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1 sed assay in a cellular system containing mu-opioid receptor.
2 d probes for exploring the role of the kappa-opioid receptor.
3 ivity, and functional activity toward the mu-opioid receptor.
4 that functions as an antagonist of the kappa opioid receptor.
5 argeting truncated splice variants of the mu-opioid receptor.
6 current opioid analgesics that target the mu opioid receptor.
7 equirements of the binding pocket across the opioid receptors.
8 lkaloids at the human mu-, kappa-, and delta-opioid receptors.
9 in regions that contain a high expression of opioid receptors.
10 genetic data suggest the importance of delta-opioid receptors.
11 petitive antagonists at the kappa- and delta-opioid receptors.
12 elying on its partial agonist activity at mu opioid receptors.
13 , structures expressing high levels of kappa opioid receptors.
14 ic-associated subcompartments enriched in mu opioid receptors.
15 which can inhibit dopamine release via kappa-opioid receptors.
16 y for mu (MOR), delta (DOR), and kappa (KOR) opioid receptors across the series, with the diimidazodi
17 ng respiratory pattern, the mechanisms of mu opioid receptor activation in this nucleus were investig
19 s in humans demonstrating that pharmacologic opioid receptor activation induces some of the clinical
20 echanisms that modulate calcium channels via opioid receptor activation is fundamental to our underst
21 hydroxylase (TH) promoter, we found that mu opioid receptor activation led to a decrease in inhibito
23 igand recognition features important for pan opioid receptor activity, using chemical modifications o
24 mily, including rhodopsin (visual receptor), opioid receptors, adrenergic receptors, adenosine recept
25 single-digit nanomolar to subnanomolar kappa-opioid receptor affinity, full kappa agonistic activity
27 with a mechanism of action that includes mu opioid receptor agonism/delta opioid receptor antagonism
30 ent with mixed opioid effects (mu- and kappa-opioid receptor agonist and delta-opioid receptor antago
31 vation through both pathways, whereas the mu opioid receptor agonist DAMGO decreased D2-receptor acti
32 ining addicted pregnant women on long-acting opioid receptor agonist is the most common strategy to m
34 sion of phasic dopamine release by the kappa-opioid receptor agonist, salvinorin A, supporting a sele
37 ous natural compound known to function as an opioid-receptor agonist, and is undergoing clinical tria
42 gynine, are partial agonists of the human mu-opioid receptor and competitive antagonists at the kappa
43 itro, the hybrids behaved as agonists at the opioid receptors and antagonists at the nociceptin recep
44 by the activation of mu-, delta-, and kappa-opioid receptors and by adrenergic alpha2A receptors in
45 ade tracer from rVLM were co-labeled with mu-opioid receptors and juxtaposed to endorphinergic fibers
46 oncomitant opioid release could downregulate opioid receptors and promote the development of obesity.
48 lation of the vPAG/DR dopamine neurons by mu opioid receptors and to (2) dissect the anatomy and neur
49 rescued by the expression of the human kappa opioid receptor, and injection of human opioid receptor
50 asal forebrain cholinergic neurons via kappa-opioid receptors, and decreases afferent excitatory syna
51 inhibition, in pain perception pathways via opioid receptors, and is also involved in alcoholism.
52 f which cause toxicity via interactions with opioid receptors, and result in a multifunctional bioche
53 hormones (estrogen and progesterone), delta-opioid receptors, and T cells of the adaptive immune sys
54 h G protein-coupled receptors, in particular opioid receptors, and their downstream effectors PKA/CRE
56 , (+)-naloxone, the non-opioid isomer of the opioid receptor antagonist (-)-naloxone, in infection-as
57 show further that a selective and potent mu-opioid receptor antagonist (GSK1521498) reduced both alc
58 latory effects of OPRM1 genetic variation on opioid receptor antagonist attenuation of alcohol- and f
59 ABAA agonist muscimol into the IC and the mu-opioid receptor antagonist CTAP into the contralateral N
62 stemic or hypothalamic administration of the opioid receptor antagonist naloxone blocks acute CB1R-in
63 VT administration of OrxA+/-DynA+/-the kappa-opioid receptor antagonist nor-binaltorphimine (NorBNI)
65 his SNP on alcohol-related behaviors, and on opioid receptor antagonist treatments, have been inconsi
66 and kappa-opioid receptor agonist and delta-opioid receptor antagonist), in patients with IBS with d
67 al pretreatment with naloxone, non-selective opioid receptor antagonist, did not affect the effect of
68 ety of naldemedine, a peripherally acting mu-opioid receptor antagonist, for the treatment of opioid-
70 onthly injectable formulation of the full mu-opioid receptor antagonist, is effective for the prevent
73 trexone and GSK1521498, a novel selective mu-opioid receptor antagonist, on both voluntary alcohol-in
74 en A118G variation and the effects of two mu-opioid receptor antagonists in a clinical lab setting.
75 l-4-(3-hydroxyphenyl)piperidine (1) class of opioid receptor antagonists, procedures were developed f
76 lpiperazines 4 and 5 were reported to be pan opioid receptor antagonists, while 6 was a MOR agonist.
79 phai-G-protein-coupled receptor inactivation.Opioid receptors are important modulators of nociceptive
80 imaging in HEK293 cells revealed that delta opioid receptors are in pre-engaged complexes with arres
81 both expression levels and the proportion of opioid receptors are strongly lateralized in the spinal
82 elop a new Gi-coupled DREADD using the kappa-opioid receptor as a template (KORD) that is activated b
83 n of spinal opioid receptors, putatively mu1-opioid receptors, as indicated by its sensitivity to spi
84 3 is in pre-engaged complexes with the delta opioid receptor at the cell membrane and low-internalizi
86 g associations between baseline IL-18 and mu-opioid receptor availability in major depressive disorde
87 , showed an overall reduction of baseline mu-opioid receptor availability in regions implicated in pa
88 were negatively correlated with baseline mu-opioid receptor availability in the aINS and subgenual a
89 G, BED patients show widespread losses of mu-opioid receptor availability together with presynaptic d
90 restrict expression of the inhibitory kappa opioid-receptor based DREADD (KORD) in vSub-->NAc shell
93 in D2/D3R BPND were also correlated with mu-opioid receptor BPND and pain-induced endogenous opioid
94 gonists in [(35)S]GTPgammaS assays at the mu opioid receptor but failed to recruit beta-arrestin-2, w
95 cell lines affected endocytosis of the delta-opioid receptor, but not the beta2-adrenergic receptor,
96 ts MCPO/SI cholinergic neurons through kappa-opioid receptors by (1) activation of a G protein-couple
98 peroxiredoxin 6 (PRDX6) is recruited to the opioid receptor complex by c-Jun N-terminal kinase (JNK)
100 is a structurally distinct PAM for the delta-opioid receptor (delta-OR) that has been reported to exh
106 found increased G protein coupling for delta opioid receptor (DOR) and mu opioid, but not other Gi/o
107 receptors (KORs) and some affinity at delta opioid receptor (DOR) and opioid receptor-like 1 (ORL-1)
108 es of mu-opioid receptor (MOR) agonist/delta-opioid receptor (DOR) antagonist ligands increases DOR a
111 inhibit glutamate release through the delta-opioid receptor (DOR), an effect potentiated by a DOR-po
113 depends heavily on opioids acting through mu opioid receptors encoded by the Oprm1 gene, which underg
114 conserved allosteric binding site across the opioid receptor family that can accommodate structurally
115 The NOP receptor, the fourth member of the opioid receptor family, is involved in pain, drug abuse,
117 ucleotide polymorphism (SNP) in the human mu-opioid receptor gene (OPRM1 A118G) has been widely studi
118 whether the sole targeted deletion of the mu opioid receptor gene (Oprm1) alters the brain connectome
119 ymorphism (rs1799971, Asn40Asp) of the micro-opioid receptor gene (OPRM1) is associated with the risk
121 Extensive 3' alternative splicing of the mu opioid receptor gene OPRM1 creates multiple C-terminal s
122 otide polymorphism (SNP rs1799971) in the mu-opioid receptor gene, OPRM1, has been much studied in re
123 ed the colocalization of mu-opioid and kappa-opioid receptor genes and OT genes at the OT-releasing s
124 rs of G protein-coupled receptors, including opioid receptors, have been proposed as possible therape
126 by the expression of npr-17 or a human kappa opioid receptor in the two ASI sensory neurons, with ASI
127 First, Dbx1 preBotC neurons express kappa-opioid receptors in addition to mu-opioid receptors that
131 ing of the neuropeptide beta-endorphin to mu-opioid receptors in the central nervous system (CNS) is
133 naloxone, suggesting the participation of mu-opioid receptors in the reinforcing properties of sufent
136 tion of NF1 in striatal neurons prevents the opioid-receptor-induced activation of Ras and eliminates
137 or sufentanil when given the preferential mu-opioid receptor inverse agonist naloxone, suggesting the
138 systemic side effects, targeting peripheral opioid receptors is an attractive alternative treatment
139 rthermore, we show that the activation of mu-opioid receptors is not due to the release of endogenous
141 or insula with a downregulation of the kappa opioid receptor (Kappa), as well as decreased DNA methyl
142 effective PAM at the mu-OR and at the kappa-opioid receptor (kappa-OR), but it is ineffective at the
147 promoted phosphorylation of the mouse kappa opioid receptor (KOPR) at residues S356, T357, T363, and
148 TEMENT Emerging evidence suggests that kappa opioid receptor (KOR) activation can selectively modulat
149 design of highly potent and selective kappa-opioid receptor (KOR) agonists (conorphins) with excepti
154 peptide (dynorphin) bound to the human kappa opioid receptor (KOR) has been determined by liquid-stat
157 Endogenous dynorphin signaling via the kappa-opioid receptor (KOR) in the nucleus accumbens (NAcc) po
158 like peptide expression and heightened kappa-opioid receptor (KOR) signaling in the central nucleus o
159 Previously it was demonstrated that kappa-opioid receptor (KOR) signaling in the striatum plays a
160 increased spinal dynorphin release and kappa-opioid receptor (KOR) signaling, as well as the emergenc
165 ioid receptors with preference for the kappa opioid receptor (KOR), and its structure-activity relati
166 (5),Dap(8))]dynorphin A(1-11)NH2) is a kappa opioid receptor (KOR)-selective antagonist in vitro, is
167 ide dynorphin, an endogenous ligand at kappa opioid receptors (KOR) that suppresses dopamine release
168 l inhibitory DREADD in which a mutated kappa-opioid receptor (KORD) is activated by the pharmacologic
169 mogenetic tool based on the inhibitory kappa opioid receptor (KORD) that can be used in conjunction w
170 nity for mu opioid receptor (MORs) and kappa opioid receptors (KORs) and some affinity at delta opioi
171 iated through downstream activation of kappa-opioid receptors (KORs) and that activation of these rec
176 e dynorphin, which acts at presynaptic kappa-opioid receptors (KORs) on dopaminergic afferents and ca
177 se in arachidonic acid levels through the mu-opioid receptors leads to the sole activation of microgl
178 were introduced into the endogenous peptide opioid receptor ligand Leu-enkephalin as a model compoun
180 appa opioid receptor, and injection of human opioid receptor ligands mimics exogenous opiates, highli
181 represent the first example of mirror image opioid receptor ligands with both optical antipodes havi
183 s and side effects; endogenous and exogenous opioid receptor ligands; and conventional and novel opio
184 esis of the gem-difluoro group present in an opioid receptor-like 1 (ORL-1) antagonist that is curren
188 dministration of 14 produced dose-dependent, opioid-receptor mediated antinociception in the mouse, a
189 Therefore, this remission represents an opioid receptor-mediated suppression of a sustained hype
191 ls coexpressing TRPC4 and Gi/o-coupled micro opioid receptor, micro agonist elicited currents biphasi
196 member mitragynine, are an unusual class of opioid receptor modulators with distinct pharmacological
197 e tyrosine kinase, c-Src, participates in mu opioid receptor (MOP) mediated inhibition in sensory neu
199 residues in the C-terminal tail of the micro-opioid receptor (MOPr) is thought to be a key step in de
203 ids analgesics is mainly attributed to micro-opioid receptor (MOR) activation leading to G protein si
204 orphinan skeleton plays a key role in the mu-opioid receptor (MOR) activity in vitro and in vivo.
205 kurkinorin (5), is a potent and selective mu-opioid receptor (MOR) agonist (EC50 = 1.2 nM, >8000 mu/k
207 ed intradermal injection of the selective mu-opioid receptor (MOR) agonist DAMGO induced mechanical h
208 ahydroquinoline (THQ) core of a series of mu-opioid receptor (MOR) agonist/delta-opioid receptor (DOR
210 there was no difference in the ability of mu-opioid receptor (MOR) agonists to inhibit sIPSCs in POMC
213 on specific to PDAC is identified between mu opioid receptor (MOR) and somatostatin receptor 2 (SSTR2
214 ized in substance dependence, with higher mu-opioid receptor (MOR) availability reported in alcohol,
215 t induced by inhibition of the endogenous mu-opioid receptor (MOR) by naltrexone, MOR knockout, and G
217 report convergent evidence for decreased mu-opioid receptor (MOR) function in the female rat LC.
219 the function of class A GPCRs such as the mu-opioid receptor (MOR) is still unclear, insight as to ho
220 IFICANCE STATEMENT Desensitization of the mu-opioid receptor (MOR) is thought to underlie the develop
222 in 2 [EM2; the highly specific endogenous mu-opioid receptor (MOR) ligand] induces antinociception th
226 eptor subtypes, we reveal that endogenous mu-opioid receptor (MOR) signaling strongly drives sodium a
228 ivate a potassium conductance through the mu-opioid receptor (MOR), suggesting for the first time tha
235 lasticity by regulating activation of the mu-opioid receptor (MOR).D1LR stimulation with agonist SKF
237 at dopamine D1-like receptors (D1LRs) and mu-opioid receptors (MOR) in the spinal dorsal horn constit
238 f acute physical exercise on the cerebral mu-opioid receptors (MOR) of 22 healthy recreationally acti
239 gands with agonist bioactivities at mu/delta opioid receptors (MOR/DOR) and antagonist bioactivity at
240 scribe structural features of a series of mu-opioid-receptor (MOR)-selective agonists that preferenti
242 In addition to binding to the neuronal mu-opioid receptor, morphine binds to the innate immune rec
243 hine (BPN), a drug with high affinity for mu opioid receptor (MORs) and kappa opioid receptors (KORs)
245 e provide evidence that the activation of mu-opioid receptors (MORs) by the specific agonist DAMGO ([
249 crued to suggest that excessive intra-PFC mu-opioid receptor (mu-OR) signaling alters the PFC respons
251 depression-are thought to be mediated by mu-opioid-receptor (muOR) signalling through the beta-arres
252 esics, such as morphine, which target the mu opioid receptor (muR), have been the mainstay of pain ma
253 ecades since the discovery of the nociceptin opioid receptor (NOP) and its ligand, nociceptin/orphani
254 ased signaling at the nociceptin/orphanin FQ opioid receptor (NOPR), the most recently identified mem
255 nversely, pharmacological activation of rACC opioid receptors of injured, but not pain-free, animals
257 esults from iLTD through activation of delta-opioid receptors on parvalbumin-expressing interneurons.
258 ing mice with genetic deletion of individual opioid receptors or after pharmacological blockade of re
259 tial evidence in support of the formation of opioid receptor (OR) di-/oligomers suggests previously u
261 and delta opioid receptor antagonist, kappa opioid receptor partial agonist that has recently been a
262 nderstanding the pharmacology of this fourth opioid receptor/peptide system, aided by genetic and pha
263 his depression required activation of spinal opioid receptors, putatively mu1-opioid receptors, as in
264 ular mechanisms of protection, such as delta-opioid receptor regulation and mitophagy, reinforce the
265 lpha2A adrenergic and mu-, delta-, and kappa-opioid receptors reinstated hyperalgesia during remissio
266 Antagonists of alpha2A-adrenergic and delta-opioid receptors reinstated hyperalgesia in WT mice and
270 ed to attenuate the central projection of mu-opioid receptor-sensitive locomotor muscle afferents dur
271 h the ebb and flow of spinal dynorphin/kappa-opioid receptor signaling over the estrous cycle, as wel
272 d the impact of modulating both mu and kappa opioid receptor signaling using the mixed agonist/antago
273 ereas a role for kappa (KOR) and delta (DOR) opioid receptor signaling was not detected, at least in
274 ine with previous studies suggesting that mu-opioid receptor signalling has been elaborated beyond it
277 sal root ganglion neurons, independent of mu opioid receptor stimulation or G protein activation.
278 es by dose dependently acting on distinct mu-opioid receptor subtypes located at different levels of
279 petite, the endogenous influence of specific opioid receptor subtypes within distinct brain regions r
280 opioid ligands binding to the three classic opioid receptor subtypes, mu, kappa and delta, have high
281 ing selective pharmacological antagonists of opioid receptor subtypes, we reveal that endogenous mu-o
284 yna alkaloids adopt a binding pose at the mu-opioid receptor that is distinct from that of classical
285 ess kappa-opioid receptors in addition to mu-opioid receptors that heretofore have been associated wi
286 l (50 mM) to striatal slices activates delta opioid receptors that reside on FSI axon terminals and n
287 and delta, have high affinity at the fourth opioid receptor, the nociceptin/orphanin FQ receptor (NO
289 s the structure, function, and plasticity of opioid receptors; the central and peripheral sites of an
290 o acids do not bind to either cannabinoid or opioid receptors, thus reducing adverse actions and maki
291 venous PG-M exclusively activated peripheral opioid receptors to produce analgesia in inflamed rat pa
293 Using mouse and human recombinant kappa opioid receptors transfected into a host cell, two selec
294 to a similar region on all three traditional opioid receptor types (micro-OR, delta-OR, and kappa-OR)
295 increased enkephalin tone on presynaptic mu opioid receptors was responsible for occluding the LTD.
297 Therefore, these studies examined which opioid receptors were involved in BPN's effects on anima
298 nine are G-protein-biased agonists of the mu-opioid receptor, which do not recruit beta-arrestin foll
299 is is consistent with nalmefene's actions on opioid receptors, which modulate the mesolimbic dopamine
300 in A (Dyn A) is an endogenous ligand for the opioid receptors with preference for the kappa opioid re
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