ライフサイエンスコーパス: kappa opioid receptor

1 anomolar to low nanomolar K(e) values at the kappa opioid receptor.

2 lbene that functions as an antagonist of the kappa opioid receptor.

3 oid peptides are endogenous agonists for the kappa opioid receptor.

4 ent and probes for exploring the role of the kappa-opioid receptor.

5 understanding of its role in binding to the kappa-opioid receptor.

6 reciable binding affinity for delta, mu, and kappa opioid receptors.

7 orphin A (Dyn A) is an endogenous ligand for kappa opioid receptors.

8 by their binding affinity at mu, delta, and kappa opioid receptors.

9 ioid receptors or singly expressed delta and kappa opioid receptors.

10 not distinguish ORL1 from the mu, delta, and kappa opioid receptors.

11 nic (m2), adenosine (A1), and mu, delta, and kappa opioid receptors.

12 y in the adenylyl cyclase assay using cloned kappa opioid receptors.

13 competitive binding assays at mu, delta, and kappa opioid receptors.

14 s exhibited similar nanomolar affinities for kappa opioid receptors.

15 nuclei, structures expressing high levels of kappa opioid receptors.

16 onally potent agonist in cells expressing mu/kappa-opioid receptors.

17 rphin which can inhibit dopamine release via kappa-opioid receptors.

18 unctional activity of human mu-, delta-, and kappa-opioid receptors.

19 es of morphine appear to be mediated through kappa-opioid receptors.

20 through a combined action at mu-, delta- and kappa-opioid receptors.

21 ty against the cloned human mu-, delta-, and kappa-opioid receptors.

22 K(i) ratio (kappa/mu/delta) = 1/194/330) for kappa-opioid receptors.

23 ference of this residue for interaction with kappa-opioid receptors.

24 produce dynorphin, an endogenous agonist of kappa-opioid receptors.

25 nregulated), hypocretin receptor 1 (Hcrtr1), kappa opioid receptor 1 (Oprk1), and transient receptor

26 alues suggests that the potent and selective kappa opioid receptors 4, 5, 13, and 14 deserve consider

27 Finally, we demonstrate that blockade of kappa-opioid receptors (500 ng nor-BNI) within the nucle

28 We previously showed that kappa-opioid receptor activation of JNK by one class of

29 ously demonstrated that mu and delta but not kappa opioid receptors affect EA anti-hyperalgesia in an

30 5)]Dyn A-(1-11)NH(2) exhibited 2-fold higher kappa opioid receptor affinity and 16-fold higher select

31 The higher kappa-opioid receptor affinity of the (R)-Atc4 analogue

32 Atc4,D-Ala8]Dyn A-(1-11)NH2 exhibited higher kappa-opioid receptor affinity than the (S)-Atc4 isomer.

33 phe4,D-Ala8]Dyn A-(1-11)NH2 exhibited higher kappa-opioid receptor affinity than the D-Homophe4 isome

34 In addition to high kappa-opioid receptor affinity they demonstrate high sel

35 show single-digit nanomolar to subnanomolar kappa-opioid receptor affinity, full kappa agonistic act

36 rminal alpha-helix associated with decreased kappa-opioid receptor affinity.

37 Analgesia induced by a kappa opioid receptor agonist administered at the supras

38 has been found to be a potent and selective kappa opioid receptor agonist in vitro and in vivo.

39 Bath application of the kappa opioid receptor agonist U69593 decreased D2-recept

40 nd for aversion induced by thermal pain or a kappa opioid receptor agonist.

41 ral agent with mixed opioid effects (mu- and kappa-opioid receptor agonist and delta-opioid receptor

42 ve-like (threshold-elevating) effects of the kappa-opioid receptor agonist U50,488.

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

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

45 the leaves of Salvia divinorum, is a potent kappa-opioid receptor agonist, making it an attractive s

46 uppression of phasic dopamine release by the kappa-opioid receptor agonist, salvinorin A, supporting

47 tionality on the A-ring in its activity as a kappa-opioid receptor agonist.

48 Kappa opioid receptor agonists inhibit VTA DA neurons th

49 the NAc, are reduced after local infusion of kappa opioid receptor agonists into the VTA.

50 tions and experimental evidence from several kappa opioid receptor agonists, we illustrate a "competi

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

52 larizations since these were not affected by kappa-opioid receptor agonists or antagonists.

53 were designed as conformationally restricted kappa-opioid receptor agonists restricted to the periphe

54 alogues showed sub-nanomolar potency for the kappa opioid receptor and were highly selective relative

55 gues do not show affinity for both delta and kappa opioid receptors and bind only poorly to the mu re

56 aboratory, showed sub-nanomolar affinity for kappa opioid receptors and potent agonist activity in th

57 ologous interaction between the mu, delta or kappa opioid receptors and the receptors for the chemoki

58 by their binding affinity at mu, delta, and kappa opioid receptors and their relative efficacy in th

59 ors could increase the binding of nor-BNI to kappa opioid receptors and vice versa, suggesting recipr

60 ressed by the activation of mu-, delta-, and kappa-opioid receptors and by adrenergic alpha2A recepto

61 vivo functional relevance of heteromeric mu/kappa-opioid receptors and suggests an approach to poten

62 an be rescued by the expression of the human kappa opioid receptor, and injection of human opioid rec

63 g K(i) values of 0.47 nM for both the mu and kappa opioid receptors, and 4a, having K(i) values of 0.

64 s such as the beta2-adrenergic receptor, the kappa-opioid receptor, and the parathyroid hormone recep

65 bits basal forebrain cholinergic neurons via kappa-opioid receptors, and decreases afferent excitator

66 r define the pharmacophore for this class of kappa opioid receptor antagonist and has identified new

67 cle, EA at 10 Hz plus either a mu, delta, or kappa opioid receptor antagonist did not significantly d

68 5a, KAA-1) as the first potent and selective kappa opioid receptor antagonist from the 5-(3-hydroxyph

69 (JDTic, 1) as the first potent and selective kappa opioid receptor antagonist from the trans-3,4-dime

70 receptors was the most potent and selective kappa opioid receptor antagonist identified.

71 east as potent and selective as nor-BNI as a kappa opioid receptor antagonist in the [35S]GTP-gamma-S

72 receptor-1 antagonist antalarmin but not the kappa opioid receptor antagonist JDTic.

73 benzamide (11a), a compound that showed good kappa opioid receptor antagonist properties.

74 ptor antagonist, naltrexone or the selective kappa opioid receptor antagonist, nor-binaltorphimine, b

75 identified as the first potent and selective kappa-opioid receptor antagonist from the trans-3,4-dime

76 Derivatives of the highly selective kappa-opioid receptor antagonist GNTI (2a) have been pre

77 tra-pPVT administration of OrxA+/-DynA+/-the kappa-opioid receptor antagonist nor-binaltorphimine (No

78 retory vesicles) and by nor-binaltorphimine (kappa-opioid receptor antagonist), but not by an oxytoci

79 ce with an ultra-low-dose (0.1 ng/kg) of the kappa-opioid receptor antagonist, nor-binaltorphimine (n

80 release in VP neurons was also blocked by a kappa-opioid receptor antagonist.

81 ficacy and thus represents a novel selective kappa-opioid receptor antagonist.

82 Animal studies suggest that kappa opioid receptor antagonists (KORAn) potentially co

83 mediate the response, selective mu, delta or kappa opioid receptor antagonists were microinjected int

84 l of the analogues were potent and selective kappa opioid receptor antagonists.

85 rest in the discovery and development of new kappa opioid receptor antagonists.

86 racterize the SAR of the compound 3 class of kappa opioid receptor antagonists.

87 s from the pooled data set of delta, mu, and kappa opioid receptor antagonists.

88 terials and their use in preparing potential kappa opioid receptor antagonists.

89 hat the duration of action of small molecule kappa-opioid receptor antagonists in vivo is determined

90 Variations in OPRK1, which encodes the kappa-opioid receptor, are associated with the risk for

91 to develop a new Gi-coupled DREADD using the kappa-opioid receptor as a template (KORD) that is activ

92 naling than in regulating the mu, delta, and kappa opioid receptors, as measured by the effectiveness

93 and delta opioid receptors at 2-15 Hz and by kappa opioid receptor at 100 Hz.

94 hanced both micro-opioid receptor reward and kappa-opioid receptor aversion.

95 ach to restrict expression of the inhibitory kappa opioid-receptor based DREADD (KORD) in vSub-->NAc

96 The pharmacological blockade of kappa-opioid receptors before the extinction trials but

97 ts a gauche (-) or trans conformation in the kappa-opioid receptor binding site.

98 Mu/kappa opioid-receptor blockade and activation had exagge

99 ses food intake, and the LHa contains mu and kappa opioid receptors, both of which are involved in fe

100 oral responses suggests an activation of the kappa opioid receptor by a stress-induced release of dyn

101 inhibits MCPO/SI cholinergic neurons through kappa-opioid receptors by (1) activation of a G protein-

102 (ORL1) receptor or one of the mu, delta, and kappa opioid receptors, by transfecting dual-expression

103 ity in this series for coexpressed delta and kappa opioid receptors (CDK).

104 ppreciable selectivity for delta over mu and kappa opioid receptors (delta/mu = 80; delta/kappa > 200

105 e transmembrane helices (TMs) 7 of delta and kappa opioid receptors (deltaOR and kappaOR) that are on

106 heir in vitro efficacy at the mu, delta, and kappa opioid receptors determined and compared to JDTic

107 eir binding affinities at the mu, delta, and kappa opioid receptors determined.

108 After they are released, they activate kappa opioid receptors distributed throughout the brain

109 Interestingly, a selective antagonist of kappa-opioid receptors enhanced activity of the hypocret

110 onstrated that traditional mu(1), delta, and kappa opioid receptor gene expression is not detected in

111 ablished the colocalization of mu-opioid and kappa-opioid receptor genes and OT genes at the OT-relea

112 Dynorphin, an endogenous ligand of kappa (kappa) opioid receptors, has multiple roles in the brain

113 crease selectivity for the delta over mu and kappa opioid receptors have been predicted on the basis

114 al studies suggesting the existence of delta-kappa opioid receptor heterodimers/oligomers in the spin

115 ndular epithelial cell 1) bound to the human kappa opioid receptor (hKOPR) and promoted cell surface

116 ted protein (MAP) family, bound to the human kappa opioid receptor (hKOPR) and promoted hKOPR cell su

117 he proteins co-immunoprecipitated with human kappa-opioid receptor (hKOPR) from extracts of solubiliz

118 /EBP50) co-immunoprecipitated with the human kappa opioid receptor (hKOR) and that its overexpression

119 that interacts with the C-tail of the human kappa opioid receptor (hKOR) by yeast two-hybrid screeni

120 e present study examined the distribution of kappa opioid receptor immunoreactivity in the RVM of mal

121 imals by the expression of npr-17 or a human kappa opioid receptor in the two ASI sensory neurons, wi

122 First, Dbx1 preBotC neurons express kappa-opioid receptors in addition to mu-opioid receptor

123 A) that selectively activates heteromeric mu/kappa-opioid receptors in HEK-293 cells and induces pote

124 logue antagonizes dynorphin A-(1-13)NH(2) at kappa-opioid receptors in the adenylyl cyclase assay (K(

125 ere pan-agonists, binding to mu-, delta-, or kappa-opioid receptors in the low nanomolar range (2.2-3

126 ks acute analgesic tolerance to morphine and kappa opioid receptor inactivation in vivo.

127 pJNK-ir did not increase in mice lacking the kappa-opioid receptor; increased pJNK-ir returned to bas

128 gation of bivalent ligands at mu, delta, and kappa opioid receptors is focused on the preparation of

129 The kappa-opioid receptor is a widely expressed G-protein-co

130 ral basis to salvinorin A recognition of the kappa-opioid receptor is evaluated using a combination o

131 d exhibit low nanomolar binding affinity for kappa opioid receptors (K(i) = 0.84-11 nM).

132 anterior insula with a downregulation of the kappa opioid receptor (Kappa), as well as decreased DNA

133 is an effective PAM at the mu-OR and at the kappa-opioid receptor (kappa-OR), but it is ineffective

134 respiratory drive, mood, and--in the case of kappa-opioid receptor (kappa-OR)--dysphoria and psychoto

135 Mice lacking the kappa opioid receptor (kappaOR) and adenoviral vectors o

136 The dynorphin (DYN)-kappa opioid receptor (kappaOR) system has been implicat

137 Among the opioid receptors, the kappa-opioid receptor (kappaOR) has been gaining conside

138 Antagonists of glucocorticoid receptors and kappa opioid receptors (kappaORs) were administered at v

139 Stressful experiences potently activate kappa opioid receptors (kappaORs).

140 The kappa-opioid receptor (KOP-r) system and its endogenous

141 The present studies examined the kappa-opioid receptor (KOP-R) system in Withdrawal Seizu

142 0,488H promoted phosphorylation of the mouse kappa opioid receptor (KOPR) at residues S356, T357, T36

143 kappa-Opioid receptors (KOPr; encoded by OPRK1), and the

144 CE STATEMENT Emerging evidence suggests that kappa opioid receptor (KOR) activation can selectively m

145 We hypothesized that kappa opioid receptor (KOR) activation during chronic op

146 endogenous dynorphin opioids and subsequent kappa opioid receptor (KOR) activation.

147 r(1)]Dyn A-(1-11)NH(2) resulted in increased kappa opioid receptor (KOR) affinity for all of the line

148 y 0.5 nM) to both receptors, but also showed kappa opioid receptor (KOR) agonist activity.

149 Dual-acting kappa opioid receptor (KOR) agonist and mu opioid recept

150 Here we show that kappa opioid receptor (KOR) agonists act as anti-angioge

151 Kappa opioid receptor (KOR) agonists have the potential

152 Kappa opioid receptor (KOR) agonists such as U-50488H an

153 The kappa opioid receptor (KOR) and its endogenous agonist,

154 th varying pharmacological properties at the kappa opioid receptor (KOR) and mu opioid receptor (MOR)

155 roxyphenyl) piperidine (JDTic) are selective kappa opioid receptor (KOR) antagonists having very long

156 We have studied changes in kappa opioid receptor (KOR) binding availability in vivo

157 mRNA of kappa opioid receptor (KOR) can be transported to nerve

158 ond and the third generation ones showed MOR/kappa opioid receptor (KOR) dual selectivity.

159 The mouse kappa opioid receptor (KOR) gene is constitutively expre

160 1-13) peptide (dynorphin) bound to the human kappa opioid receptor (KOR) has been determined by liqui

161 This study reveals a functional role for kappa opioid receptor (KOR) in EGF-stimulated neurite ex

162 AtT-20 cells expressing the wild-type kappa opioid receptor (KOR) increased phospho-p38 MAPK f

163 The expression of kappa opioid receptor (KOR) is subjected to both transcr

164 The kappa opioid receptor (KOR) is widely expressed in the C

165 Kappa opioid receptor (KOR) ligands alter nociceptive re

166 as the agonist effect of beta-FNA is clearly kappa opioid receptor (KOR) mediated.

167 Activation of the dynorphin/kappa opioid receptor (KOR) system by either repeated st

168 The endogenous dynorphin-kappa opioid receptor (KOR) system encodes the dysphoric

169 Given that the kappa opioid receptor (KOR) system has been implicated i

170 lts suggest that activation of the dynorphin/kappa opioid receptor (KOR) system is likely to play a m

171 have shown that activation of the dynorphin-kappa opioid receptor (KOR) system leads to aversive, dy

172 the opioid receptors with preference for the kappa opioid receptor (KOR), and its structure-activity

173 at activation of the dynorphin receptor, the kappa opioid receptor (KOR), is required for the BDNF-me

174 (d-Asp(5),Dap(8))]dynorphin A(1-11)NH2) is a kappa opioid receptor (KOR)-selective antagonist in vitr

175 ibutable to the endogenous activation of the kappa opioid receptor (KOR).

176 of Netrin-1 in translational stimulation of kappa opioid receptor (KOR).

177 is a new antagonist PET radioligand for the kappa opioid receptor (KOR).

178 eceptor gene (NK3) and the Dyn receptor [the kappa opioid receptor (KOR)] gene.

179 Using a phosphoselective antibody [kappa opioid receptor (KOR-P)] able to detect the serine

180 ropeptide dynorphin, an endogenous ligand at kappa opioid receptors (KOR) that suppresses dopamine re

181 but not in dynorphin knock-out, mice lacking kappa opioid receptors (KOR-/-) or in wild-type mice pre

182 orphin, the endogenous ligand for the kappa (kappa) opioid receptor (KOR), is thought to be involved

183 ioid peptide dynorphin, we microinjected the kappa-opioid receptor (KOR) agonist U50,488 directly int

184 is an apparently selective and highly potent kappa-opioid receptor (KOR) agonist.

185 tional design of highly potent and selective kappa-opioid receptor (KOR) agonists (conorphins) with e

186 rphin function, because they are mimicked by kappa-opioid receptor (KOR) agonists and attenuated by K

187 kappa-Opioid receptor (KOR) agonists do not activate the

188 Kappa-opioid receptor (KOR) agonists have dysphoric prop

189 previously demonstrated that the spinal cord kappa-opioid receptor (KOR) and mu-opioid receptor (MOR)

190 peated swim stress caused activation of both kappa-opioid receptor (KOR) and p38 mitogen-activated pr

191 R and fluorescence spectroscopy in the human kappa-opioid receptor (KOR) and the human A2A adenosine

192 ed aversive behaviors that were blocked by a kappa-opioid receptor (KOR) antagonist and absent in mic

193 Administration of the kappa-opioid receptor (KOR) antagonist JDTic (30 mg/kg,

194 Similar modification of the kappa-opioid receptor (KOR) antagonist norBNI (1a) and i

195 Administration of a kappa-opioid receptor (KOR) antagonist reduced stress ef

196 Recent work indicates that kappa-opioid receptor (KOR) antagonists can block CRF ef

197 The kappa-opioid receptor (KOR) has been implicated in depre

198 The kappa-opioid receptor (KOR) has emerged as a promising t

199 We examined whether genetic deletion of the kappa-opioid receptor (KOR) in mice alters metabolic phy

200 Endogenous dynorphin signaling via the kappa-opioid receptor (KOR) in the nucleus accumbens (NA

201 kappa-opioid receptor (KOR) is detected pre- and postsyn

202 The kappa-opioid receptor (KOR) is the primary target for th

203 evidence to suggest that drug actions at the kappa-opioid receptor (KOR) may represent a means to con

204 Three kappa-opioid receptor (KOR) mRNA isoforms have been dete

205 wild-type mice, but not in mice lacking the kappa-opioid receptor (KOR) or lacking the G-protein rec

206 YN) A-like peptide expression and heightened kappa-opioid receptor (KOR) signaling in the central nuc

207 Previously it was demonstrated that kappa-opioid receptor (KOR) signaling in the striatum pl

208 rats, increased spinal dynorphin release and kappa-opioid receptor (KOR) signaling, as well as the em

209 Activation of the dynorphin/kappa-opioid receptor (KOR) system by repeated stress ex

210 dies have demonstrated an enhanced dynorphin/kappa-opioid receptor (KOR) system following repeated co

211 The dynorphin (DYN)/kappa-opioid receptor (KOR) system has been implicated i

212 The dynorphin/kappa-opioid receptor (KOR) system has been previously i

213 data have implicated the activated dynorphin/kappa-opioid receptor (KOR) system in relation to these

214 Whereas the kappa-opioid receptor (KOR) system is known to mediate s

215 esigned to test the hypotheses that: (1) the kappa-opioid receptor (KOR) system mediates phenotypes r

216 The dynorphin (DYN)/kappa-opioid receptor (KOR) system plays a conserved rol

217 The dynorphin (DYN)/kappa-opioid receptor (KOR) system undergoes neuroadapta

218 an increasing amount of attention since the kappa-opioid receptor (KOR) was identified as its princi

219 arrestin mediated desensitization of the rat kappa-opioid receptor (KOR) was previously shown using X

220 pha-subunits (Galpha16 or Galphai2) with the kappa-opioid receptor (KOR) were examined.

221 molecular determinants for activation of the kappa-opioid receptor (KOR) were studied using a combina

222 while reducing affinity and efficacy at the kappa-opioid receptor (KOR), and (3) improving in vivo e

223 phin A (Dyn A), an endogenous agonist of the kappa-opioid receptor (KOR), directly inhibits proopiome

224 The kappa-opioid receptor (KOR)-dynorphin system has been im

225 due to MOR activation, but had no effect on kappa-opioid receptor (KOR)-mediated inhibition.

226 idence that DOR can form heteromers with the kappa-opioid receptor (KOR).

227 (K(i) = 390 and 23 nM, respectively) for the kappa-opioid receptor (KOR).

228 cholecystokinin receptor A (CCKAR), and the kappa-opioid receptor (KOR).

229 We detected mu-opioid receptor (MOR-1) and kappa-opioid receptor (KOR-1) expression and immunoreact

230 rmacological approaches were used to examine kappa-opioid receptor (KOR-1) regulation of dopamine (DA

231 Kappa-opioid receptors (KOR) are believed to be involved

232 The kappa-opioid receptors (KOR) are involved in mood disord

233 D" chemogenetic tool based on the inhibitory kappa opioid receptor (KORD) that can be used in conjunc

234 a novel inhibitory DREADD in which a mutated kappa-opioid receptor (KORD) is activated by the pharmac

235 a novel inhibitory DREADD in which a mutated kappa-opioid receptor (KORD) is activated by the pharmac

236 h affinity for mu opioid receptor (MORs) and kappa opioid receptors (KORs) and some affinity at delta

237 Kappa opioid receptors (KORs) are highly enriched within

238 sent study was designed to determine whether kappa opioid receptors (KORs) are localized to cells of

239 kappa opioid receptors (KORs) belong to the G-protein-co

240 Kappa opioid receptors (KORs) have an important role in

241 Kappa opioid receptors (KORs) have been implicated in an

242 eptides including dynorphin, which activates kappa opioid receptors (KORs) in the central and periphe

243 Here we show that blocking kappa opioid receptors (KORs) prior to forced-swim stres

244 Dynorphin, an endogenous ligand at kappa opioid receptors (KORs), produces depressive-like

245 these calcium oscillations are regulated by kappa opioid receptors (KORs).

246 is mediated through downstream activation of kappa-opioid receptors (KORs) and that activation of the

247 kappa-Opioid receptors (KORs) and their endogenous ligan

248 The kappa-opioid receptors (KORs) are implicated in several

249 Brain kappa-opioid receptors (KORs) are implicated in states o

250 Kappa-opioid receptors (KORs) are important for motivati

251 norphins and causes subsequent activation of kappa-opioid receptors (KORs) in limbic brain regions.

252 mRNA expression for prodynorphin (PDYN) and kappa-opioid receptors (KORs) in mesocorticolimbic brain

253 Activation of kappa-opioid receptors (KORs) in monoamine circuits resu

254 peptide dynorphin, which acts at presynaptic kappa-opioid receptors (KORs) on dopaminergic afferents

255 norumthat selectively and potently activates kappa-opioid receptors (KORs).

256 However, the effects of kappa opioid receptor ligands are distinct in males and

257 r-mediated excitotoxic inflammation; and [5] kappa-opioid receptor ligands also modulate Type-I audit

258 the durations of antagonist action of novel kappa-opioid receptor ligands and examined their efficac

259 mediated through a common nor-BNI-sensitive (kappa-opioid receptor-like) pathway.

260 , and more specifically, enhances delta- and kappa-opioid-receptor-mediated hypoalgesia and attenuate

261 the concomitant activation of spinal mu- and kappa-opioid receptors (MOR and KOR, respectively).

262 t upon intact opioid receptor signaling with kappa opioid receptors more involved than mu and delta o

263 led to significantly decreased mu, delta and kappa opioid receptor mRNA expression as analyzed by qua

264 exposure alters the expression of mu- and/or kappa-opioid receptor mRNA or pro-opioimelanocortin (POM

265 CX3CL1/fractalkine receptor and mu, delta or kappa opioid receptors occurs in the periaqueductal grey

266 more selectively relative to mixed delta and kappa opioid receptors or singly expressed delta and kap

267 of the vmPFC, and intra-vmPFC stimulation of kappa-opioid receptors or blockade of 5-HT2A (5-hydroxyt

268 Brain kappa-opioid receptors (ORs) may be involved in several

269 micro and delta opioid receptor antagonist, kappa opioid receptor partial agonist that has recently

270 To characterize delta- and kappa-opioid receptor phenotypes, bivalent ligands (KDAN

271 s of alpha2A adrenergic and mu-, delta-, and kappa-opioid receptors reinstated hyperalgesia during re

272 himine, an antagonist for dynorphin-targeted kappa-opioid receptor, rescued memory in old WT mice.

273 atios of 103- and 132-fold versus the mu and kappa opioid receptors, respectively.

274 as established that stably expressed the rat kappa-opioid receptor (rKOR) with a FLAG epitope at the

275 th met-enkephalin (ME) or by mu-, delta-, or kappa-opioid receptor selective agonists, namely D-Ala2-

276 neither compound showed the high potency and kappa opioid receptor selectivity of JDTic.

277 ermined the impact of modulating both mu and kappa opioid receptor signaling using the mixed agonist/

278 such as morphine in that it mediates potent kappa opioid receptor signaling yet leads to less recept

279 kappa opioid receptors, unmasking inhibitory kappa opioid receptor signaling, and converting endogeno

280 Our findings establish a role of dynorphin kappa-opioid receptor signaling in fear extinction.

281 by both the ebb and flow of spinal dynorphin/kappa-opioid receptor signaling over the estrous cycle,

282 i.c.v.) of CGRP (1.5 microg) with the mu and kappa opioid receptor-specific antagonists naloxone (10

283 tor antagonist naloxone and by the selective kappa-opioid receptor subtype antagonist nor-BNI (nor-Bi

284 uperfamily that also includes mu, delta, and kappa opioid receptor subtypes (MOR, DOR, and KOR, respe

285 our maps corresponding to the delta, mu, and kappa opioid receptor subtypes reflected the characteris

286 phore formation for wild-type mu, delta, and kappa opioid receptors suggest that these conserved resi

287 ction for the dysphoric effects of dynorphin-kappa-opioid receptor system activation during stress-ev

288 the stress circuits, including the dynorphin/kappa-opioid receptor system, modulates the rewarding ef

289 dynorphin, which in turn acts on presynaptic kappa-opioid receptors to inhibit glutamate release.

290 Using mouse and human recombinant kappa opioid receptors transfected into a host cell, two

291 sing a G-protein coupled receptor, the human kappa opioid receptor type 1 (hKOR1).

292 ling by endogenous GM1-sensitized excitatory kappa opioid receptors, unmasking inhibitory kappa opioi

293 JNK-mediated receptor inactivation of the kappa-opioid receptor was evident in both agonist-stimul

294 electivity of KDN21 for phenotypic delta and kappa opioid receptors, we investigated the effect of KD

295 prises three members, the micro-, delta- and kappa-opioid receptors, which respond to classical opioi

296 pionamide (6d) with a K(e) of 0.27 nM at the kappa opioid receptor with 154- and 46-fold selectivity

297 voked bursts were prolonged by antagonism of kappa-opioid receptors with nor-binaltorphimine and by d

298 We first show that peripheral blockade of kappa-opioid receptors with the antagonist norbinaltorph

299 Thus, kappa-opioid receptors within the NAc shell mediate aver

300 Blockade of kappa-opioid receptors within the ventral pallidum or mu