Receptor agonist damgo. Medical search. Frequent questions

However, a role for opioid receptor heterodimerization in neurons has yet to be identified. (aspetjournals.org)
We examined μ-receptor coupling to VDCCs in dorsal root ganglion neurons of δ(+/+), δ(+/-), and δ(-/-) mice. (aspetjournals.org)
Neurons deficient in δ receptors exhibited reduced inhibition of VDCCs by morphine and [ d -Ala 2 ,Phe 4 ,Gly 5 -ol]-enkephalin (DAMGO). (aspetjournals.org)
Flow cytometry revealed a reduction in μ-receptor surface expression in δ(-/-) neurons without altered DAMGO-induced internalization. (aspetjournals.org)
d -Phe-Cys-Tyr- d -Trp-Arg-Thr-Pen-Thr-NH 2 -sensitive μ-receptor-coupling efficacy was fully restored to δ(+/+) levels in δ(-/-) neurons by expression of recombinant δ receptors. (aspetjournals.org)
However, the dimerization-deficient δ-15 construct expressed in δ(-/-) neurons failed to fully restore the inhibitory coupling of μ receptors compared with that seen in δ(+/+) neurons, suggesting that, although not essential for μ-receptor function, μ-δ receptor dimerization contributes to full μ-agonist efficacy. (aspetjournals.org)
Because DAMGO exhibited a similar potency in δ(+/+) and δ(-/-) neurons and caused similar levels of internalization, the role for heterodimerization is probably at the level of receptor biosynthesis. (aspetjournals.org)
We investigated the mechanisms underlying MOR desensitization, in adult mammalian neurons, caused by morphine (a partial agonist in this system) and DAMGO (a high-efficacy agonist). (bath.ac.uk)
Specific isoforms of PKC were inhibited by using inhibitors of the receptors for activated C-kinase (RACK), and in vivo viral-mediated gene-transfer was used to transfect neurons with dominant negative mutants (DNMs) of specific G-protein-coupled receptor kinases (GRKs). (bath.ac.uk)
CONCLUSIONS AND IMPLICATIONS: In mature mammalian neurons, different MOR agonists can induce MOR desensitization by different mechanisms, morphine by a PKCalpha-mediated, heterologous mechanism and DAMGO by a GRK-mediated, homologous mechanism. (bath.ac.uk)
To establish whether DAMGO alter the effect of CXCL12 on neuronal survival, the ability of CXCL12 to protect neurons from N-methyl-d-aspartate (NMDA)-induced death is examined in the presence and absence of DAMGO. (molcore.com)
In the current study, the authors investigated the effects of remifentanil hydrochloride, with and without its vehicle, glycine, on the activation of NMDA receptors and the modulation of NMDA-induced current on neurons inside the lamina II from the dorsal horn of rat spinal cord. (silverchair.com)
However, the mechanism of the neurotransmitter norepinephrine (NE) released by sympathetic nerve fiber endings on the excitability of DRG neurons is still controversial, and the adrenergic receptor subtypes involved in this biological process are also controversial. (bvsalud.org)
2) To determine which adrenergic receptors are involved in the excitability of DRG neurons by NE released by sprouting sympathetic fibers. (bvsalud.org)
discharge of endogenous endomorphins that activate opioid receptors in GABAnergic neurons to suppress the discharge of GABA. (gasyblog.com)
Immunolabeling indicates that GABA neurons in the rostromedial tegmental nucleus (RMTg), also known as the tail of the ventral tegmental area, send a dense projection to midbrain dopamine neurons stain for μ-opioid receptors. (elsevierpure.com)
The rhythmic spontaneous firing rate of RMTg neurons was decreased and the membrane potential was hyperpolarized in response to application of μ-opioid agonist DAMGO. (elsevierpure.com)
Agonists that act at κ-and Δ -opioid receptors (U69593 and DPDPE) failed to hyperpolarize RMTg neurons. (elsevierpure.com)
In addition, electrical and channelrhodopsin-2 stimulation within the RMTg evoked GABA-A IPSCs in dopamine neurons that were inhibited by μ -opioid agonists DAMGO, but not κ - and Δ -opioid agonists. (elsevierpure.com)
Thus, this study demonstrates functional connection from the RMTg to the VTA/SN mediated by a dense, opioid-sensitive GABA innervation, and that the RMTg is a key structure in the μ -opioid receptor-dependent regulation of dopamine neurons. (elsevierpure.com)
Mu-opioid receptor (MOR) agonists potently inhibited MThal inputs without affecting ACC inputs to individual striatal medium spiny neurons (MSNs). (elifesciences.org)
We further determined that the increased sensitivity of D40 iN cells to DAMGO was caused by a more robust inhibition of excitability and synaptic release by DAMGO in D40 MOR expressing neurons. (rutgers.edu)
The μ-agonist DAMGO reduced GABAergic evoked inhibitory postsynaptic currents (IPSCs) in retro-labelled, RVM-projecting neurons to a greater extent than in unlabelled neurons. (nih.gov)
DAMGO and U69593 both produced a reduction in the rate, but not amplitude of spontaneous miniature IPSCs and asynchronous evoked IPSCs in retro-labelled neurons. (nih.gov)
DAMGO and U69593 also suppressed glutamatergic EPSCs in retro-labelled and unlabelled neurons. (nih.gov)
The DAMGO inhibition of evoked EPSCs, however, was less than that for evoked IPSCs in retro-labelled, but not unlabelled neurons. (nih.gov)
In current clamp, DAMGO produced a depolarizing increase in evoked postsynaptic potentials in retro-labelled neurons, but directly inhibited unlabelled neurons. (nih.gov)

It was synthesized as a biologically stable analog of δ-opioid receptor-preferring endogenous opioids, leu- and met-enkephalin. (wikipedia.org)
Opioids, extensively used as analgesics, markedly depress ventilation, particularly the ventilatory responsiveness to hypercapnia in humans and animals predominantly via acting on mu receptors. (silverchair.com)
14 Opioids inhibit respiration mainly via stimulating central μ receptors, 12,15-20 although some early studies indicate involvement of both μ and Δ receptors. (silverchair.com)
The rigid structural and stereochemical requirements essential for the analgesic actions of morphine and related opioids led to the theory that they produce their effects by interacting with a specific receptor. (opioids.wiki)
5. Block of carbachol activation of muscarinic receptors with atropine (10 μM) abolished the elevation of [Ca 2+ ](i) by the opioids. (edu.au)
The nicotinic receptor antagonist, mecamylamine (10 μM), did not affect the elevations of [Ca 2+ ](i) caused by opioids in the presence of carbachol. (edu.au)
Thus, in SH-SY5Y cells, opioids can mobilize Ca 2+ from intracellular stores but they require ongoing muscarinic receptor activation. (edu.au)

DAMGO and 6beta-glycine substituted 14-O-methyloxymorphone but not morphine show peripheral, preemptive antinociception after systemic administration in a mouse visceral pain model and high intrinsic efficacy in the isolated rat vas deferens. (springer.com)
Morphine-induced flexor responses were markedly inhibited by naloxone and D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr amide (CTOP) both MOP-R antagonists and by intrathecal injection of antisense oligodeoxynucleotide (AS-ODN) for MOP-R which is expected to reduce the receptor expression in sensory nerve endings. (illinois.edu)
Prior incubation with capsaicin, a depletor of SP from polymodal C fibers and [(+)-(2S,3S)-(2-methoxybenzylamino)-2-phenylpiperidine] (CP-99994), a tachykinin 1 receptor antagonist, also blocked the morphine-induced flexor responses. (illinois.edu)
xestospongin C, a membrane-permeable inositol trisphosphate (InsP 3 ) receptor antagonist inhibited the morphine-flexor responses. (illinois.edu)
However, thapsigargin, a depletor of intracellular Ca 2+ concentration and diphenhydramine, a histamine (His) H1 receptor antagonist, were unable to block the morphine-induced flexor responses. (illinois.edu)
1 The concept that there is more than one type of opioid receptor arose to explain the dual actions of the synthetic opioid nalorphine, which antagonises the analgesic effect of morphine in man but also acts as an analgesic in its own right. (opioids.wiki)
Martin (1967) concluded that the analgesic action of nalorphine is mediated by a receptor, later called the k -opioid receptor, that is different from the morphine receptor. (opioids.wiki)
2 Evidence for multiple receptors, m , k and s , came from the demonstration of different profiles of pharmacological activity in the chronic spinal dog with the prototype agonists morphine, ketazocine and N-allylnormetazocine (SKF 10047). (opioids.wiki)
10 Furthermore, in the MOR-1 knockout mouse, morphine does not induce antinociception demonstrating that at least in this species morphine's analgesia is not mediated through d - or k -receptors. (opioids.wiki)
Intravenous (i.v.) administration of μ opioid receptor (MOR) agonists (fentanyl, alfentanil, remifentanil, and morphine) evoked scratching in a dose- and time-dependent manner. (ewha.ac.kr)
Antagonist studies revealed that i.v. administration of an opioid receptor antagonist (naltrexone, 0.0032-0.1 mg/kg) dose dependently attenuated scratching induced by i.v. fentanyl (0.018 mg/kg) or morphine (1 mg/kg). (ewha.ac.kr)

Handa BK, Land AC, Lord JA, Morgan BA, Rance MJ, Smith CF. Analogues of beta-LPH61-64 possessing selective agonist activity at mu-opiate receptors. (springer.com)
DAMGO acetate is a μ-opioid receptor ( μ-OPR ) selective agonist with a K d of 3.46 nM for native μ-OPR [1] . (molcore.com)
DAMGO, a μ-opioid receptor selective agonist, distinguishes between μ- and δ-opioid receptors around their first extracellular loops. (molcore.com)
DAMGO is a selective μ-opioid peptide. (molcore.com)
3 The existence of the d -receptor was subsequently proposed to explain the profile of activity in vitro of the enkephalins (the first endogenous opioid peptides), and on the basis of the relative potency of the non-selective opioid antagonist naloxone to reverse endogenous opioid peptide inhibition of the nerve-evoked contractions of the mouse vas deferens. (opioids.wiki)
At the extreme, functionally selective ligands may be both agonists and antagonists at different functions mediated by the same receptor. (aspetjournals.org)
Binaltorphimine ( BNI ) is a selective antagonist of the κ-opioid receptor (KOR). (wikipedia.org)
More precisely, supraspinal Nocistatin by itself had no significative effect on nociception and opioid analgesia in the tail flick test but, at the dose of 0.5ng/rat, it reversed the nociceptive effect of Nociceptin and also the antagonistic effect of Nociceptin against analgesia caused by the selective opioid agonists: DAMGO, DPDPE, Deltorphin II and U50 488H. (unict.it)

mu-Opioid agonists have no effect on calcium currents (I(Ca)) in neurohypophysial terminals when recorded using the classic whole-cell patch-clamp configuration. (umassmed.edu)

An absence of δ receptors reduced neither the density of VDCCs nor their inhibition by either the GABA B receptor agonist baclofen or intracellular guanosine 5′- O -(3-thio)triphosphate. (aspetjournals.org)
Furthermore, previous data suggest that the intracellular mechanisms underlying desensitization may be agonist-specific. (bath.ac.uk)
9 As would be predicted from their known abilities to couple through pertussis toxin-sensitive G-proteins, all of the cloned opioid receptors possess the same general structure of an extracellular N-terminal region, seven transmembrane domains and intracellular C-terminal tail structure. (opioids.wiki)
1. In this study we have investigated δ and μ opioid receptor-mediated elevation of intracellular Ca 2+ concentration ([Ca 2+ ](i)) in the human neuroblastoma cell line, SH-SY5Y. (edu.au)
Our results show a rise in basal intracellular calcium ([Ca(2+)]i) in response to application of [D-Ala(2)-N-Me-Phe(4),Gly5-ol]-Enkephalin (DAMGO), a MOR agonist, that is blocked by D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP), a MOR antagonist. (umassmed.edu)
G protein-coupled receptors (GPCRs) are the largest family of plasma membrane receptors that orchestrate intracellular signaling in response to diverse extracellular stimuli [ 1 , 2 ]. (biomedcentral.com)

However, mu-opioid receptor (MOR)-mediated inhibition of I(Ca) is reliably demonstrated using the perforated-patch configuration. (umassmed.edu)
Buffering DAMGO-induced changes in [Ca(2+)]i with BAPTA-AM completely blocked the inhibition of both I(Ca) and high-K(+)-induced rises in [Ca(2+)]i due to MOR activation, but had no effect on kappa-opioid receptor (KOR)-mediated inhibition. (umassmed.edu)
Given the presence of ryanodine-sensitive stores in isolated terminals, we tested 8-bromo-cyclic adenosine diphosphate ribose (8Br-cADPr), a competitive inhibitor of cyclic ADP-ribose (cADPr) signaling that partially relieves DAMGO inhibition of I(Ca) and completely relieves MOR-mediated inhibition of high-K(+)-induced and DAMGO-induced rises in [Ca(2+)]i. (umassmed.edu)

Neither the δ-opioid agonist, DPDPE ([D-Pen 2,5 ]-enkephalin) nor the μ-opioid agonist, DAMGO (Tyr-D-Ala-Gly-N-Me-Phe-Gly-ol enkephalin) elevated [Ca 2+ ](i) when applied alone. (edu.au)
However, when either DPDPE or DAMGO was applied in the presence of the cholinoceptor agonist, carbachol (100 nM-1 mM) they evoked an elevation of [Ca 2+ ](i) above that caused by carbachol alone. (edu.au)
4. The δ-receptor antagonist, naltrindole (30 nM), blocked the elevations of [Ca 2+ ](i) by DPDPE (100 nM) without affecting those caused by DAMGO while the μ-receptor antagonist, CTAP (D-Phe-Cys-Tyr-D-Trp-Arg-Pen-Thr-NH 2 ) (100 nM-1 μM) blocked the elevations of [Ca 2+ ](i) caused by DAMGO (1 μM) without affecting those caused by DPDPE. (edu.au)
The elevations of [Ca 2+ ](i) by DPDPE and DAMGO were abolished by pretreatment of the cells with pertussis toxin (200 ng ml -1 , 16 h). (edu.au)
Both DPDPE and DAMGO continued to elevate [Ca 2+ ](i) when applied in nominally Ca 2+ -free external buffer or when applied in a buffer containing a cocktail of Ca 2+ entry inhibitors. (edu.au)

The splice variants exhibit differences in their rate of onset and recovery from agonist-induced internalization but their pharmacology does not appear to differ in ligand binding assays. (opioids.wiki)

Moreover, our findings propose a therapeutic potential in combined CXCR4 and LPA 1 inhibitors for cancer and inflammatory diseases associated with these receptors, simultaneously raising concerns about the use of LPA 1 antagonists alone for such conditions. (biomedcentral.com)

Nevertheless, intra-RVM infusion of either DAMGO, a opioid receptor agonist, or "type":"entrez-nucleotide","attrs":"text message":"U69593″,"term_id":"4205069″,"term_text message":"U69593″U69593, a opioid receptor agonist, elevated paw drawback latency (PWL) within an inflammatory discomfort rat model (Schepers et al. (gasyblog.com)
The κ-opioid agonist U69593 reduced evoked IPSCs to a similar extent in both neuronal groups, while the δ-opioid agonist deltorphin-II was without effect. (nih.gov)

Since beta-endorphins can bind both mu opioid and kappa-opioid receptors we investigated the effect of a mu specific receptor agonist, D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin (DAMGO) and a mu specific antagonist, D-Phe-Cys-Trp-Arg-Thr-Pen-Thr-NH2 (CTAP) on cardiovascular responses in conscious control and obese rats. (nih.gov)
The mu agonist, DAMGO, increased blood pressure (BP) in control rats. (nih.gov)
DAMGO also increased BP in obese rats but only at high concentrations. (nih.gov)
The expression of mu opioid receptors was increased in obese rats. (nih.gov)
Supraspinal opioid receptor participation in EA anti-hyperalgesia in swollen rats is not 1226056-71-8 manufacture examined. (gasyblog.com)

DAMGO ([D-Ala2, N-MePhe4, Gly-ol]-enkephalin) is a synthetic opioid peptide with high μ-opioid receptor specificity. (wikipedia.org)
We found that encapsulation of the peptide DAMGO in fast-releasing polyethylene glycol (PEG)ylated liposomes, either with or without the specific brain targeting ligand glutathione (GSH), doubled the uptake of DAMGO into the rat brain. (springer.com)
Lindqvist A, Rip J, Gaillard PJ, Bjorkman S, Hammarlund-Udenaes M. Enhanced brain delivery of the opioid peptide DAMGO in glutathione pegylated liposomes: a microdialysis study. (springer.com)
However, non-formylated peptide ligands have also been found for this receptor class. (lookformedical.com)
Nocistatin does not bind to Nociceptin/Orphanin FQ peptide (NOP) receptor but it antagonizes the allodynic and hyperalgesic effect of intrathecal (i.t. (unict.it)

2004). On the other hand, vertebral endomorphin-1, an endogenous receptor agonist, mediates 2 1226056-71-8 manufacture however, not 100 Hz EA analgesia in uninjured rat versions (Han et al. (gasyblog.com)

Finally, we concluded that NE from sympathetic fiber endings is involved in the regulation of pain signaling by acting on α2A-adrenergic receptors in DRG. (bvsalud.org)
Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors. (lookformedical.com)
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). (lookformedical.com)
The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. (lookformedical.com)
A ubiquitously expressed G-protein-coupled receptor kinase subtype that has specificity for the agonist-occupied form of BETA-ADRENERGIC RECEPTORS and a variety of other G-PROTEIN-COUPLED RECEPTORS. (lookformedical.com)
It may be initiated by differences in ligand-induced intermediate conformational states, as shown for the β 2 -adrenergic receptor. (aspetjournals.org)

DAMGO inhibits neuronal survival promoted by CXCL12 [2] . (molcore.com)

An absence of δ receptors caused reduced efficacy of DAMGO without affecting potency. (aspetjournals.org)
The concept of intrinsic efficacy has been enshrined in pharmacology for half of a century, yet recent data have revealed that many ligands can differentially activate signaling pathways mediated via a single G protein-coupled receptor in a manner that challenges the traditional definition of intrinsic efficacy. (aspetjournals.org)

A family of serine-threonine kinases that are specific for G-PROTEIN-COUPLED RECEPTORS. (lookformedical.com)

Such effect was completely reversed both by the opioid receptor antagonist naloxone and by the unselective muscarinic receptor antagonist atropine. (researchgate.net)
Application of remifentanil hydrochloride potentiated the NMDA-induced inward current, and this potentiation was abolished by the mu-opioid receptor antagonist naloxone. (silverchair.com)

The inhibitory coupling of opioid receptors to voltage-dependent Ca 2+ channels (VDCCs) is a relatively inefficient process and therefore provides a sensitive assay of altered opioid receptor function and expression. (aspetjournals.org)
Interestingly, upon MOR activation by the agonist DAMGO, D40 MOR iN cells exhibit consistently stronger suppression of spontaneous inhibitory postsynaptic currents (sIPSCs) than N40 MOR iN cells across multiple subjects. (rutgers.edu)

The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. (lookformedical.com)
G protein-coupled receptor heteromerization is believed to exert dynamic regulatory impact on signal transduction. (biomedcentral.com)

In contrast, delta-opioid receptor (DOR) agonists disinhibited ACC pyramidal neuron responses to MThal inputs by suppressing local feed-forward GABA signaling from parvalbumin-positive interneurons. (elifesciences.org)

6. Muscarinic receptor activation, not a rise in [Ca 2+ ](i), was required to reveal the opioid response. (edu.au)

In this study, we examined the effect of Nocistatin on nociception and opioid analgesia by itself and the nociceptive effect of Nociceptin and antagonistic effect of nociceptin on opioid receptors in tail flick test when given the i.c.v. route. (unict.it)

Together, these data suggest that MOR, not other opioid receptor types or histamine, mediates scratching evoked by opioid analgesics. (ewha.ac.kr)

They are regulatory proteins that play a role in G-protein-coupled receptor densensitization. (lookformedical.com)
Although it is highly homologous to G-PROTEIN-COUPLED RECEPTOR KINASE 2, it is not considered to play an essential role in regulating myocardial contractile response. (lookformedical.com)
A G-protein-coupled receptor kinase subtype that is primarily expressed in the MYOCARDIUM and may play a role in the regulation of cardiac functions. (lookformedical.com)

21,22 Intravenous administration of μ-receptor agonists significantly depressed ventilatory responsiveness to hypercapnia in a dose-dependent manner in awake and/or anesthetized human and animals. (silverchair.com)

The medullary raphe region (MRR) contains abundant mu receptors responsible for analgesia and is also an important central area involving carbon dioxide chemoreception and contributing to the ventilatory responsiveness to hypercapnia. (silverchair.com)
It's been reported that intracerebroventricular shot of the receptor antagonist blocked 2 however, not 100 Hz electroacupuncture (EA)-produced analgesia within an uninjured pet model. (gasyblog.com)
Furthermore, within an uninjured pet model, 2 and 100 Hz EA analgesia is certainly mediated, respectively, by and opioid receptors (Han, 2003). (gasyblog.com)
On the supraspinal level, intracerebroventricular shot of CTOP, a receptor antagonist, obstructed 2 however, not 100 Hz EA-produced analgesia within an uninjured pet model (Huang et al. (gasyblog.com)

In view of postsynaptic density 95kDA (PSD95) tethers neuronal NO synthase (nNOS) to N-methyl-d-aspartate receptor (NMDAR), the PSD95-nNOS complex represents a therapeutic target of neuropathic pain. (bvsalud.org)
The A118G SNP causes a switch of asparagine (N) at position 40 of the mu-opioid receptor (MOR) to aspartate (D). To dissect the underlying neural and synaptic basis of the N40D MOR variant, we generated human GABAergic induced neuronal (iN) cells from induced pluripotent stem (iPS) cells of donors homozygous for either the major (N40) or minor (D40) alleles of the MOR. (rutgers.edu)

These data represent functional selectivity at the level of receptor desensitization. (bath.ac.uk)

Remifentanil hydrochloride contained in Ultiva (GlaxoSmithKline, Genval, Belgium) has been incriminated in difficult postoperative pain management, promotion of hyperalgesia, and direct N-methyl-D-aspartate (NMDA) receptor activation, but the involved mechanisms have remained unclear. (silverchair.com)
Considering that both components of Ultiva (remifentanil hydrochloride and glycine) could be involved in NMDA receptor activation, experiments were performed first with remifentanil hydrochloride, second with glycine, and third with the two components within Ultiva. (silverchair.com)
These results show that remifentanil hydrochloride does not directly activate NMDA receptors. (silverchair.com)
Induced NMDA current is potentiated by application of remifentanil hydrochloride through a pathway involving the mu-opioid receptor. (silverchair.com)

There is pharmacological evidence for subtypes of each receptor and other types of novel, less well-characterised opioid receptors, e , l , i , z , have also been postulated. (opioids.wiki)

The addition of a GSH coating on the liposomes did not result in an additional increase in DAMGO concentrations in the brain, in contrast to earlier studies on GSH coating. (springer.com)
In contrast, DAMGO-induced MOR desensitization was independent of PKC activity but was reduced by over-expression of the GRK2 DNM but not by that of a GRK6 DNM. (bath.ac.uk)
In sharp contrast, these responses were not observed when the DAMGO microinjection was made in the middle MRR or rostral MRR. (silverchair.com)

The responsiveness to the mu agonist and antagonist was greater in controls. (nih.gov)

furthermore, oxytocin-induced synaptic plasticity requires activation of nucleus accumbens 5-ht1b receptors, the blockade of which prevents social reward. (cognitive-liberty.online)
Specifically, D40 iN cells are unable to develop adaptive changes in synaptic function unlike N40 iN cells following long-term mu opioid receptor activation by DAMGO. (rutgers.edu)

CXC chemokine receptor 4 (CXCR4) and its ligand CXCL12, both of which are overexpressed in many cancers, play a pivotal role in metastasis. (biomedcentral.com)

Some terms for this phenomenon include functional selectivity, agonist-directed trafficking, and biased agonism. (aspetjournals.org)
Besides the heuristically interesting nature of functional selectivity, there is a clear impact on drug discovery, because this mechanism raises the possibility of selecting or designing novel ligands that differentially activate only a subset of functions of a single receptor, thereby optimizing therapeutic action. (aspetjournals.org)
Description Association of the non-synonymous single nucleotide polymorphism (SNP) rs1799971 in OPRM1 to drug dependence and alcohol abuse suggests it may have a functional consequence in altering receptor signaling in the brain. (rutgers.edu)

The authors found that systemic DAMGO significantly inhibited ventilation and the response to carbon dioxide by 20% and 31%, respectively, and these responses were significantly diminished to 11% and 14% after pretreatment of the caudal MRR with CTAP. (silverchair.com)
Since N-formyl peptides are found in MITOCHONDRIA and BACTERIA, this class of receptors is believed to play a role in mediating cellular responses to cellular damage and bacterial invasion. (lookformedical.com)

BACKGROUND AND PURPOSE: The ability of an agonist to induce desensitization of the mu-opioid receptor (MOR) depends upon the agonist used. (bath.ac.uk)

DAMGO ([d-Ala2, N-Me-Phe4, Gly-ol]-enkephalin), a mu-receptor agonist, was systemically administered (100 mug/kg) before and/or after local injection of CTAP (D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2) (100 ng/100 nl), a mu-receptor antagonist, into the caudal MRR, or locally administered (35 ng/100 nl) into the MRR subnuclei. (silverchair.com)

2002). It's been demonstrated the fact that vertebral opioid receptor antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) blocks 10 and100 Hz EA-produced anti-hyperalgesia within a comprehensive Freunds adjuvant (CFA)-induced inflammatory discomfort rat model, as the receptor antagonist nor-binaltorphimine (Nor-BNI) will not (Zhang et al. (gasyblog.com)
1996), however the function of RVM and opioid receptors in EA-produced anti-hyperalgesia within an inflammatory discomfort rat model had not been examined. (gasyblog.com)

A family of G-protein-coupled receptors that was originally identified by its ability to bind N-formyl peptides such as N-FORMYLMETHIONINE LEUCYL-PHENYLALANINE. (lookformedical.com)

Subsequent mechanisms that may play a role include diversity of G proteins, scaffolding and signaling partners, and receptor oligomers. (aspetjournals.org)

The aim of this study was to elucidate the roles of opioid receptor types and the site of action in opioid-induced itch in monkeys. (ewha.ac.kr)

In other animals the brains were excised and the ventral medial hypothalamic area removed and mu receptor expression determined using PCR. (nih.gov)
Therefore, the authors asked whether activation of mu receptors in the caudal, medial, or rostral MRR depressed ventilation and the response to hypercapnia, respectively. (silverchair.com)

Organisms2

Chemicals and Drugs41

Phenomena and Processes1

Information Science1

Neurons27

Opioids7

Morphine11

Selective8

Opioid agonists1

Intracellular6

Inhibition3

DPDPE5

Internalization1

Antagonists1

U695932

Rats5

Peptide5

Endogenous1

Adrenergic6

Inhibits1

Efficacy2

Kinases1

Antagonist naloxone2

Inhibitory2

SIGNAL TRANSDUCTION2

Delta-opioid r1

Muscarinic receptor1

Nociceptin1

Scratching evoked1

Protein-coupled receptor3

Intravenous1

Analgesia4

Neuronal2

Level of receptor1

Remifentanil4

Subtypes1

Contrast3

Responsiveness1

Synaptic2

Ligand1

Functional3

Responses2

Induce1

CTAP1

Hyperalgesia2

Bind1

Mechanisms1

Elucidate1

Medial2