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Kor Antagonist

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https://www.readbyqxmd.com/read/29056156/dynorphin-kappa-opioid-receptor-signaling-in-preclinical-models-of-alcohol-drug-and-food-addiction
#1
Anushree Karkhanis, Katherine M Holleran, Sara R Jones
The dynorphin/kappa opioid receptor (KOR) system is implicated in the "dark side" of addiction, in which stress exacerbates maladaptive responses to drug and alcohol exposure. For example, acute stress and acute ethanol exposure result in an elevation in dynorphin, the KOR endogenous ligand. Activation of KORs results in modulation of several neurotransmitters; however, this chapter will focus on its regulatory effects on dopamine in mesolimbic areas. Specifically, KOR activation has an inhibitory effect on dopamine release, thereby influencing reward processing...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/29037662/effects-of-pharmacological-manipulation-of-the-kappa-opioid-receptors-on-the-aversive-effects-of-nicotine
#2
Melissa Ward, Haval Norman, Manoranjan S D'Souza
Nicotine, an addictive component of tobacco smoke, produces both rewarding and aversive effects. Increasing the aversive effects of nicotine may help in promoting smoking cessation. However, neural targets mediating the aversive effects of nicotine have not been fully identified. In this study, we evaluated the role of kappa opioid receptors (KORs) in the aversive effects of nicotine (0.4 mg/kg, base; s.c.) using the nicotine-induced conditioned taste aversion (CTA) model in Wistar rats. The KORs were activated using the selective KOR agonist (±)U-50,488H (0, 0...
October 14, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28975684/salvinorin-a-reduces-neuropathic-nociception-in-the-insular-cortex-of-the-rat
#3
U Coffeen, A Canseco-Alba, K Simón-Arceo, A Almanza, F Mercado, M León-Olea, F Pellicer
BACKGROUND: Neuropathic pain is one of the most important challenges in public health. The search for novel treatments is important for an adequate relief without adverse effects. In this sense salvinorin A (SA), the main diterpene of the medicinal plant Salvia divinorum is an important antinociceptive compound, which acts as a potent agonist of kappa opioid receptor (KOR) and cannabinoid CB1 receptors. METHODS: We evaluated nociceptive responses in a neuropathic pain model induced by the sciatic nerve ligature (SNL) in the right hind paw, after the microinjection of SA, Salvinorin B (SB), KOR and CB1 antagonists directly in the insular cortex (IC) in male wistar rats...
October 4, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28945940/opioid-receptors-mediate-inotropic-and-depressor-effects-of-apelin-in-rats-with-2k1c-induced-chronic-renovascular-hypertension
#4
Farzaneh Rostamzadeh, Hamid Najafipour, Mahboobeh Yeganeh-Hajahmadi, Siyavash Joukar
Apelin receptors (APJ) cross-talk with other G-protein-coupled receptors. However, the role of APJ interaction with opioid receptors (OPR) on the cardiovascular effects of apelin in hypertension is not clear. Renovascular hypertension was induced by placing a Plexiglas clip on the left kidney of rats. After 16 weeks, F13A (an APJ antagonist), naloxone (a general OPR inhibitor), and nor-binaltorphimine dihydrochloride (nor-BNI; a selective inhibitor of KOR) were given prior to injections of apelin at doses of 40 and 60 μg/kg...
September 25, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28930716/antinociceptive-effect-of-ghrelin-in-a-rat-model-of-irritable-bowel-syndrome-involves-trpv1-opioid-systems
#5
Yuqing Mao, Zhengyang Li, Kan Chen, Huafang Yu, Shaoren Zhang, Miao Jiang, Yuanhua Ma, Chunli Liang, Hongyan Liu, Huanqing Li, Qian Hua, Hao Zhou, Yonghong Sun, Xiaoming Fan
BACKGROUND/AIMS: Irritable bowel syndrome (IBS), defined as recurrent abdominal pain and changes in bowel habits, seriously affects quality of life and ability to work. Ghrelin is a brain-gut hormone, which has been reported to show antinociceptive effects in peripheral pain. We investigated the effect of ghrelin on visceral hypersensitivity and pain in a rat model of IBS. METHODS: Maternal deprivation (MD) was used to provide a stress-induced model of IBS in Wistar rats...
2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28807672/pharmacological-characterization-of-novel-synthetic-opioids-nso-found-in-the-recreational-drug-marketplace
#6
REVIEW
Michael H Baumann, Susruta Majumdar, Valerie Le Rouzic, Amanda Hunkele, Rajendra Uprety, Xi Ping Huang, Jin Xu, Bryan L Roth, Ying-Xian Pan, Gavril W Pasternak
Novel synthetic opioids (NSO) are increasingly encountered in illicit heroin and counterfeit pain pills. Many NSO are resurrected from older biomedical literature or patent applications, so limited information is available about their biological effects. Here we examined the pharmacology of three structurally-distinct NSO found in the recreational drug market: N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylbutyramide (butyrylfentanyl), 3,4-dichloro-N-[(1R,2R)-2-(dimethylamino)cyclohexyl]-N-methylbenzamide (U-47700) and 1-cyclohexyl-4-(1,2-diphenylethyl)piperazine (MT-45)...
August 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28770825/kappa-opioid-receptor-agonist-u50448h-protects-against-renal-ischemia-reperfusion-injury-in-rats-via-activating-the-pi3k-akt-signaling-pathway
#7
Li-Jie Liu, Jian-Jun Yu, Xiao-Lin Xu
Renal ischemia-reperfusion injury (IRI) is regarded as a leading cause of acute kidney failure and renal dysfunction. Previous studies show that kappa opioid receptor (KOR) agonists can attenuate IRI in cardiomycytes and neuronal cells. In this study we explored the effects of a KOR agonist on renal IRI and the underlying mechanisms in vivo and in vitro. An IRI model was established in SD rats, which were intravenously pretreated with a KOR agonist U50448H (1 mg/kg), a KOR antagonist Nor-BNI (2 mg/kg) followed by U50448H (1 mg/kg), or the PI3K inhibitor wortmannin (1...
August 3, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28747521/a-novel-18-f-labeled-kappa-opioid-receptor-antagonist-as-pet-radiotracer-synthesis-and-in-vivo-evaluation-of-18-f-ly2459989-in-non-human-primates
#8
Songye Li, Zhengxin Cai, Ming-Qiang Zheng, Daniel Holden, Mika Naganawa, Shu-Fei Lin, Jim Ropchan, David Labaree, Michael Kapinos, Teresa Lara-Jaime, Antonio Navarro, Yiyun Huang
The kappa opioid receptor (KOR) is implicated in depression, addictions, and other central nervous system (CNS) disorders and thus an important target for drug development. We have previously developed a number of (11)C-labeled PET radiotracers for KOR imaging in humans. Here we report the synthesis and evaluation of (18)F-LY2459989 as the first (18)F-labeled KOR antagonist radiotracer in non-human primates and its comparison with (11)C-LY2459989. Methods: The novel radioligand (18)F-LY2459989 was synthesized by (18)F-displacement of a nitro group or an iodonium ylide...
July 26, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28739044/essential-structure-of-orexin-1-receptor-antagonist-ynt-707-part-i-role-of-the-4-5-epoxy-ring-for-binding-with-orexin-1-receptor
#9
Naoshi Yamamoto, Sayaka Ohrui, Takahiro Okada, Masahiro Yata, Tsuyoshi Saitoh, Noriki Kutsumura, Yasuyuki Nagumo, Yoko Irukayama-Tomobe, Yasuhiro Ogawa, Yukiko Ishikawa, Yurie Watanabe, Daichi Hayakawa, Hiroaki Gouda, Masashi Yanagisawa, Hiroshi Nagase
The essential structure of the orexin 1 receptor (OX1R) antagonist YNT-707 (2) was clarified, particularly the roles to OX1R antagonist activities of the 3-OMe, the 4,5-epoxy ring, the 14-hydroxy group, and the orientation of the 6-amide side chain. The 3-OMe and 17-sulfonamide group were shown to be essential for the OX1R antagonistic activity. The 4,5-epoxy ring plays an important role for the active orientation of the 6-amide group. The 14-hydroxy group could lower the activity of the 6β-amide isomer by the interaction of the 14-hydroxy group with the 6-amide group, which could orient the 6-amide group toward the upper side of the C-ring...
September 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28738113/estrogen-status-gates-effects-of-kappa-opioid-receptor-on-temporomandibular-joint-responsive-neurons-at-the-spinomedullary-junction-in-female-rats
#10
Akimasa Tashiro, David A Bereiter, Yasuhiro Nishida
AIMS: To determine whether estrogen status alters κ-opioid inhibition of nociceptive processing by affecting temporomandibular joint (TMJ) input to neurons in the trigeminal subnucleus caudalis [Vc]/C1-2 region at the spinomedullary junction in female rats. METHODS: TMJ-responsive neurons were recorded in laminae I-II of the Vc/C1-2 region at the spinomedullary junction of ovariectomized female rats treated for 2 days with low-dose estradiol (LE group; 2 mg/day) or high-dose estradiol (HE group; 20 mg/day)...
July 2017: Journal of Oral & Facial Pain and Headache
https://www.readbyqxmd.com/read/28726402/opioid-receptor-modulators-with-a-cinnamyl-group
#11
Lokesh Ravilla, N Venkata Subba Naidu, Shalini Dogra, Deepmala Umrao, Prem N Yadav, Ansuman Biswas, Daliah Michael, Kanagaraj Sekar, Kuppuswamy Nagarajan
To obtain selective and potent opioid receptor ligands, we synthesized dehydro derivatives of alvimopan and found compound (28f), a selective but modest affinity MOR antagonist weaker than alvimopan (1). We replaced the arylpiperidine unit by an arylpiperazine to obtain the 1-(α-carboxycinnamyl)-4-arylpiperazines like 13h, which to our surprise had no MOR or DOR activity but was a KOR agonist with moderate affinity. In contrast, literature examples of arylpiperazines 4 and 5 were reported to be pan opioid receptor antagonists, while 6 was a MOR agonist...
August 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28674176/effects-of-chronic-social-defeat-stress-on-sleep-and-circadian-rhythms-are-mitigated-by-kappa-opioid-receptor-antagonism
#12
Audrey M Wells, Elysia Ridener, Clinton A Bourbonais, Woori Kim, Harry Pantazopoulos, F Ivy Carroll, Kwang-Soo Kim, Bruce M Cohen, William A Carlezon
Stress plays a critical role in the neurobiology of mood and anxiety disorders. Sleep and circadian rhythms are affected in many of these conditions. Here we examined the effects of chronic social defeat stress (CSDS), an ethological form of stress, on sleep and circadian rhythms. We exposed male mice implanted with wireless telemetry transmitters to a 10 day CSDS regimen known to produce anhedonia (a depressive-like effect) and social avoidance (an anxiety-like effect). EEG, EMG, body temperature, and locomotor activity data were collected continuously during the CSDS regimen and a 5 day recovery period...
August 9, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28649993/kappa-opioid-receptor-activation-in-dopamine-neurons-disrupts-behavioral-inhibition
#13
Antony D Abraham, Harrison M Fontaine, Allisa J Song, Mackenzie M Andrews, Madison A Baird, Brigitte L Kieffer, Benjamin B Land, Charles Chavkin
The dynorphin/kappa opioid receptor (KOR) system has been previously implicated in the regulation of cognition, but the neural circuitry and molecular mechanisms underlying KOR-mediated cognitive disruption are unknown. Here, we used an operational test of cognition involving timing and behavioral inhibition and found that systemic KOR activation impairs performance of male and female C57BL/6 mice in the differential reinforcement of low response rates (DRL) task. Systemic KOR antagonism also blocked stress-induced disruptions of DRL performance...
June 26, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28642282/kappa-opioid-receptors-mediate-heterosynaptic-suppression-of-hippocampal-inputs-in-the-rat-ventral-striatum
#14
Julie M Brooks, Patricio O'Donnell
Kappa opioid receptors (KORs) are highly enriched within the ventral striatum (VS) and are thought to modulate striatal neurotransmission. This includes presynaptic inhibition of local glutamatergic release from excitatory inputs to the VS. However, it is not known which inputs drive this modulation and what impact they have on the local circuit dynamics within the VS. Individual medium spiny neurons (MSNs) within the VS serve as a site of convergence for glutamatergic inputs arising from the PFC and limbic regions, such as the hippocampus (HP)...
July 26, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28590714/reaching-out-for-sensitive-evaluation-of-the-mu-opioid-receptor-in-vivo-positron-emission-tomography-imaging-of-the-agonist-11-c-ah7921
#15
Waqas Rafique, Shivashankar Khanapur, Mona M Spilhaug, Patrick J Riss
Imaging of the mu opioid receptor (MOR) availability with positron emission tomography (PET) is a pertinent challenge in Neuroscience. Both, regulation of receptor expression and occupancy by endogeneous opioids play into cognitive and behavioral phenotypes of healthy function and disease. Receptor expression in the active and inactive states can be measured using high affinity radioagonist and radioantagonist PET tracers, respectively. Occupancy assessment requires radioligands showing competitive and reversible binding with moderate affinity to the MOR, which may lead to physical extinction of the receptor specific signal in vivo...
June 27, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28589966/role-of-%C3%AE%C2%BA-opioid-receptors-in-the-bed-nucleus-of-stria-terminalis-in-reinstatement-of-alcohol-seeking
#16
A D Lê, Douglas Funk, Kathleen Coen, Sahar Tamadon, Yavin Shaham
κ-Opioid receptors (KORs) and their endogenous ligand dynorphin are involved in stress-induced alcohol seeking but the mechanisms involved are largely unknown. We previously showed that systemic injections of the KOR agonist U50,488, which induce stress-like aversive states, reinstate alcohol seeking after extinction of the alcohol-reinforced responding. Here, we used the neuronal activity marker Fos and site-specific injections of the KOR antagonist nor-BNI and U50,488 to study brain mechanisms of U50,488-induced reinstatement of alcohol seeking...
June 7, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28512665/involvement-of-%C3%A2%C2%B5-opioid-receptors-and-%C3%AE%C2%BA-opioid-receptors-in-itch-related-scratching-behaviour-of-imiquimod-induced-psoriasis-like-dermatitis-in-mice
#17
Nobuaki Takahashi, Mitsutoshi Tominaga, Ryohei Kosaka, Yayoi Kamata, Yoshie Umehara, Hironori Matsuda, Azumi Sakaguchi, Hideoki Ogawa, Kenji Takamori
The pathogenesis of psoriatic itch is poorly understood. The aim of this study was to investigate the involvement of opioid receptors in scratching behaviour of imiquimod-induced psoriasis-like dermatitis model mice. Topical application of 5% imiquimod cream to the rostral back skin of mice induced antihistamine-resistant scratching behaviour. The expression of µ-opioid receptor (MOR) protein increased in the epidermis, dorsal root ganglia (DRG) and spinal cord of imiquimod-treated mice. In contrast, the expression of κ-opioid receptor (KOR) protein decreased in the DRG and spinal cord of imiquimod-treated mice, and was undetectable in the epidermis of both groups...
August 31, 2017: Acta Dermato-venereologica
https://www.readbyqxmd.com/read/28501425/the-effects-of-kratom-on-restraint-stress-induced-analgesia-and-its-mechanisms-of-action
#18
José Luis Vázquez López, Lorenz Schild, Thomas Günther, Stefan Schulz, Hartmud Neurath, Axel Becker
ETHNOPHARMACOLOGICAL RELEVANCE: Mitragyna speciosa and its extracts are called kratom (dried leaves, extract). They contain several alkaloids with an affinity for different opioid receptors. They are used in traditional medicine for the treatment of different diseases, as a substitute by opiate addicts, and to mitigate opioid withdrawal symptoms. Apart from their medical properties, they are used to enhance physical endurance and as a means of overcoming stress. PURPOSE: The aim of this study was to determine the mechanisms underlying the effects of kratom on restraint-stress-induced analgesia which occurs during or following exposure to a stressful or fearful stimulus...
June 9, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28449351/long-term-plasticity-of-corticostriatal-synapses-is-modulated-by-pathway-specific-co-release-of-opioids-through-%C3%AE%C2%BA-opioid-receptors
#19
Sarah L Hawes, Armando G Salinas, David M Lovinger, Kim T Blackwell
KEY POINTS: Both endogenous opioids and opiate drugs of abuse modulate learning of habitual and goal-directed actions, and can also modify long-term plasticity of corticostriatal synapses. Striatal projection neurons of the direct pathway co-release the opioid neuropeptide dynorphin which can inhibit dopamine release via κ-opioid receptors. Theta-burst stimulation of corticostriatal fibres produces long-term potentiation (LTP) in striatal projection neurons when measured using whole-cell patch recording...
August 15, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28425121/role-of-the-dynorphin-kappa-opioid-receptor-system-in-the-motivational-effects-of-ethanol
#20
REVIEW
Rachel I Anderson, Howard C Becker
Evidence has demonstrated that dynorphin (DYN) and the kappa opioid receptor (KOR) system contribute to various psychiatric disorders, including anxiety, depression, and addiction. More recently, this endogenous opioid system has received increased attention as a potential therapeutic target for treating alcohol use disorders. In this review, we provide an overview and synthesis of preclinical studies examining the influence of alcohol (ethanol [EtOH]) exposure on DYN/KOR expression and function, as well as studies examining the effects of DYN/KOR manipulation on EtOH's rewarding and aversive properties...
August 2017: Alcoholism, Clinical and Experimental Research
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