQ/N(1-17) binds poorly

69 Less evidence is available for the opioid antagonist extended release naltrexone, with a me

70 Naltrexone, an opioid antagonist, has been shown to modulate expression

71 Naltrexone, an opioid antagonist, has been used in clinical trials to t

72 property design, a series of selective kappa opioid antagonists have been discovered.

73 ents with schizophrenia to determine whether opioid antagonists have therapeutic efficacy on positive

74 However, the prototypical selective kappa-opioid antagonists have very long durations of action th

75 he loss of antinociceptive effect or rebound opioid antagonist hyperalgesia (i.e., expression of tole

76 st that GNTI is a potent anorectic agent and opioid antagonist in rats.

77 nyl)piperidine derivative 3, prototypical mu-opioid antagonist in this series.

78 hether pretreatment of general and selective opioid antagonists in the amygdala blocked OFQ/N(1-17)-i

79 alon, and the small hyperalgesia elicited by opioid antagonists in the PAG could not account for the

80 hether pretreatment of general and selective opioid antagonists in the vlPAG blocked OFQ/N(1-17)-indu

81 orphamine: NBNI) or delta (naltrindole: NTI) opioid antagonists in the VTA, and correspondingly, whet

82 All of the compounds acted as opioid antagonists, including those with N-substituents

83 dole, which has been used as a classic delta opioid antagonist, inhibited growth and induced apoptosi

84 n of the opioid agonist into the PVN and the opioid antagonist into the CNA, and vice versa.

85 on of an opioid agonist into one site and an opioid antagonist into the other.

86 elta1 or delta2 (naltrindole isothiocyanate) opioid antagonists into the ventral tegmental area.

87 Administration of naloxone, an opioid antagonist, into the CNA prior to DAMGO blocks DA

88 nts, mood stabilizers, antianxiety drugs and opioid antagonists is difficult to interpret because it

89 operties of nicotine, and suggest that kappa-opioid antagonists may be useful therapeutic tools to re

90 Peripheral opioid antagonists may represent an important therapeuti

91 Opioid antagonists may represent effective treatments fo

92 availability is proposed to be the target of opioid antagonist medication to prevent relapse.

93 ), but not by the peripherally restricted mu-opioid antagonist, methyl-naloxone (0.4 mg/kg i.v.).

94 tra-NAc (Experiment 2) with the nonselective opioid antagonist methylnaloxonium (0-ng, 375-ng, or 750

95 e produced by intracerebral injections of an opioid antagonist, methylnaloxonium (MN), into the locus

96 Both mu and kappa opioid antagonists microinjected into either the hypotha

97 lthy volunteers suggest that samidorphan, an opioid antagonist, mitigates weight gain associated with

98 Opioid antagonists modulate cannabinoid effects and may

99 ormetazocine, 12) was about as potent as the opioid antagonist N-allylnormetazocine (AD(50) in the ta

100 Oral administration of the opioid antagonist nalmefene alone (up to 20 mg/kg) faile

101 xamined the efficacy and tolerability of the opioid antagonist nalmefene in the treatment of adults w

102 s of acute and chronic administration of the opioid antagonist, nalmefene, on the binding activity of

103 cked by (1) SN and VTA injections of the mu1 opioid antagonist naloxonazine and (2) striatal injectio

104 tion by microdialysis (retrodialysis) of the opioid antagonist naloxone (0.1-1.0 microgram microliter

105 s heat and intravenous administration of the opioid antagonist naloxone (0.15 mg/kg bolus + 0.1 mg/kg

106 ses of all 4 agonists were blocked by the mu-opioid antagonist naloxone (0.4 mg/kg i.v.), but not by

107 Pretreatment with the nonselective opioid antagonist naloxone (1.0 mg/kg, i.p.) attenuated

108 morphine), a specific effect blocked by the opioid antagonist naloxone (10 muM).

109 icotine on presynaptic GABA release, and the opioid antagonist naloxone (100 nM) antagonized the acti

110 Intravenous administration of the opioid antagonist naloxone (250 microg) completely block

111 Selected animals were pretreated with the opioid antagonist naloxone (3 mg/kg; intraperitoneally).

112 reduces ischemic injury, the effects of the opioid antagonist naloxone (3 mg/kg; IP) on retinal neur

113 duced by intravenous (i.v.) injection of the opioid antagonist naloxone (5 mg kg-1).

114 This analgesic activity was reversed by the opioid antagonist naloxone (5 mg/kg, s.c.) and kappa(1)-

115 allodynic effect could be reversed by the mu-opioid antagonist naloxone 4 months after gene transfer

116 etic resonance imaging (fMRI) study with the opioid antagonist naloxone and different levels of aerob

117 se to noxious heat and administration of the opioid antagonist naloxone and placebo saline.

118 -dependent manner, and both the nonselective opioid antagonist naloxone and the kappa-selective block

119 -1 in the globus pallidus was blocked by the opioid antagonist naloxone and the mu-selective peptide

120 Fentanyl effects were blocked by the opioid antagonist naloxone and were not evident in neuro

121 Previous studies on rats have shown that the opioid antagonist naloxone attenuates amphetamine-induce

122 l and electrophysiological studies using the opioid antagonist naloxone demonstrate that endogenous o

123 Meanwhile, the opioid antagonist naloxone increased the density of spin

124 k), methionine-enkephalin (Met-Enk), and the opioid antagonist naloxone on gonad development in the E

125 166p-ir was blocked by pretreatment with the opioid antagonist naloxone or the Src kinase inhibitor 4

126 Here we reveal that the opioid antagonist naloxone possesses potent analgesic ac

127 Application of the opioid antagonist naloxone potentiates noxious periphera

128 The opioid antagonist naloxone prevented mossy fiber LTP in

129 The u-opioid antagonist naloxone significantly increased overa

130 t yohimbine, 5 mg/kg, i.p.; that of F by the opioid antagonist naloxone, 5 mg/kg, i.p.

131 zation was reversed by administration of the opioid antagonist naloxone, apparently acting in the spi

132 e inhibitory effects were insensitive to the opioid antagonist naloxone, but were effectively antagon

133 tenuated by pretreatment of animals with the opioid antagonist naloxone, confirming opioid receptor-m

134 Treatment with the opioid antagonist naloxone, the agonist etorphine, and o

135 il-induced antinociception comparable to the opioid antagonist naloxone, the standard of care drug fo

136 inactive thiirane analogue of 14,15-EET, the opioid antagonist naloxone, the thromboxane mimetic U466

137 temic administration of the CNS-nonpenetrant opioid antagonist naloxone-methiodide did not induce an

138 is short-lasting and can be reversed by the opioid antagonist naloxone.

139 tagonist SR141716A (1 microM) but not by the opioid antagonist naloxone.

140 ssion, and its response is attenuated by the opioid antagonist naloxone.

141 tory drive) that was rapidly reversed by the opioid antagonist naloxone.

142 by pretreatment with pertussis toxin or the opioid antagonist naloxone.

143 the pretreatment with pertussis toxin or the opioid antagonist naloxone.

144 After chronic treatment, the mu-opioid antagonists naloxone and beta-chlornaltrexamine (

145 ediated antihyperalgesia was reversed by the opioid antagonists naloxone and naloxone methiodide (a p

146 thy volunteers and their reversal by the pan-opioid antagonists naloxone and naltrexone and evidence

147 mice pretreated with the readily reversible opioid antagonists naloxone or buprenorphine before norB

148 FQ/N analgesia is readily antagonized by the opioid antagonists naloxone or diprenorphine, despite th

149 the effects of NPY is pretreatment with the opioid antagonists naloxone or naltrexone.

150 The opioid antagonists naloxone/naltrexone are involved in i

151 er a dopamine antagonist (flupentixol) or an opioid antagonist (naloxone) into the nucleus accumbens.

152 ted by means of GABA B agonist (baclofen) or opioid antagonist (naloxone) treatments.

153 The non-selective opioid antagonist, naloxone, returned the water content

154 uch as the benzomorphans, and the classic mu opioid antagonists, naloxone, naltrexone, and nalmefene.

155 Rats pretreated with the non-selective opioid antagonist naltrexone (1.25-3.75 microg/0.25 micr

156 ticipants received either the competitive mu-opioid antagonist naltrexone (25 mg) or a placebo in a r

157 Intrathecal injection of the opioid antagonist naltrexone (97 nmol) partially reverse

158 , [Met(5)]-enkephalin) and a low dose of the opioid antagonist naltrexone (LDN) on expression of myel

159 l(5)]-enkephalin (DAMGO) in one site and the opioid antagonist naltrexone (NTX) in the other site.

160 l(5)]-enkephalin (DAMGO) in one site and the opioid antagonist naltrexone (NTX) in the other site.

161 inical and clinical studies suggest that the opioid antagonist naltrexone (NTX) is effective in reduc

162 tions and topical applications of the potent opioid antagonist naltrexone (NTX).

163 whether this effect might be blocked by the opioid antagonist naltrexone (NTX).

164 To study whether intervention by the opioid antagonist naltrexone (NTX; 30 mg/kg, twice daily

165 The administration of the opioid antagonist naltrexone blocked placebo analgesia a

166 In these animals, the opioid antagonist naltrexone elicited antinociceptive ef

167 The oral formulation of the opioid antagonist naltrexone has shown limited effective

168 The opioid antagonist naltrexone has shown promise to reduce

169 in virgin female rats, and injection of the opioid antagonist naltrexone into the VTA disrupts the o

170 bilateral intra-VTA injection of either the opioid antagonist naltrexone methobromide (quaternary na

171 ighteen mothers received an injection of the opioid antagonist naltrexone or saline for 5 days per we

172 The opioid antagonist naltrexone significantly blocked Salmo

173 which were blocked by pretreatment with the opioid antagonist naltrexone, confirming the opioid natu

174 icantly attenuated in rats trained under the opioid antagonist naltrexone, consistent with an opioid-

175 induced internalization was prevented by the opioid antagonist naltrexone, suggesting that translocat

176 t with the NMDA antagonist memantine and the opioid antagonist naltrexone, when compared with naltrex

177 eous implantation of a pellet containing the opioid antagonist naltrexone.

178 heavy drinking following treatment with the opioid antagonist naltrexone.

179 rescued by a pharmacological chaperone, the opioid antagonist naltrexone.

180 opamine D1 receptor agonist SKF 38393 or the opioid antagonist naltrexone.

181 e was blocked by prior administration of the opioid antagonist naltrexone.

182 Other opioid antagonists (naltrexone, norbinaltorphimine, and

183 use of opioid agonists (heroin, prescription opioids), antagonists (naltrexone), agonist-antagonist c

184 with morphine plus an ultra-low dose of the opioid antagonist, naltrexone (NTX) which blocks opioid-

185 was studied using the potent and long-acting opioid antagonist, naltrexone (NTX; 10(-6) M), and the e

186 that a single dose (5 microg) of the general opioid antagonist, naltrexone reduced feeding elicited b

187 systemic administration of the nonselective opioid antagonist, naltrexone, induces Fos-like immunore

188 gdala could be altered by either the general opioid antagonist, naltrexone, the mu-selective antagoni

189 rough systemic administration of the general opioid antagonist, naltrexone, through central administr

190 The delta-selective opioid antagonist naltrindole (NTI), as well as the kapp

191 The delta-opioid antagonist naltrindole was inactive in both treat

192 The indole moiety in the delta-opioid antagonist, naltrindole (2, NTI), was employed as

193 reverse microdialysis of the selective delta opioid antagonist, naltrindole, on extracellular striata

194 (CNV-NLX), a caged analog of the competitive opioid antagonist NLX, was readily synthesized from comm

195 The kappa-opioid antagonist nor-binalorphimine completely blocked

196 opioid antagonist CTAP (6.6 nMol), the kappa opioid antagonist Nor-binaltorphimine (Nor-BNI, 6.6 nMol

197 effect of U50,488 was abolished by the kappa-opioid antagonist nor-Binaltorphimine dihydrochloride (n

198 oxone (5 mg/kg, s.c.) and kappa(1)-selective opioid antagonist nor-BNI (60 microg, i.c.v.), despite t

199 were not reversed by preincubation with the opioid antagonists nor-binaltorphimine or naltrexone, su

200 In Experiment 2, the kappa opioid antagonist, nor-binaltorphimine (Nor-BNI; 20.0 mi

201 Molecular modifications of both the kappa opioid antagonist norbinaltorphimine (norBNI, 1) and the

202 hibition was partially reversed by the kappa opioid antagonist norbinaltorphimine.

203 indole (NTI), as well as the kappa-selective opioid antagonists norbinaltorphimine (norBNI) and 5'-gu

204 retreatment with the kappa- and mu-selective opioid antagonists norbinaltorphimine and beta-funaltrex

205 A combination of a kappa-opioid antagonist (norbinaltorphimine, 10 mg/kg, s.c.) a

206 interaction by administration of the potent opioid antagonist, NTX, increased the number of epitheli

207 Thus, opioid antagonist-opioid agonist and GABA antagonist-GAB

208 Naltrexone (5 mg/kg, sc), an opioid antagonist, or naltrindole (5 mg/kg, sc), a delta

209 ivalent ligand that contains delta and kappa opioid antagonist pharmacophores linked through a 21-ato

210 ontribute to the autonomic manifestations of opioid antagonist-precipitated withdrawal in morphine-to

211 licited from the amygdala that is blocked by opioid antagonist pretreatment in the ventrolateral peri

212 ether such feeding responses were altered by opioid antagonist pretreatment, and whether such feeding

213 agonists may not be necessary for their pure opioid antagonist properties.

214 we report that mu opioid agonists and kappa opioid antagonists reduce distress from social isolation

215 In each case, these opioid antagonists reduced or eliminated ethanol's reinf

216 ut not delta1 ([D-Ala2,Leu5,Cys6]enkephalin) opioid antagonists reducing each form of intake followin

217 Naloxone, an opioid antagonist, restores HPA axis responses to IL-1be

218 The use of selective opioid antagonists revealed that mu-selective antagonist

219 gonist, buprenorphine (BUP), and a potent mu-opioid antagonist, samidorphan (SAM), would demonstrate

220 oid partial agonist, buprenorphine, and a mu-opioid antagonist, samidorphan, would exhibit antidepres

221 is important for potent and selective kappa opioid antagonist selectivity.

222 mox (DOC-CAM) which acted as a high-affinity opioid antagonist similar to C-CAM but with greater mu s

223 nities for [3H]diprenorphine, a nonselective opioid antagonist, similar to that of the template recep

224 pharmacological blockade with non-selective opioid antagonists such as naloxone and naltrexone is ty

225 To reverse the effects of anesthesia, opioid antagonists such as naloxone are commonly used.

226 chimeric receptor, mu delta2, that classical opioid antagonists such as naloxone, naltrexone, naltrib

227 sn314Ala mutations transform classical delta-opioid antagonists such as naltrindole into potent beta-

228 The results suggest that, like other kappa opioid antagonists such as nor-BNI and GNTI, JDTic requi

229 Opioid antagonists, such as naloxone and naltrexone, eli

230 inhibition of sucrose intake by dopamine and opioid antagonists, suggesting that distinct neurochemic

231 Increasing access to naloxone (an opioid antagonist that can reverse overdose) could slow

232 l withdrawal, by intrathecal injection of an opioid antagonist that does not cross the BBB, provoked

233 Naloxone is a general opioid antagonist that has not been characterized in Ran

234 Nalmefene is a newer opioid antagonist that is structurally similar to naltre

235 knock-in strategy to test the ability of the opioid antagonist to produce analgesic effects.

236 Based on the in vitro ability of opioid antagonists to activate a mu-opioid receptor muta

237 e S196A mutant of the mu-opioid receptor and opioid antagonists to minimize the spectrum of unwarrant

238 ntly increased by general, but not selective opioid antagonist treatment alone in the amygdala, but n

239 Naloxone is an opioid antagonist used to reverse opioid overdose, and t

240 methylnaloxonium (M-NX, a limited diffusion opioid antagonist) was given to rats in a 'low-drive' co

241 volved in the effects of morphine, selective opioid antagonists were microinjected into the lateral v

242 Compound 6 was found to be a mu-opioid antagonist, whereas the constrained analogue 9 di

243 Nalmefene is an opioid antagonist which as a once-a-day tablet formulati

244 f earlier pharmacological manipulations with opioid antagonists, which indicated that activation of m

245 he effects of ADL 8-2698, an investigational opioid antagonist with limited oral absorption that does

246 The highly-selective opioid antagonists yielded similar K(i) values ranging f