ライフサイエンスコーパス: opioid antagonist

1 whether these effects can be blocked via 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 blocked by pretreatment with naloxone, a mu-opioid antagonist.

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

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

7 stemic and central administration of general opioid antagonists.

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

9 administration of appropriately low doses of opioid antagonists.

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

11 lective opioid agonists and highly-selective opioid antagonists.

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

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

14 nduced constipation with peripherally acting opioid antagonists.

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

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

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

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

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

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

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

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

23 5'-regioisomer (GNTI) possessed potent kappa-opioid antagonist activity and high affinity at kappa-re

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

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

26 Yet, opioid antagonists administered into misplaced amygdala

27 In contrast, opioid antagonists administered into misplaced mesenceph

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

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

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

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

32 Opioid antagonists and mixed agonist/antagonists appear

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

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

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

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

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

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

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

40 Opioid antagonists block the positive hedonic response t

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

76 Peripheral opioid antagonists may represent an important therapeuti

77 Opioid antagonists may represent effective treatments fo

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

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

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

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

82 Opioid antagonists modulate cannabinoid effects and may

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

101 -1 in the globus pallidus was blocked by the opioid antagonist naloxone and the mu-selective peptide

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

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

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

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

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

107 166p-ir was blocked by pretreatment with the opioid antagonist naloxone or the Src kinase inhibitor 4

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

109 Application of the opioid antagonist naloxone potentiates noxious periphera

110 The opioid antagonist naloxone prevented mossy fiber LTP in

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

128 The opioid antagonists naloxone/naltrexone are involved in i

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

144 The opioid antagonist naltrexone has shown promise to reduce

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

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

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

148 The opioid antagonist naltrexone significantly blocked Salmo

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

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

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

152 heavy drinking following treatment with the opioid antagonist naltrexone.

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

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

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

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

157 Other opioid antagonists (naltrexone, norbinaltorphimine, and

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

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

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

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

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

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

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

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

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

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

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

169 The kappa-opioid antagonist nor-binalorphimine completely blocked

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

201 Opioid antagonists, such as naloxone and naltrexone, eli

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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