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1. Full Text Modified Synthesis of NOP Receptor Antagonist SB612111
by Perrey, David A and Li, Jun-Xu and Zhang, Yanan
Synthesis, ISSN 0039-7881, 03/2017, Volume 49, Issue 6, pp. 1394 - 1400
Abstract SB612111 [(5 S ,7 S )-7-{[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl}-1-methyl-6,7,8,9-tetrahydro-5 H -benzo[7]annulen-5-ol] is a potent and... 
paper | modified synthesis | SB612111 | antagonist | NOP | PHARMACOLOGICAL CHARACTERIZATION | CHEMISTRY, ORGANIC | ORL1 | DISCOVERY | MEMBER | OPIOID RECEPTOR | THERAPEUTIC TARGET | GENE FAMILY | CDNA CLONING | SB-612111 | NOCICEPTIN/ORPHANIN FQ RECEPTOR
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2. Full Text Pharmacological properties of S1RA, a new sigma‐1 receptor antagonist that inhibits neuropathic pain and activity‐induced spinal sensitization
by Romero, L and Zamanillo, D and Nadal, X and Sánchez‐Arroyos, R and Rivera‐Arconada, I and Dordal, A and Montero, A and Muro, A and Bura, A and Segalés, C and Laloya, M and Hernández, E and Portillo‐Salido, E and Escriche, M and Codony, X and Encina, G and Burgueño, J and Merlos, M and Baeyens, JM and Giraldo, J and López‐García, JA and Maldonado, R and Plata‐Salamán, CR and Vela, JM
British Journal of Pharmacology, ISSN 0007-1188, 08/2012, Volume 166, Issue 8, pp. 2289 - 2306
BACKGROUND AND PURPOSE The sigma‐1 (σ 1 ) receptor is a ligand‐regulated molecular chaperone that has been involved in pain, but there is limited understanding... 
central sensitization | neuropathic pain | S1RA (E‐52862) | sigma‐1 receptor | S1RA (E-52862)σ-1 receptor | NMDA RECEPTOR | ACTIVATION | RAT | PHOSPHORYLATION | S1RA (E-52862) | sigma-1 receptor | GUINEA-PIG BRAIN | PERIPHERAL-NERVE INJURY | CORTICAL-NEURONS | OPIOID ANALGESIA | PHARMACOLOGY & PHARMACY | FORMALIN TEST | METHYL-D-ASPARTATE | Analgesics - pharmacology | Electric Stimulation | Capsaicin - toxicity | Gene Expression Regulation - physiology | Morpholines - pharmacology | Male | Receptors, sigma - antagonists & inhibitors | Neuralgia - drug therapy | Behavior, Animal | Gene Expression Regulation - drug effects | Animals | Mice | Formaldehyde - toxicity | Pain Measurement | Pyrazoles - pharmacology | Physiological aspects | Care and treatment | Pain | Analysis | Medical research | Index Medicus | Research Papers
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3. Full Text Modulation of gastrointestinal function by MuDelta, a mixed µ opioid receptor agonist/ µ opioid receptor antagonist
by Wade, PR and Palmer, JM and McKenney, S and Kenigs, V and Chevalier, K and Moore, BA and Mabus, JR and Saunders, PR and Wallace, NH and Schneider, CR and Kimball, ES and Breslin, HJ and He, W and Hornby, PJ
British Journal of Pharmacology, ISSN 0007-1188, 11/2012, Volume 167, Issue 5, pp. 1111 - 1125
BACKGROUND & PURPOSE Loperamide is a selective µ opioid receptor agonist acting locally in the gastrointestinal (GI) tract as an effective anti‐diarrhoeal but... 
δ opioid receptor | motility | visceral pain | gastrointestinal secretion | irritable bowel syndrome | opioid | Guinea Pigs | Rats, Wistar | Humans | Analgesics, Opioid - pharmacology | Gastrointestinal Motility - drug effects | Gastrointestinal Motility - physiology | Macaca fascicularis | Rats | Male | Receptors, Opioid, mu - agonists | Receptors, Opioid, mu - antagonists & inhibitors | Rats, Sprague-Dawley | Animals | Narcotic Antagonists - pharmacology | HEK293 Cells | Female | Mice | Receptors, Opioid, mu - physiology | Index Medicus | Research Papers
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4. Full Text A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies
by Post, Anke and Smart, Trevor S and Krikke-Workel, Judith and Dawson, Gerard R and Harmer, Catherine J and Browning, Michael and Jackson, Kimberley and Kakar, Rishi and Mohs, Richard and Statnick, Michael and Wafford, Keith and McCarthy, Andrew and Barth, Vanessa and Witkin, Jeffrey M
Neuropsychopharmacology, ISSN 0893-133X, 06/2016, Volume 41, Issue 7, pp. 1803 - 1812
Nociceptin/Orphanin FQ (N/OFQ) is an endogenous ligand of the N/OFQ peptide (NOP) receptor, which is a G protein-coupled receptor in brain regions associated... 
ANTIDEPRESSANT-LIKE | EFFICACY | PSYCHIATRY | FORCED SWIMMING TEST | NEUROSCIENCES | REUPTAKE INHIBITION | IN-VIVO | MEDIAL PREFRONTAL CORTEX | DOUBLE-BLIND | ORL1 RECEPTOR | FQ RECEPTOR | PHARMACOLOGY & PHARMACY | RATING-SCALE | Follow-Up Studies | Humans | Middle Aged | Male | Spiro Compounds - therapeutic use | Eye Movements - drug effects | Young Adult | Depression - drug therapy | Prefrontal Cortex - drug effects | Adult | Female | Chlordiazepoxide - pharmacology | Pyrans - therapeutic use | Disease Models, Animal | Receptors, Opioid - metabolism | Double-Blind Method | Anti-Anxiety Agents - pharmacology | Rats | Rats, Sprague-Dawley | Pregnancy | Animals | Narcotic Antagonists - therapeutic use | Adolescent | Prefrontal Cortex - metabolism | Aged | Mice | Index Medicus | Original
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5. Full Text The NK1 receptor antagonist L822429 reduces heroin reinforcement
by Barbier, Estelle and Vendruscolo, Leandro F and Schlosburg, Joel E and Edwards, Scott and Juergens, Nathan and Park, Paula E and Misra, Kaushik K and Cheng, Kejun and Rice, Kenner C and Schank, Jesse and Schulteis, Gery and Koob, George F and Heilig, Markus
Neuropsychopharmacology, ISSN 0893-133X, 05/2013, Volume 38, Issue 6, pp. 976 - 984
Genetic deletion of the neurokinin 1 receptor (NK1R) has been shown to decrease the reinforcing properties of opioids, but it is unknown whether... 
heroin | substance P | self-administration | neurokinin receptor | opioids | MORPHINE | PSYCHIATRY | BEHAVIOR | RATS | REWARD | NEUROSCIENCES | MICE LACKING | DRUG-ADDICTION | GENE-EXPRESSION | PHARMACOLOGY & PHARMACY | SUBSTANCE-P | STRESS | BRAIN | Rats, Wistar | Reinforcement (Psychology) | Rats | Male | Receptors, Neurokinin-1 - physiology | Behavior, Addictive - prevention & control | Motivation - drug effects | Heroin - antagonists & inhibitors | Self Administration | Animals | Motivation - physiology | Piperidines - pharmacology | Piperidines - therapeutic use | Receptors, Neurokinin-1 - metabolism | Behavior, Addictive - psychology | Heroin - administration & dosage | Index Medicus | animal models | addiction & substance abuse | neuropeptides | Original
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6. Full Text Neural and Behavioral Effects of a Novel Mu Opioid Receptor Antagonist in Binge-Eating Obese People
by Cambridge, Victoria C and Ziauddeen, Hisham and Nathan, Pradeep J and Subramaniam, Naresh and Dodds, Chris and Chamberlain, Samuel R and Koch, Annelize and Maltby, Kay and Skeggs, Andrew L and Napolitano, Antonella and Farooqi, I. Sadaf and Bullmore, Edward T and Fletcher, Paul C
Biological Psychiatry, ISSN 0006-3223, 2013, Volume 73, Issue 9, pp. 887 - 894
Background Binge eating is associated with obesity and has been conceptualized as “food addiction.” However, this view has received only inconsistent support... 
Psychiatry | fMRI | Binge eating | obesity | hedonics | motivation | opioid | ACTIVATION | MORPHINE | BRAIN DOPAMINE | TASTE HEDONICS | REWARD | NEUROSCIENCES | ADDICTION | NUCLEUS-ACCUMBENS | NEURONS | FOOD | HYPOTHALAMUS | Binge-Eating Disorder - complications | Binge-Eating Disorder - physiopathology | Double-Blind Method | Obesity - complications | Brain - physiopathology | Humans | Middle Aged | Male | Obesity - physiopathology | Receptors, Opioid, mu - antagonists & inhibitors | Feeding Behavior - drug effects | Brain - drug effects | Motivation - drug effects | Triazoles - pharmacology | Magnetic Resonance Imaging | Motivation - physiology | Functional Neuroimaging | Narcotic Antagonists - pharmacology | Adolescent | Brain Mapping | Adult | Female | Indans - pharmacology | Obesity | Neurosciences | Compulsive eating | Index Medicus | Archival Report
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7. Full Text Modulation of gastrointestinal function by MuDelta, a mixed mu opioid receptor agonist/mu opioid receptor antagonist
by Wade, PR and Palmer, JM and McKenney, S and Kenigs, V and Chevalier, K and Moore, BA and Mabus, JR and Saunders, PR and Wallace, NH and Schneider, CR and Kimball, ES and Breslin, HJ and He, W and Hornby, PJ
BRITISH JOURNAL OF PHARMACOLOGY, ISSN 0007-1188, 11/2012, Volume 167, Issue 5, pp. 1111 - 1125
BACKGROUND & PURPOSE Loperamide is a selective mu opioid receptor agonist acting locally in the gastrointestinal (GI) tract as an effective anti-diarrhoeal but... 
RAT | irritable bowel syndrome | DELTA | opioid | VISCERAL HYPERALGESIA | gastrointestinal secretion | KNOCKOUT MICE | ARRIVE GUIDELINES | MUSCLE-CELLS | INTESTINAL INFLAMMATION | visceral pain | IN-VIVO | motility | PHARMACOLOGY & PHARMACY | SYNDROME IBS | d opioid receptor | IRRITABLE-BOWEL-SYNDROME
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8. Full Text A Pharmacogenetic Determinant of Mu-Opioid Receptor Antagonist Effects on Alcohol Reward and Consumption: Evidence from Humanized Mice
by Bilbao, Ainhoa and Robinson, J. Elliott and Heilig, Markus and Malanga, C.J and Spanagel, Rainer and Sommer, Wolfgang H and Thorsell, Annika and Avdelningen för neuro- och inflammationsvetenskap and Medicinska fakulteten and Region Östergötland and Närsjukvården i centrala Östergötland and Linköpings universitet and Institutionen för klinisk och experimentell medicin and Psykiatriska kliniken
Biological Psychiatry, ISSN 0006-3223, 2015, Volume 77, Issue 10, pp. 850 - 858
Abstract Background It has been proposed that therapeutic responses to naltrexone in alcoholism are moderated by variation at the mu-opioid receptor gene locus... 
Psychiatry | Alcohol | Pharmacogenetics | Reward | Mouse | Mu-opioid receptor | Intracranial self-stimulation (ICSS) | FUNCTIONAL POLYMORPHISM | PSYCHIATRY | DEPENDENT PATIENTS | NALTREXONE RESPONSE | SINGLE-NUCLEOTIDE POLYMORPHISM | KNOCKOUT MICE | NEUROSCIENCES | NUCLEUS-ACCUMBENS | INTRACRANIAL SELF-STIMULATION | GENE OPRM1 | SUBJECTIVE RESPONSES | A118G POLYMORPHISM | Naltrexone - analogs & derivatives | Electric Stimulation | Ethanol | Humans | Mice, Inbred C57BL | Male | Mice, Transgenic | Receptors, Opioid, mu - agonists | Alcohol Drinking - genetics | Self Administration | Animals | Conditioning, Operant - drug effects | Mice | Receptors, Opioid, mu - genetics | Naltrexone - administration & dosage | Receptors, Opioid, mu - physiology | Medical colleges | Health aspects | Alcoholism | Analysis | Index Medicus | Basic Medicine | Farmakologi och toxikologi | Medical and Health Sciences | Pharmacology and Toxicology | Medicin och hälsovetenskap | Medicinska och farmaceutiska grundvetenskaper
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9. Full Text Antipruritic treatment with systemic mu-opioid receptor antagonists: A review
by Phan, NQ and Bernhard, JD and Luger, TA and Stander, S
JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY, ISSN 0190-9622, 10/2010, Volume 63, Issue 4, pp. 680 - 688
During the past two decades, systemic mu-opioid receptor antagonists (MORA) have been used in the treatment of various forms of chronic pruritus. In a number... 
pruritus | itch | OPIATE ANTAGONIST | INTRATHECAL MORPHINE | NALOXONE INFUSIONS | therapy | atopic dermatitis | CHRONIC CHOLESTASIS | INTRACTABLE PRURITUS | NALMEFENE THERAPY | DERMATOLOGY | opioid receptor antagonist | ATOPIC-DERMATITIS | DOUBLE-BLIND | UREMIC PRURITUS | sensory nerve fibers | ORAL NALTREXONE TREATMENT
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10. Full Text Delta-opioid receptor antagonist naltrindole reduces oxycodone addiction and constipation in mice
by Yang, Pao-Pao and Yeh, Teng-Kuang and Loh, Horace H and Law, Ping-Yee and Wang, Yun and Tao, Pao-Luh
European Journal of Pharmacology, ISSN 0014-2999, 06/2019, Volume 852, pp. 265 - 273
Oxycodone, a widely prescribed and very potent oral opioid analgesic agent, is highly addictive and has many side effects, including troublesome constipation.... 
Tolerance | Naltrindole | Conditioned place preference | Delta-opioid receptor | Oxycodone | Dependence | UNITED-STATES | DOPAMINE RELEASE | ANALGESIC ABUSE | MORPHINE | NUCLEUS-ACCUMBENS | GASTROINTESTINAL TRANSIT | PAIN | RELAPSE VULNERABILITY | PHARMACOLOGY & PHARMACY | Naltrexone - analogs & derivatives | Naltrexone - therapeutic use | Respiratory Insufficiency - complications | Opioid-Related Disorders - drug therapy | Opioid-Related Disorders - etiology | Mice, Inbred C57BL | Drug Tolerance | Male | Constipation - chemically induced | Naltrexone - pharmacology | Animals | Narcotic Antagonists - therapeutic use | Narcotic Antagonists - pharmacology | Receptors, Opioid, delta - antagonists & inhibitors | Constipation - drug therapy | Mice | Oxycodone - adverse effects | Analgesics - adverse effects | Opioid-Related Disorders - complications | Drug abuse | Liability (Law) | Constipation | Opioids | Index Medicus
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11. Full Text CGRP receptor antagonist activity of olcegepant depends on the signalling pathway measured
by Walker, Christopher S and Raddant, Ann C and Woolley, Michael J and Russo, Andrew F and Hay, Debbie L
Cephalalgia, ISSN 0333-1024, 3/2018, Volume 38, Issue 3, pp. 437 - 451
Background Calcitonin gene-related peptide (CGRP) is a neuropeptide that acts in the trigeminovascular system and is believed to play an important role in... 
trigeminal ganglia | calcitonin gene-related peptide (CGRP) | pain | CREB | migraine | bias | Amylin 1 (AMY | Amylin 1 (AMY1) | CONTROLLED-TRIAL | TRIGEMINAL GANGLION | AMYLIN RECEPTORS | TRIGEMINOVASCULAR SYSTEM | GENE-RELATED PEPTIDE | COUPLED RECEPTOR | NEUROSCIENCES | MU-OPIOID RECEPTOR | CLINICAL NEUROLOGY | CALCITONIN-RECEPTOR | INTERNATIONAL UNION | ACTIVITY-MODIFYING PROTEIN-1 | Calcitonin Gene-Related Peptide Receptor Antagonists - pharmacology | Receptors, Calcitonin Gene-Related Peptide - drug effects | Rats, Wistar | Dipeptides - pharmacology | Humans | Receptors, Islet Amyloid Polypeptide - antagonists & inhibitors | Cercopithecus aethiops | Rats | Trigeminal Ganglion - drug effects | Animals | Transfection | Signal Transduction - drug effects | Signal Transduction - physiology | Neurons - drug effects | Quinazolines - pharmacology | COS Cells | Index Medicus | amylin 1 (AMY1)
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12. Full Text Synthesis and Evaluation of C-11-LY2795050 as a kappa-Opioid Receptor Antagonist Radiotracer for PET Imaging
by Zheng, MQ and Nabulsi, N and Kim, SJ and Tomasi, G and Lin, SF and Mitch, C and Quimby, S and Barth, V and Rash, K and Masters, J and Navarro, A and Seest, E and Morris, ED and Carson, RE and Huang, YY
JOURNAL OF NUCLEAR MEDICINE, ISSN 0161-5505, 03/2013, Volume 54, Issue 3, pp. 455 - 463
Kappa-opioid receptors (KOR) are believed to be involved in the pathophysiology of depression, anxiety disorders, drug abuse, and alcoholism. To date, only 1... 
synthesis | kappa opioid receptor | IN-SITU HYBRIDIZATION | KNOCKOUT MICE | antagonist | radioligand | MESSENGER-RNA | CENTRAL-NERVOUS-SYSTEM | RAT-BRAIN | BINDING-SITES | VIVO BINDING | EXPRESSION | RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING | PET | OPIATE RECEPTORS
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13. Full Text New opioid receptor antagonist: Naltrexone-14-O-sulfate synthesis and pharmacology
by Zádor, Ferenc and Király, Kornél and Váradi, András and Balogh, Mihály and Fehér, Ágnes and Kocsis, Dóra and Erdei, Anna I and Lackó, Erzsébet and Zádori, Zoltán S and Hosztafi, Sándor and Noszál, Béla and Riba, Pál and Benyhe, Sándor and Fürst, Susanna and Al-Khrasani, Mahmoud
European Journal of Pharmacology, ISSN 0014-2999, 08/2017, Volume 809, pp. 111 - 121
Opioid antagonists, naloxone and naltrexone have long been used in clinical practice and research. In addition to their low selectivity, they easily pass... 
Isolated organs | Opioid receptor binding | Mouse tail-flick assay | Naltrexone-14-O-sulfate | MORPHINE | NALOXONE | ANTINOCICEPTION | DELTA-AGONIST | IN-VITRO | N-ALLYLNOROXYMORPHONE | PHARMACOLOGY & PHARMACY | INFLAMMATORY PAIN | NARCOTIC-ANTAGONISTS | RAT-BRAIN | EXPRESSION | Naltrexone - analogs & derivatives | Analgesics - pharmacology | Chemistry Techniques, Synthetic | Morphine - pharmacology | Rats, Wistar | Colon - drug effects | Narcotic Antagonists - chemical synthesis | Rats | Male | Naltrexone - chemical synthesis | Colon - metabolism | Naltrexone - pharmacology | Animals | Analgesics - chemical synthesis | Narcotic Antagonists - pharmacology | Vas Deferens - metabolism | Behavior, Animal - drug effects | Mice | Vas Deferens - drug effects | Receptors, Opioid - metabolism | Morphine | Pharmacology | Surface active agents | Naltrexone | Sulfates | Protein binding | Index Medicus
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14. Full Text The CGRP receptor antagonist BIBN4096BS peripherally alleviates inflammatory pain in rats
by Hirsch, Silke and Corradini, Laura and Just, Stefan and Arndt, Kirsten and Doods, Henri
Pain, ISSN 0304-3959, 05/2013, Volume 154, Issue 5, pp. 700 - 707
Calcitonin gene–related peptide (CGRP) antagonism reduces inflammatory pain. A peripheral site of action is assumed, as blockage of peripheral CGRP receptors...