ライフサイエンスコーパス: opioid receptor agonist

1 ity on the A-ring in its activity as a kappa-opioid receptor agonist.

2 e manner with an exogenously administered mu opioid receptor agonist.

3 in amplitude following the exposure to a mu opioid receptor agonist.

4 rin A is also the only known non-nitrogenous opioid receptor agonist.

5 aversion induced by thermal pain or a kappa opioid receptor agonist.

6 2066; spiradoline; 0, 100, 150, or 200 nmol) opioid receptor agonist.

7 t is produced by morphine, a preferential mu-opioid-receptor agonist.

8 y of systemically administered mu, and kappa opioid receptor agonists.

9 eported "cocaine-antagonist" effect of kappa-opioid receptor agonists.

10 responses to the prototypical mu- and delta-opioid receptor agonists.

11 g the signaling profile of most endogenous u-opioid receptor agonists.

12 of neuropathic pain by morphine and other mu-opioid receptor agonists.

13 dependence issues compared with orthosteric opioid receptor agonists.

14 ter antinociceptive effects of GABA(B) or mu-opioid receptor agonists.

15 nt, selective, and orally bioavailable delta opioid receptor agonists.

16 tification of a novel structural class of mu opioid receptor agonists.

17 lu4]deltorphin II (deltorphin II), a delta 2-opioid receptor agonist (20 micrograms per mouse) twice

18 [D-Pen2,D-Pen5]enkephalin (DPDPE), a delta 1-opioid receptor agonist (20 micrograms per mouse) twice

19 sed an increase of maximal binding of the mu-opioid receptor agonist [3H][d-Ala(2),N-Me-Phe(4),Gly(5)

20 o (DAMGO), kappa (U50488), and Delta (DPDPE) opioid receptor agonists 48 hrs after infection.

21 Kappa opioid receptor agonists acting peripherally had differe

22 Analgesia induced by a kappa opioid receptor agonist administered at the supraspinal

23 ta- ([D-Pen2, D-Pen5]enkephalin- and SNC-80) opioid receptor agonists affected responses to CRD.

24 ng upon their nervous system site of action, opioid receptor agonists alter food consumption, pain pe

25 Morphine, a preferential mu-opioid receptor agonist, alters astroglial development b

26 orin A is the first reported non-nitrogenous opioid receptor agonist and (2) its effects are not medi

27 Salvinorin A (SA) is a kappa-opioid receptor agonist and atypical dissociative halluc

28 re, a combination of subanalgesic doses of u-opioid receptor agonist and CB1R agonist markedly reduce

29 ent with mixed opioid effects (mu- and kappa-opioid receptor agonist and delta-opioid receptor antago

30 icacy and safety of a minimally absorbed, mu-opioid receptor agonist and delta-opioid receptor antago

31 Buprenorphine, the partial mu-opioid receptor agonist and kappa-, delta-opioid recepto

32 ublished lead peptide KGFF09, which contains opioid receptor agonist and neuropeptide FF receptor ant

33 Current treatments consist of opioid receptor agonists and antagonists, which are safe

34 ips between feeding responses produced by mu opioid receptor agonists and melanocortin-3 or 4 (MC-3/4

35 ionamide derivatives was developed as dual u-opioid receptor agonists and o(1) receptor antagonists.

36 N-Me-Phe4, Gly-ol5]-enkephalin (DAMGO), a mu opioid receptor agonist, and of bicuculline, a GABAA rec

37 ous natural compound known to function as an opioid-receptor agonist, and is undergoing clinical tria

38 Buprenorphine is a mixed opioid receptor agonist-antagonist used clinically for m

39 epressants such as sertraline or doxepin, or opioid receptor agonist/antagonists such as naltrexone o

40 n mice leads to formation of (a) a potent mu opioid receptor agonist antinociceptive agent, 7-hydroxy

41 3 trials of difelikefalin, a selective kappa-opioid receptor agonist approved for treating moderate-t

42 Opioid receptor agonists are known to alter the activity

43 Selective delta opioid receptor agonists are promising potential therape

44 ly reduced analgesic effects of mu and delta opioid receptor agonists at both spinal and supraspinal

45 groups: a) pentazocine (0.3 mg/kg), a delta-opioid receptor agonist; b) pentazocine pretreated with

46 of this study was to assess a non-selective opioid receptor agonist, biphalin, in decreasing reducin

47 ce on the response to the prototypical kappa-opioid receptor agonist, but decreases responses to the

48 Mice were rendered tolerant to opioid receptor agonists by injecting morphine (20 mg/kg

49 red integrator sensors for the mu- and kappa-opioid receptor agonists called M- and K-Single-chain Pr

50 Thus, our results suggest that kappa opioid receptor agonists can exert direct inhibitory act

51 ed target for analgesia(1), yet conventional opioid receptor agonists cause serious adverse effects,

52 Morphine is a mu-opioid receptor agonist commonly used for pain treatment

53 We propose that G protein-biased mu opioid receptor agonists, currently in development as an

54 The opioid receptor agonist D-Ala(2)-N-Me-Phe(4),Gly-ol(5)-e

55 ore ischemic preconditioning or given the mu-opioid receptor agonist D-Ala,2N-Me-Phe,4glycerol5-enkep

56 gically from the nucleus accumbens by the mu-opioid receptor agonist D-Ala-Tyr-Gly-NMePhe-Gly-OH (DAM

57 duced by intra-accumbens injection of the mu-opioid receptor agonist D-Ala2-N-Me-Phe4-gly5-ol-enkepha

58 the spinal cord, brief application of the mu-opioid receptor agonist (D-Ala(2),N-Me-Phe(4),Gly-ol(5))

59 Intrathecal injection of the mu-opioid receptor agonist [D-Ala(2), NMe-Phe(4), Gly-ol(5)

60 which allowed for coadministration of the mu-opioid receptor agonist [D-Ala(2), NMe-Phe(4), Gly-ol(5)

61 hich allowed for co-administration of the mu-opioid receptor agonist [D-Ala(2), NMe-Phe(4), Gly-ol(5)

62 sic and antinociceptive effects of the delta opioid receptor agonist [D-Ala(2),Glu(4)]deltorphin were

63 The antihyperalgesic potency of the mu opioid receptor agonist [D-Ala(2),N-Me-Phe(4),Gly(5)-ol]

64 und that the disinhibitory effects of the mu-opioid receptor agonist [D-Ala2, MePhe4,Gly-(ol)5]-enkep

65 investigated the effects of the selective mu-opioid receptor agonist [D-Ala2-N-Me-Phe4,Gly-ol5]-enkep

66 The delta-opioid receptor agonist [D-Pen2,5]-enkephalin (DPDPE) pr

67 e inhibited by both nociceptin and the delta-opioid receptor agonist, [D-ala2, D-leu5]-enkephalin (DA

68 oiontophoretic application of a selective mu-opioid receptor agonist, [D-Ala2,N-Me-Phe4,Gly5-ol]enkep

69 contrast, application of a selective delta 1-opioid receptor agonist, [D-Pen2,5]enkephalin (DPDPE), r

70 The mu-opioid receptor agonist DAGO reversibly suppressed high-

71 rons responded to bath application of the mu-opioid receptor agonist DAMGO (93%) or the GABA(B) recep

72 erridge observed that an injection of the mu-opioid receptor agonist DAMGO (D-ala(2) -N-Me-Phe(4) -Gl

73 vation through both pathways, whereas the mu opioid receptor agonist DAMGO decreased D2-receptor acti

74 ic inhibition of VTA GABA(A) IPSCs by the mu-opioid receptor agonist DAMGO is significantly reduced i

75 ns, and these IPSCs were inhibited by the mu opioid receptor agonist DAMGO.

76 ced by nucleus accumbens injection of the mu-opioid receptor agonist DAMGO.

77 reducing inhibition of cAMP signaling by mu-opioid receptor agonists DAMGO and morphine.

78 Administration of mu- and kappa-opioid receptor agonists (DAMGO and U50488H respectively

79 In contrast, treatment with a mu opioid receptor agonist, DAMGO, or a delta opioid recept

80 Low concentrations (< nM) of most opioid receptor agonists decrease the K+ conductance (gK

81 bination of subanalgesic doses of CB1R and u-opioid receptor agonists decreased VMR; importantly, thi

82 bath-applied met-enkephalin, a nonselective opioid receptor agonist, decreased the number of tetrodo

83 In a phase 2 study of the mixed mu-opioid receptor agonist/delta-opioid receptor antagonist

84 substrates, estrone 3-sulfate and two delta-opioid receptor agonists, deltorphin II, and [D-penicill

85 Recently, a series of mu and delta opioid receptor agonists [dermorphins and deltorphins] a

86 kappa- (U69 593) or delta-selective (DPDPE) opioid receptor agonists did not affect IBa.

87 o evaluate the impact of the selective kappa-opioid receptor agonist difelikefalin (DFK) on pruritus

88 Here, we demonstrate that delta opioid receptor agonists differentially recruit arrestin

89 tive possibility; whether tolerance of delta opioid receptor agonists (DORs) could be related to agon

90 n contrast, kappa- (U-50,488 and fedotozine) opioid receptor agonists dose-dependently attenuated res

91 has been known for a number of years that mu-opioid receptor agonists (e.g., morphine, beta-endorphin

92 st actions but differ in the nature of their opioid receptor agonist effects; 2a is a predominant MOR

93 ervised withdrawal include treatment with mu-opioid receptor agonists, (eg, methadone), partial agoni

94 Mixed NOP/opioid receptor agonists elicit similar effects to stron

95 nduced by incubating the slices with a micro-opioid receptor agonist (endomorphin-2, 100 nM).

96 This study examined the effects of the kappa opioid receptor agonists fedotozine and U50488H on the a

97 In Experiment 3, increasing doses of the mu-opioid receptor agonist fentanyl (0, 0.0004, 0.004, and

98 self-administration of the high-efficacy mu opioid receptor agonist fentanyl and characterized MCAM

99 is locus also affected sensitivity to the mu-opioid receptor agonist fentanyl.

100 As a potent mu-opioid receptor agonist, fentanyl canonically inhibits e

101 1 (NeuroD) is modulated differentially by mu-opioid receptor agonists; fentanyl increases NeuroD leve

102 n, and identify the cellular target of kappa opioid receptor agonists for the inhibition of itch.

103 Cultures were treated with the selective mu opioid receptor agonist H-Tyr-Pro-Phe (N-Me)-D-Pro-NH2 (

104 Difelikefalin, a selective kappa opioid receptor agonist, has shown efficacy in other chr

105 Systemically active, nonpeptidic delta opioid receptor agonists have been shown to produce anti

106 While synergistic actions of mu-opioid receptor agonists have been shown, it is unclear

107 Selective, nonpeptidic delta opioid receptor agonists have been the subject of great

108 , but inhibition of Ca2+ channel currents by opioid receptor agonist in dorsal root ganglion cells wa

109 rance to these effects of U-50,488H, a kappa-opioid receptor agonist in mice and rats.

110 tolerance to the analgesic action of delta 2-opioid receptor agonist in the mouse.

111 een found to be a potent and selective kappa opioid receptor agonist in vitro and in vivo.

112 , but not microinjection of the mu- or kappa-opioid receptor agonists in control shRNA-treated animal

113 nce for the psychotomimetic effects of kappa opioid receptor agonists in healthy volunteers and their

114 eptive action of mu- but not kappa- or delta-opioid receptor agonists in mice.

115 gate the clinical utility of kappa and delta-opioid receptor agonists in the peripheral setting.

116 They act as potent kappa opioid receptor agonists in vitro and in vivo, but exhib

117 -Phe(4), Gly-ol(5)]-enkephalin (DAMGO), a mu-opioid receptor agonist, in the periacqueductal gray and

118 sex in mediating the larger magnitude of mu-opioid receptor agonist-induced analgesia in male relati

119 Butorphanol (BT), a mixed kappa- and mu-opioid receptor agonist, induces vigorous food intake in

120 Kappa opioid receptor agonists inhibit VTA DA neurons that pro

121 Microinjection of a mu opioid receptor agonist into the BLA resulted in a time

122 following the administration of mu and kappa opioid receptor agonists into the periaqueductal gray ar

123 c, are reduced after local infusion of kappa opioid receptor agonists into the VTA.

124 ining addicted pregnant women on long-acting opioid receptor agonist is the most common strategy to m

125 alkaloid morphine, in addition to being a mu-opioid receptor agonist, is a potent competitive inhibit

126 Coadministration of kappa-opioid receptor agonists (kappa-agonists) with cocaine p

127 kappa-opioid receptor agonists (kappa-ORAs) have been shown to

128 overexpression of enkephalin, an endogenous opioid receptor agonist, leading to opioid-dependent ana

129 The opioid receptor agonist, leu-enkephalin, was predicted t

130 eaves of Salvia divinorum, is a potent kappa-opioid receptor agonist, making it an attractive scaffol

131 ggest these diazaheterocyclic mixed activity opioid receptor agonists may hold potential as new analg

132 ponsiveness to GABAB, but not to delta or mu opioid receptor agonist-mediated analgesia specifically

133 ihyperalgesic and antinociceptive effects of opioid receptor agonists microinjected in the rostral ve

134 elective (DAMGO) and delta-selective (DPDPE) opioid receptor agonists, mimicked the effect of morphin

135 Therefore, by regulating NeuroD activity, mu-opioid receptor agonists modulate the stability of dendr

136 Rats were pretreated with the opioid receptor agonist morphine (1 mg/kg; intraperitone

137 A 5-minute exposure of the myocytes to the opioid receptor agonist morphine protected the myocytes

138 abrogated by systemic administration of the opioid receptor agonist morphine.

139 ha(2)-adrenoceptor agonist clonidine, the mu-opioid receptor agonists morphine and methadone, and the

140 We then show that the kappa opioid receptor agonist nalfurafine relieves itch by sel

141 As gabapentin and the kappa opioid receptor agonist, nalfurafine, but not morphine,

142 This study focuses on the effect of mu-opioid receptor agonists on CXCR4 signaling in neurons a

143 The complementary action of CB1 and opioid receptor agonists on populations of DRG neurons p

144 as investigated the effect of morphine (a mu-opioid receptor agonist) on the cardiac chronotropic res

145 Both delta 1- and delta 2-opioid receptor agonist, on chronic administration, resu

146 tions since these were not affected by kappa-opioid receptor agonists or antagonists.

147 lgesic and antinociceptive effects of the mu opioid receptor agonist (ORA) [D-Ala(2), NMePhe(4), Gly(

148 (PhNX), photoactivatable variants of the mu opioid receptor agonist oxymorphone and the antagonist n

149 It is concluded that mu- and delta-opioid receptor agonists produce a predominantly inhibit

150 Mu-opioid receptor agonists represent mainstays of pain man

151 II (DELT), selective mu, delta1, and delta2 opioid receptor agonists, respectively, in mice selectiv

152 halin (DPDPE) which are mu- kappa- and delta-opioid receptor agonists, respectively, were determined

153 lin (DPDPE), which are mu-, kappa- and delta-opioid receptor agonists, respectively, were determined

154 esigned as conformationally restricted kappa-opioid receptor agonists restricted to the periphery.

155 , multiple injections of delta 1- or delta 2-opioid receptor agonists results in the development of t

156 sion of phasic dopamine release by the kappa-opioid receptor agonist, salvinorin A, supporting a sele

157 stereoenantiomer, d-morphine, an ineffective opioid receptor agonist, significantly reduced LPS- or 1

158 The highly selective delta (delta) opioid receptor agonist SNC 80 [(+)-4- [(alpha R)-alpha-

159 The delta-opioid receptor agonist, SNC 80, did not inhibit PACAP-i

160 is study examined if the delta-opioid (delta-opioid) receptor agonist, SNC-121, can improve retinal f

161 A high-internalizing delta opioid receptor agonist (SNC80) preferentially recruited

162 lls, the potency and maximal effect of delta-opioid receptor agonist (SNC80)-mediated inhibition of f

163 u opioid receptor agonist, DAMGO, or a delta opioid receptor agonist, SNC80, did not prevent angiogen

164 m PV and nNos-expressing interneurons by a u-opioid receptor agonist, strongly enhances LTP in 4-week

165 Potent, selective, and efficacious delta-opioid receptor agonists such as (+)-4-[(alphaR)-alpha-(

166 IH.SIGNIFICANCE STATEMENT Clinically used mu-opioid receptor agonists such as fentanyl can produce hy

167 has been demonstrated previously that kappa opioid receptor agonists, such as dynorphin, inhibit oxy

168 In Caenorhabditis elegans, opioid receptor agonists, such as morphine, mimic seroto

169 receptor agonists, endotoxin derivatives, or opioid receptor agonists), suggesting that this phenomen

170 In Caenorhabditis elegans, opioid receptor agonists suppress the overall withdrawal

171 pondingly, in vitro bath application of a mu opioid receptor agonist suppresses the activity of the f

172 cyclase cDNA imparted to dopamine and to mu-opioid receptor agonists the ability to modulate the act

173 her buprenorphine or the G protein-biased mu opioid receptor agonist TRV130.

174 a potent, selective, and G protein biased mu opioid receptor agonist, TRV130 ((R)-30).

175 adenosine (200 microM) nor the selective mu-opioid receptor agonist Tyr-D-Ala-Gly-MePhe-Gly-ol (DAMG

176 ocaine (80 microM) or to the kappa-selective opioid receptor agonist U-50,488H (1 microM) displayed a

177 al hypothalamus or administration of a kappa opioid receptor agonist (U-50,488) or antagonist (nor-bi

178 e (threshold-elevating) effects of the kappa-opioid receptor agonist U50,488.

179 hilar pathway were decreased by the kappa(1) opioid receptor agonist U69,593, an effect blocked by th

180 set and recovery from tolerance to the kappa opioid receptor agonist (U69,593) which were measured wi

181 onditioned place aversion (CPA) to the kappa-opioid receptor agonist U69593 (2 x 0.16 mg/kg s.c.).

182 B) agonist baclofen (1 microM) and the kappa-opioid receptor agonist U69593 [(+)-(5alpha,7alpha,8beta

183 Bath application of the kappa opioid receptor agonist U69593 decreased D2-receptor act

184 Methadone is a mu-opioid receptor agonist used for treating opiate depende

185 In addition, an opioid receptor agonist was found to increase the oxLDL

186 TAN-67, a delta1-opioid receptor agonist, was administered 10 or 30 mg/kg

187 the tolerance and physical dependence of mu opioid receptor agonists, we have investigated the possi

188 and experimental evidence from several kappa opioid receptor agonists, we illustrate a "competitive"

189 of VP afferents and their sensitivity to mu opioid receptor agonists, we virally expressed channel r

190 lu4 deltorphin II (deltorphin II), a delta 2-opioid receptor agonist were determined in mice.

191 f activation, while neither delta- nor kappa-opioid receptor agonists were effective in modifying cal

192 of tolerance to the analgesic effects of mu-opioid receptor agonists, which are necessary to improve

193 Etorphine is an non-selective opioid receptor agonist with very potent analgesic effec

194 design novel mixed mu (MOR) and kappa (KOR) opioid receptor agonists with reduced arrestin signaling

195 differentially affect feeding elicited by mu opioid receptor agonists within the nucleus accumbens sh

196 pe mice, suggesting that G protein biased mu opioid receptor agonists would be more efficacious with