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Mu opiod

Ismaliza Ismail, Suzaily Wahab, Hatta Sidi, Srijit Das, Loo Jiann Lin, Rosdinom Razali
Kratom (Mitragynaspeciosa), a natural existing plant found in South-East Asia, is tradi-tionally used as an herb to help to elevate a person's energy and also to treat numerous medical ailments. Other than the analgesic property, kratom has been used as an agent to overcome opioid withdrawal as it contains natural alkaloids, i.e. mitragynine, 7-hydroxymitragynine, and MGM-9, which has agonist affinity on the opioid receptors, including mu (μ) and kappa (κ). The role of neural reward pathway linked to μ-opioid receptors and both dopaminergic and GABA-ergic interneurons that express μ-opioid receptors were deliberated...
April 25, 2017: Current Drug Targets
Neel Mehta, Kelli O'Connell, Gregory P Giambrone, Aisha Baqai, Sudhir Diwan
OBJECTIVE: Constipation is a common adverse effect in patients requiring long-term opioid therapy for pain control. Methylnaltrexone, a quaternary peripheral mu-opioid receptor antagonist, is an effective treatment of opioid induced constipation (OIC) without affecting centrally mediated analgesia. Our objective was to conduct a review and meta-analysis to evaluate the efficacy of methylnaltrexone for treatment of OIC, as well as to provide a clinical discussion regarding newly developed alternatives and provide the current treatment algorithm utilized at our institution...
2016: Postgraduate Medicine
Gina Games, Amber Hutchison
With the prevalence of diabetes mellitus (DM) increasing, pathologic complications such as diabetic peripheral neuropathy (DPN) are also becoming more common. Of those diagnosed with DM, 10% to 20% of patients suffer from painful DPN. Until recently, only pregabalin and duloxetine possessed Food and Drug Administration (FDA) approval for this condition. However, FDA recently approved tapentadol-ER [extended release] (Nucynta ER) for painful DPN. Tapentadol-ER is an opioid analgesic commonly used for the treatment of moderate-to-severe chronic pain that contains a unique dual mechanism acting as both a weak mu-opiod receptor agonist and norepinephine-reuptake inhibitor...
October 2013: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
Elzbieta P Wala, Joseph R Holtman, Paul A Sloan
BACKGROUND: Opioids may cause progressive enhancement of pain sensitivity (opioid-induced hyperalgesia [OIH]) and thus, exacerbate existing pain. Animal studies also demonstrate paradoxical OIH with an ultralow dose (ULD, subanalgesic) of opioid; eg, the μ-opioid, morphine. Repeated administration of ULD-morphine resulted in tolerance to ULD-OIH. Prior exposure to ULD-morphine prolonged subsequent morphine antinociception in intact rats (delay of tolerance) and blocked neuropathic pain in nerve-injured rats (no hyperalgesia)...
March 2013: Journal of Opioid Management
Shanna L Resendez, Brandon J Aragona
Social bonds are important for human health and well-being, and a crucial component of these bonds is the ability to maintain a bond once it has been formed. Importantly, although bond maintenance is required for social attachments, very little is known about the neural mechanisms that mediate this behavior. Recently, laboratory studies utilizing the socially monogamous prairie vole (an excellent animal model for the neurobiology of selective social attachment), have allowed the neural correlates of selective social attachment to begin to unfold...
2013: Reviews in the Neurosciences
Peck Y Ong
Atopic dermatitis (AD) is the most common chronic inflammatory skin disease, affecting 10-20% of children and 2% of adults worldwide. Preventive treatment of AD consists of daily skin hydration and emollient therapy; but the majority of patients still require symptomatic treatment with topical corticosteroids and/or topical calcineurin inhibitors, both of which may be associated with potential long-term side effects. With increasing evidence supporting the role of skin barrier defects in the pathogenesis of AD, there is also a parallel increase in medications that claim to assist barrier repair...
March 2009: Expert Opinion on Emerging Drugs
M Gironi, F Martinelli-Boneschi, P Sacerdote, C Solaro, M Zaffaroni, R Cavarretta, L Moiola, S Bucello, M Radaelli, V Pilato, Me Rodegher, M Cursi, S Franchi, V Martinelli, R Nemni, G Comi, G Martino
A sixth month phase II multicenter-pilot trial with a low dose of the opiate antagonist Naltrexone (LDN) has been carried out in 40 patients with primary progressive multiple sclerosis (PPMS). The primary end points were safety and tolerability. Secondary outcomes were efficacy on spasticity, pain, fatigue, depression, and quality of life. Clinical and biochemical evaluations were serially performed. Protein concentration of beta-endorphins (BE) and mRNA levels and allelic variants of the mu-opiod receptor gene (OPRM1) were analyzed...
September 2008: Multiple Sclerosis: Clinical and Laboratory Research
Cindy L Ehlers, Penelope A Lind, Kirk C Wilhelmsen
BACKGROUND: Variation in response to the hedonic and adverse effects of a substance is in part an inherited factor that may influence its use, abuse and dependence. The mu opioid receptor is the primary site of action for opiates and individuals with polymorphisms in this receptor appear to have variation in the CNS effects of opiates. Several studies have suggested that this receptor may also mediate some of the effects of non-opioid drugs, such as alcohol. The purpose of this study was to investigate associations between 13 single nucleotide polymorphisms in the mu opioid receptor gene (OPRM1) with self-reported responses to alcohol, an endophenotype associated with the development of alcohol dependence, in American Indians living on eight contiguous reservations...
April 23, 2008: BMC Medical Genetics
S J Ribeiro, J G Ciscato, R de Oliveira, R C de Oliveira, R D'Angelo-Dias, A D Carvalho, T T Felippotti, E C C Rebouças, L Castellan-Baldan, A Hoffmann, S A L Corrêa, J E Moreira, N C Coimbra
In the present study, the functional neuroanatomy of nigrotectal-tectonigral pathways as well as the effects of central administration of opioid antagonists on aversive stimuli-induced responses elicited by electrical stimulation of the midbrain tectum were determined. Central microinjections of naloxonazine, a selective mu(1)-opiod receptor antagonist, in the mesencephalic tectum (MT) caused a significant increase in the escape thresholds elicited by local electrical stimulation. Furthermore, either naltrexone or naloxonazine microinjected in the substantia nigra, pars reticulata (SNpr), caused a significant increase in the defensive thresholds elicited by electrical stimulation of the continuum comprised by dorsolateral aspects of the periaqueductal gray matter (dlPAG) and deep layers of the superior colliculus (dlSC), as compared with controls...
December 2005: Journal of Chemical Neuroanatomy
Robert E Gawley, Mykhaylo Dukh, Claudia M Cardona, Stephan H Jannach, Denise Greathouse
[reaction: see text] Ohmefentanyl binds to the rat mu-opiod receptor via two dipeptide sequences (Trp-His and Asp-Tyr) that are separated by 170 residues. A turn-inducing tripeptide, Pro-Aib-Aib, holds the dipeptides in a conformation that binds the narcotic (K(b) = 7.1 x 10(4) M(-)(1)) in THF. Binding is specific for ohmefentanyl over morphine and is accompanied by a conformational change in the heptapeptide host. Control experiments with a Gly-Gly-Gly tripeptide linking the dipeptides show no evidence of binding...
July 7, 2005: Organic Letters
T Iu Rebrova, L N Maslov, Iu B Lishmanov
The six hour stress in rats was modeled by the method of O. Desiderato. Cardiac damage was estimated by myocardial uptace of radioactive 99Tc-pyrophosphate. Intravenous administration of mixed mu and delta opioid receptor agonist, D- Ala2, Leu5, Arg6-enkephalin (dalargin), (non-penetrating through the blood brain barrier) at a dose of 0.1 mg/kg before stress decreased stress-induced 99Tc-pyroposphate uptake. Pretreatment with dalargin completely abolished the stress-induced increase in conjugated dienes and malondialdehyde levels in myocardium and prevented a decrease in total lipid soluble antioxidant levels in the heart after stress exposure...
March 2005: Biomedit︠s︡inskai︠a︡ Khimii︠a︡
Brigitte L Kieffer, Claire Gavériaux-Ruff
The endogenous opioid system consists of three opioid peptide precursor genes encoding enkephalins (preproenkephalin, Penk), dynorphins (preprodynorphin, Pdyn) and beta-endorphin (betaend), proopiomelanocortin (POMC) and three receptor genes encoding mu-opiod receptor (MOR), delta-opiod receptor (DOR) and kappa-opiod receptor (KOR). In the past years, all six genes have been inactivated in mice by homologous recombination. The analysis of spontaneous behavior in mutant mice has demonstrated significant and distinct roles of each gene in modulating locomotion, pain perception and emotional behaviors...
April 2002: Progress in Neurobiology
S F Martin, M P Dwyer, B Hartmann, K S Knight
It is known that peptide mimics containing trans-substituted cyclopropanes stabilize extended conformations of oligopeptides, and molecular modeling studies now suggest that the corresponding cis-cyclopropane dipeptide isosteres could stabilize a reverse turn. To begin to assess this possibility, a series of cis-substituted cyclopropanes were incorporated as replacements of the Gly(2)-Gly(3) and Phe(4)-Leu(5) dipeptide subunits in Leu-enkephalin (H(2)N-Tyr-Gly-Gly-Phe-Leu-OH), which is believed to bind to opiod receptors in a conformation containing a beta-turn...
March 10, 2000: Journal of Organic Chemistry
T Miyagi, L F Chuang, K M Lam, H Kung, J M Wang, B I Osburn, R Y Chuang
Opioid users having acquired human immunodeficiency syndrome (AIDS) are at a greater risk than non-users of contracting opportunistic infections. Opioid-administered and simian immunodeficiency virus (SIV)-infected rhesus monkeys have been an excellent model for studying AIDS and drug abuse in humans. In this study, chemotaxis of monkey leukocytes was evaluated using the chemokines interleukin-8 (IL-8) and regulated upon activation, normal T cell expressed (RANTES) as the chemoattractants, and the effects of various opioid agonists and antagonists on the efficiency of chemotaxis were examined...
April 2000: Immunopharmacology
T Endoh, H Matsuura, A Tajima, N Izumimoto, C Tajima, T Suzuki, A Saitoh, T Suzuki, M Narita, L Tseng, H Nagase
TRK-820, a new type of 4,5-epoxymorphinan derivative, was investigated in vivo for antinociceptive activities and its selectivity on various opioid receptors in mice. TRK-820 given s.c. or p.o. was found to be 351- and 796-fold more potent than U50,488H with acetic acid-induced abdominal constriction test. The duration of the antinociceptive effect produced by TRK-820 was longer than that produced by mu-opioid receptor agonist morphine or other kappa-opioid receptor agonists. In addition, with four other antinociceptive assays, low temperature hot plate (51 degrees C), thermal tail flick, mechanical tail pressure and tail pinch tests, TRK-820 was also found to be 68- to 328-fold more potent than U-50488H, and 41- to 349-fold more potent than morphine in producing antinociception, as comparing the weight of the different compound...
1999: Life Sciences
Y X Pan, J Xu, E Bolan, C Abbadie, A Chang, A Zuckerman, G Rossi, G W Pasternak
We have identified four new mu-opiod receptor (MOR)-1 exons, indicating that the gene now contains at least nine exons spanning more than 200 kilobases. Replacement of exon 4 by combinations of the new exons yields three new receptors. When expressed in Chinese hamster ovary cells, all three variants displayed high affinity for mu-opioid ligands, but kappa and delta drugs were inactive. However, there were subtle, but significant, differences in the binding profiles of the three variants among themselves and from MOR-1...
August 1999: Molecular Pharmacology
G Ronsisvalle, O Prezzavento, L Pasquinucci, M S Pappalardo, A Marrazzo, F Vittorio, L Carboni, S Spampinato
The synthesis and the in vitro receptor affinity for sigma 1 and opiod receptors of the two diastereoisomers of (+)-cis-MPCB namely, (+)-cis-(1'S,2'R)-6,11-Dimethyl-1,2,3,4,5,6 -hexahydro-3-[[2'-(methoxycarbonyl)-2'-phenylcyclopropyl]methyl]-2 ,6 -methano-3-benzazocin-8-ol, (1'S,2'R)6a and (+)-cis-(1'R,2'S)-6,11-Dimethyl-1,2,3,4,5,6-hexahydro-3- [[2-(methoxycarbonyl)-2'-phenylcyclopropyl]methyl]-2,6-methano-3-+ ++benzazocin-8 -ol, (1'R,2'S)6a are reported. Affinities of (1'S,2'R)6a and (1'R,2'S)6a were compared with those of the (-)-cis-diastereoisomers of MPCB(1), and of its p-Cl phenyl derivative CCB(2)...
June 1997: Il Farmaco
P Sacerdote, M Bianchi, A E Panerai
This study investigates the role of the opiod receptors and of the opioid peptide beta-endorphin in the development of yeast-induced inflammation in the rat paw. Pretreatment with the opioid receptor antagonist naltrexone (10 mg/kg i.p.) exacerbates the paw edema, while morphine pretreatment (5 and 10 mg/kg) reduces it. In addition, the intravenous injection of a specific anti-beta-endorphin antibody aggravates the yeast-induced inflammation. On the contrary, both the kappa-opioid receptor antagonist MR 1452 (2...
July 5, 1996: Regulatory Peptides
P Sánchez-Blázquez, A García-España, J Garzón
For 5 consecutive days repeated intracerebroventricular (i.c.v.) administration of antisense oligodeoxynucleotides (ODNs) to G alpha subunit mRNAs was used to impair the function of mouse Gi1, Gi2, Gi3 and Gx/z regulatory proteins. Decreases of 20 to 60% on the G alpha-like immunoreactivity could be observed in neural structures of mouse brain, an effect that was not produced by a random-sequence ODN used as a control. The ODN to Gi1 alpha subunits lacked effect on opioid-evoked analgesia. In mice injected with the ODN to Gi2 alpha subunits the antinociceptive activity of all the opioids studied appeared greatly impaired...
December 1995: Journal of Pharmacology and Experimental Therapeutics
G E De Lander, G J Keil
Intrathecal administration of adenosine or adenosine analogs causes antinociception. In addition, opioid-induced antinociception is mediated, in part, by spinal adenosine release. Recent investigations from our laboratory suggest the significance of adenosine in opioid-mediated actions varies between different pharmacologic effects of opioid agonists and may vary after selective activation of different opioid receptor subtypes. A series of investigations using isobolographic analysis were designed to examine the functional significance of adenosine in antinociception induced by opioid receptor-selective agonists in the mouse tail-flick assay...
February 1994: Journal of Pharmacology and Experimental Therapeutics
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