Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Analgesics, Opioid: Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Receptors, Opioid, delta: A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.Opioid Peptides: The endogenous peptides with opiate-like activity. The three major classes currently recognized are the ENKEPHALINS, the DYNORPHINS, and the ENDORPHINS. Each of these families derives from different precursors, proenkephalin, prodynorphin, and PRO-OPIOMELANOCORTIN, respectively. There are also at least three classes of OPIOID RECEPTORS, but the peptide families do not map to the receptors in a simple way.Analgesics, Non-Narcotic: A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are not addictive. Many non-narcotic analgesics are offered as NONPRESCRIPTION DRUGS.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Morphine: The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.Pain: An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.Analgesia: Methods of PAIN relief that may be used with or in place of ANALGESICS.Pain Measurement: Scales, questionnaires, tests, and other methods used to assess pain severity and duration in patients or experimental animals to aid in diagnosis, therapy, and physiological studies.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.Opioid-Related Disorders: Disorders related or resulting from abuse or mis-use of opioids.Enkephalins: One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.Narcotics: Agents that induce NARCOSIS. Narcotics include agents that cause somnolence or induced sleep (STUPOR); natural or synthetic derivatives of OPIUM or MORPHINE or any substance that has such effects. They are potent inducers of ANALGESIA and OPIOID-RELATED DISORDERS.Pain, Postoperative: Pain during the period after surgery.Tramadol: A narcotic analgesic proposed for severe pain. It may be habituating.Immunoglobulin kappa-Chains: One of the types of light chains of the immunoglobulins with a molecular weight of approximately 22 kDa.Drug Tolerance: Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.Buprenorphine: A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.Dynorphins: A class of opioid peptides including dynorphin A, dynorphin B, and smaller fragments of these peptides. Dynorphins prefer kappa-opioid receptors (RECEPTORS, OPIOID, KAPPA) and have been shown to play a role as central nervous system transmitters.Endorphins: One of the three major groups of endogenous opioid peptides. They are large peptides derived from the PRO-OPIOMELANOCORTIN precursor. The known members of this group are alpha-, beta-, and gamma-endorphin. The term endorphin is also sometimes used to refer to all opioid peptides, but the narrower sense is used here; OPIOID PEPTIDES is used for the broader group.Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078)Benzeneacetamides: Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.Phenacetin: A phenylacetamide that was formerly used in ANALGESICS but nephropathy and METHEMOGLOBINEMIA led to its withdrawal from the market. (From Smith and Reynard, Textbook of Pharmacology,1991, p431)Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.Pain Threshold: Amount of stimulation required before the sensation of pain is experienced.Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.Morphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.Enkephalin, Leucine-2-Alanine: A delta-selective opioid (ANALGESICS, OPIOID). It can cause transient depression of mean arterial blood pressure and heart rate.Codeine: An opioid analgesic related to MORPHINE but with less potent analgesic properties and mild sedative effects. It also acts centrally to suppress cough.Injections, Spinal: Introduction of therapeutic agents into the spinal region using a needle and syringe.Diprenorphine: A narcotic antagonist similar in action to NALOXONE. It is used to remobilize animals after ETORPHINE neuroleptanalgesia and is considered a specific antagonist to etorphine.Hyperalgesia: An increased sensation of pain or discomfort produced by mimimally noxious stimuli due to damage to soft tissue containing NOCICEPTORS or injury to a peripheral nerve.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.beta-Endorphin: A 31-amino acid peptide that is the C-terminal fragment of BETA-LIPOTROPIN. It acts on OPIOID RECEPTORS and is an analgesic. Its first four amino acids at the N-terminal are identical to the tetrapeptide sequence of METHIONINE ENKEPHALIN and LEUCINE ENKEPHALIN.Anti-Inflammatory Agents, Non-Steroidal: Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions.They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects.Pentazocine: The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.PyrrolidinesPain Management: A form of therapy that employs a coordinated and interdisciplinary approach for easing the suffering and improving the quality of life of those experiencing pain.Benzomorphans: Morphine derivatives of the methanobenzazocine family that act as potent analgesics.Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3)Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.Pain, Intractable: Persistent pain that is refractory to some or all forms of treatment.Cyclazocine: An analgesic with mixed narcotic agonist-antagonist properties.Anesthetics, Local: Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate.Hydrocodone: Narcotic analgesic related to CODEINE, but more potent and more addicting by weight. It is used also as cough suppressant.Chronic Pain: Aching sensation that persists for more than a few months. It may or may not be associated with trauma or disease, and may persist after the initial injury has healed. Its localization, character, and timing are more vague than with acute pain.Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.Morphine Derivatives: Analogs or derivatives of morphine.Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)Double-Blind Method: A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.Dipyrone: A drug that has analgesic, anti-inflammatory, and antipyretic properties. It is the sodium sulfonate of AMINOPYRINE.Analgesia, Epidural: The relief of pain without loss of consciousness through the introduction of an analgesic agent into the epidural space of the vertebral canal. It is differentiated from ANESTHESIA, EPIDURAL which refers to the state of insensitivity to sensation.Analgesia, Patient-Controlled: Relief of PAIN, without loss of CONSCIOUSNESS, through ANALGESIC AGENTS administered by the patients. It has been used successfully to control POSTOPERATIVE PAIN, during OBSTETRIC LABOR, after BURNS, and in TERMINAL CARE. The choice of agent, dose, and lockout interval greatly influence effectiveness. The potential for overdose can be minimized by combining small bolus doses with a mandatory interval between successive doses (lockout interval).Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at kappa opioid receptors and an antagonist or partial agonist at mu opioid receptors.Bupivacaine: A widely used local anesthetic agent.Nociceptors: Peripheral AFFERENT NEURONS which are sensitive to injuries or pain, usually caused by extreme thermal exposures, mechanical forces, or other noxious stimuli. Their cell bodies reside in the DORSAL ROOT GANGLIA. Their peripheral terminals (NERVE ENDINGS) innervate target tissues and transduce noxious stimuli via axons to the CENTRAL NERVOUS SYSTEM.Oxycodone: A semisynthetic derivative of CODEINE.Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.Nociception: Sensing of noxious mechanical, thermal or chemical stimuli by NOCICEPTORS. It is the sensory component of visceral and tissue pain (NOCICEPTIVE PAIN).Substance Withdrawal Syndrome: Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.Prescription Drugs: Drugs that cannot be sold legally without a prescription.Ethylketocyclazocine: A kappa opioid receptor agonist. The compound has analgesic action and shows positive inotropic effects on the electrically stimulated left atrium. It also affects various types of behavior in mammals such as locomotion, rearing, and grooming.Heroin: A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed)Carrageenan: A water-soluble extractive mixture of sulfated polysaccharides from RED ALGAE. Chief sources are the Irish moss CHONDRUS CRISPUS (Carrageen), and Gigartina stellata. It is used as a stabilizer, for suspending COCOA in chocolate manufacture, and to clarify BEVERAGES.Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.Neuralgia: Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.Immunoglobulin Light Chains: Polypeptide chains, consisting of 211 to 217 amino acid residues and having a molecular weight of approximately 22 kDa. There are two major types of light chains, kappa and lambda. Two Ig light chains and two Ig heavy chains (IMMUNOGLOBULIN HEAVY CHAINS) make one immunoglobulin molecule.NF-kappa B: Ubiquitous, inducible, nuclear transcriptional activator that binds to enhancer elements in many different cell types and is activated by pathogenic stimuli. The NF-kappa B complex is a heterodimer composed of two DNA-binding subunits: NF-kappa B1 and relA.Meptazinol: A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain.Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed)Acupuncture Analgesia: Analgesia produced by the insertion of ACUPUNCTURE needles at certain ACUPUNCTURE POINTS on the body. This activates small myelinated nerve fibers in the muscle which transmit impulses to the spinal cord and then activate three centers - the spinal cord, midbrain and pituitary/hypothalamus - to produce analgesia.Diterpenes, Clerodane: A group of DITERPENES cyclized into 2-rings with a side-chain.Morphine Dependence: Strong dependence, both physiological and emotional, upon morphine.Gene Rearrangement, B-Lymphocyte, Light Chain: Ordered rearrangement of B-lymphocyte variable gene regions coding for the kappa or lambda IMMUNOGLOBULIN LIGHT CHAINS, thereby contributing to antibody diversity. It occurs during the second stage of differentiation of the IMMATURE B-LYMPHOCYTES.Drug Overdose: Accidental or deliberate use of a medication or street drug in excess of normal dosage.Nalorphine: A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.Spinal Cord: A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.Kidney Papillary Necrosis: A complication of kidney diseases characterized by cell death involving KIDNEY PAPILLA in the KIDNEY MEDULLA. Damages to this area may hinder the kidney to concentrate urine resulting in POLYURIA. Sloughed off necrotic tissue may block KIDNEY PELVIS or URETER. Necrosis of multiple renal papillae can lead to KIDNEY FAILURE.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Nociceptive Pain: Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN.Acute Pain: Intensely discomforting, distressful, or agonizing sensation associated with trauma or disease, with well-defined location, character, and timing.Periaqueductal Gray: Central gray matter surrounding the CEREBRAL AQUEDUCT in the MESENCEPHALON. Physiologically it is probably involved in RAGE reactions, the LORDOSIS REFLEX; FEEDING responses, bladder tonus, and pain.Nefopam: Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26)Prescription Drug Misuse: Improper use of drugs or medications outside the intended purpose, scope, or guidelines for use. This is in contrast to MEDICATION ADHERENCE, and distinguished from DRUG ABUSE, which is a deliberate or willful action.Cyclohexanecarboxylic AcidsImmunoglobulin lambda-Chains: One of the types of light chain subunits of the immunoglobulins with a molecular weight of approximately 22 kDa.Ibuprofen: A nonsteroidal anti-inflammatory agent with analgesic properties used in the therapy of rheumatism and arthritis.Behavior, Animal: The observable response an animal makes to any situation.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Opiate Substitution Treatment: Medical treatment for opioid dependence using a substitute opiate such as METHADONE or BUPRENORPHINE.I-kappa B Proteins: A family of inhibitory proteins which bind to the REL PROTO-ONCOGENE PROTEINS and modulate their activity. In the CYTOPLASM, I-kappa B proteins bind to the transcription factor NF-KAPPA B. Cell stimulation causes its dissociation and translocation of active NF-kappa B to the nucleus.Oligopeptides: Peptides composed of between two and twelve amino acids.Analgesia, Obstetrical: The elimination of PAIN, without the loss of CONSCIOUSNESS, during OBSTETRIC LABOR; OBSTETRIC DELIVERY; or the POSTPARTUM PERIOD, usually through the administration of ANALGESICS.Edema: Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.Reproducibility of Results: The statistical reproducibility of measurements (often in a clinical context), including the testing of instrumentation or techniques to obtain reproducible results. The concept includes reproducibility of physiological measurements, which may be used to develop rules to assess probability or prognosis, or response to a stimulus; reproducibility of occurrence of a condition; and reproducibility of experimental results.Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.Piperidines: A family of hexahydropyridines.Electroacupuncture: A form of acupuncture with electrical impulses passing through the needles to stimulate NERVE TISSUE. It can be used for ANALGESIA; ANESTHESIA; REHABILITATION; and treatment for diseases.Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Nerve Block: Interruption of NEURAL CONDUCTION in peripheral nerves or nerve trunks by the injection of a local anesthetic agent (e.g., LIDOCAINE; PHENOL; BOTULINUM TOXINS) to manage or treat pain.Injections, Intraventricular: Injections into the cerebral ventricles.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Heroin Dependence: Strong dependence, both physiological and emotional, upon heroin.Chronic Disease: Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care. (Dictionary of Health Services Management, 2d ed)Drug Prescriptions: Directions written for the obtaining and use of DRUGS.Treatment Outcome: Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.Formaldehyde: A highly reactive aldehyde gas formed by oxidation or incomplete combustion of hydrocarbons. In solution, it has a wide range of uses: in the manufacture of resins and textiles, as a disinfectant, and as a laboratory fixative or preservative. Formaldehyde solution (formalin) is considered a hazardous compound, and its vapor toxic. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p717)Nitrous Oxide: Nitrogen oxide (N2O). A colorless, odorless gas that is used as an anesthetic and analgesic. High concentrations cause a narcotic effect and may replace oxygen, causing death by asphyxia. It is also used as a food aerosol in the preparation of whipping cream.Immunoglobulin Variable Region: That region of the immunoglobulin molecule that varies in its amino acid sequence and composition, and comprises the binding site for a specific antigen. It is located at the N-terminus of the Fab fragment of the immunoglobulin. It includes hypervariable regions (COMPLEMENTARITY DETERMINING REGIONS) and framework regions.Drug and Narcotic Control: Control of drug and narcotic use by international agreement, or by institutional systems for handling prescribed drugs. This includes regulations concerned with the manufacturing, dispensing, approval (DRUG APPROVAL), and marketing of drugs.Hot Temperature: Presence of warmth or heat or a temperature notably higher than an accustomed norm.Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.Hypnotics and Sedatives: Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.Acetic Acid: Product of the oxidation of ethanol and of the destructive distillation of wood. It is used locally, occasionally internally, as a counterirritant and also as a reagent. (Stedman, 26th ed)Antipyretics: Drugs that are used to reduce body temperature in fever.Dexmedetomidine: A imidazole derivative that is an agonist of ADRENERGIC ALPHA-2 RECEPTORS. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound.Opiate Alkaloids: Alkaloids found in OPIUM from PAPAVER that induce analgesic and narcotic effects by action upon OPIOID RECEPTORS.Mice, Inbred ICRProspective Studies: Observation of a population for a sufficient number of persons over a sufficient number of years to generate incidence or mortality rates subsequent to the selection of the study group.Ketorolac Tromethamine: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Anti-Inflammatory Agents: Substances that reduce or suppress INFLAMMATION.Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.Base Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.Postoperative Nausea and Vomiting: Emesis and queasiness occurring after anesthesia.Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.Freund's Adjuvant: An antigen solution emulsified in mineral oil. The complete form is made up of killed, dried mycobacteria, usually M. tuberculosis, suspended in the oil phase. It is effective in stimulating cell-mediated immunity (IMMUNITY, CELLULAR) and potentiates the production of certain IMMUNOGLOBULINS in some animals. The incomplete form does not contain mycobacteria.Amines: A group of compounds derived from ammonia by substituting organic radicals for the hydrogens. (From Grant & Hackh's Chemical Dictionary, 5th ed)Amides: Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)Drug Combinations: Single preparations containing two or more active agents, for the purpose of their concurrent administration as a fixed dose mixture.Genes, Immunoglobulin: Genes encoding the different subunits of the IMMUNOGLOBULINS, for example the IMMUNOGLOBULIN LIGHT CHAIN GENES and the IMMUNOGLOBULIN HEAVY CHAIN GENES. The heavy and light immunoglobulin genes are present as gene segments in the germline cells. The completed genes are created when the segments are shuffled and assembled (B-LYMPHOCYTE GENE REARRANGEMENT) during B-LYMPHOCYTE maturation. The gene segments of the human light and heavy chain germline genes are symbolized V (variable), J (joining) and C (constant). The heavy chain germline genes have an additional segment D (diversity).Opium: The air-dried exudate from the unripe seed capsule of the opium poppy, Papaver somniferum, or its variant, P. album. It contains a number of alkaloids, but only a few - MORPHINE; CODEINE; and PAPAVERINE - have clinical significance. Opium has been used as an analgesic, antitussive, antidiarrheal, and antispasmodic.Disease Models, Animal: Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.Levallorphan: An opioid antagonist with properties similar to those of NALOXONE; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683)Analysis of Variance: A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.Drug Administration Schedule: Time schedule for administration of a drug in order to achieve optimum effectiveness and convenience.Self Medication: The self administration of medication not prescribed by a physician or in a manner not directed by a physician.Administration, Oral: The giving of drugs, chemicals, or other substances by mouth.Benzylidene Compounds: Compounds containing the PhCH= radical.Substance-Related Disorders: Disorders related to substance abuse.Anesthesia, Spinal: Procedure in which an anesthetic is injected directly into the spinal cord.Nonprescription Drugs: Medicines that can be sold legally without a DRUG PRESCRIPTION.Ligands: A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)Anesthetics, Dissociative: Intravenous anesthetics that induce a state of sedation, immobility, amnesia, and marked analgesia. Subjects may experience a strong feeling of dissociation from the environment. The condition produced is similar to NEUROLEPTANALGESIA, but is brought about by the administration of a single drug. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed)Plant Extracts: Concentrated pharmaceutical preparations of plants obtained by removing active constituents with a suitable solvent, which is evaporated away, and adjusting the residue to a prescribed standard.AzocinesPiroxicam: A cyclooxygenase inhibiting, non-steroidal anti-inflammatory agent (NSAID) that is well established in treating rheumatoid arthritis and osteoarthritis and used for musculoskeletal disorders, dysmenorrhea, and postoperative pain. Its long half-life enables it to be administered once daily.Amino Acid Sequence: The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.Transcutaneous Electric Nerve Stimulation: The use of specifically placed small electrodes to deliver electrical impulses across the SKIN to relieve PAIN. It is used less frequently to produce ANESTHESIA.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424)Dihydromorphine: A semisynthetic analgesic used in the study of narcotic receptors.Stereoisomerism: The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Adrenergic alpha-2 Receptor Agonists: Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.D-Ala(2),MePhe(4),Met(0)-ol-enkephalin: A stable synthetic analog of methionine enkephalin (ENKEPHALIN, METHIONINE). Actions are similar to those of methionine enkephalin. Its effects can be reversed by narcotic antagonists such as naloxone.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Transcription Factor RelB: A transcription factor that takes part in the NF-kappa-B complex by interacting with NF-KAPPA B P50 SUBUNIT or NF-KAPPA B P52 SUBUNIT. It regulates GENETIC TRANSCRIPTION that is involved in immune and inflammatory responses.Injections, Intravenous: Injections made into a vein for therapeutic or experimental purposes.Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)Pain Perception: The process by which PAIN is recognized and interpreted by the brain.ThiazinesPreanesthetic Medication: Drugs administered before an anesthetic to decrease a patient's anxiety and control the effects of that anesthetic.Proto-Oncogene Proteins c-rel: Cellular DNA-binding proteins encoded by the rel gene (GENES, REL). They are expressed predominately in hematopoietic cells and may play a role in lymphocyte differentiation. Rel frequently combines with other related proteins (NF-KAPPA B, I-kappa B, relA) to form heterodimers that regulate transcription. Rearrangement or overexpression of c-rel can cause tumorigenesis.Cannabinoids: Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.Prilocaine: A local anesthetic that is similar pharmacologically to LIDOCAINE. Currently, it is used most often for infiltration anesthesia in dentistry.Drug Synergism: The action of a drug in promoting or enhancing the effectiveness of another drug.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Posterior Horn Cells: Neurons in the SPINAL CORD DORSAL HORN whose cell bodies and processes are confined entirely to the CENTRAL NERVOUS SYSTEM. They receive collateral or direct terminations of dorsal root fibers. They send their axons either directly to ANTERIOR HORN CELLS or to the WHITE MATTER ascending and descending longitudinal fibers.Binding, Competitive: The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.Somatostatin: A 14-amino acid peptide named for its ability to inhibit pituitary GROWTH HORMONE release, also called somatotropin release-inhibiting factor. It is expressed in the central and peripheral nervous systems, the gut, and other organs. SRIF can also inhibit the release of THYROID-STIMULATING HORMONE; PROLACTIN; INSULIN; and GLUCAGON besides acting as a neurotransmitter and neuromodulator. In a number of species including humans, there is an additional form of somatostatin, SRIF-28 with a 14-amino acid extension at the N-terminal.Capsaicin: An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.Self Administration: Administration of a drug or chemical by the individual under the direction of a physician. It includes administration clinically or experimentally, by human or animal.Injections, Subcutaneous: Forceful administration under the skin of liquid medication, nutrient, or other fluid through a hollow needle piercing the skin.Drug Utilization: The utilization of drugs as reported in individual hospital studies, FDA studies, marketing, or consumption, etc. This includes drug stockpiling, and patient drug profiles.Drug Administration Routes: The various ways of administering a drug or other chemical to a site in a patient or animal from where the chemical is absorbed into the blood and delivered to the target tissue.Spiro Compounds: A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.Signal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Injections, Intra-Articular: Methods of delivering drugs into a joint space.CHO Cells: CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.Adrenergic alpha-Agonists: Drugs that selectively bind to and activate alpha adrenergic receptors.Anesthesia, General: Procedure in which patients are induced into an unconscious state through use of various medications so that they do not feel pain during surgery.Sensitivity and Specificity: Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)Conscious Sedation: A drug-induced depression of consciousness during which patients respond purposefully to verbal commands, either alone or accompanied by light tactile stimulation. No interventions are required to maintain a patent airway. (From: American Society of Anesthesiologists Practice Guidelines)Placebo Effect: An effect usually, but not necessarily, beneficial that is attributable to an expectation that the regimen will have an effect, i.e., the effect is due to the power of suggestion.
The four main opioid receptor types (delta, kappa, mu, and NOP) are found in vertebrates; hey are highly conserved in this ... The endogenous system of opioid receptors is well known for its analgesic potential in vertebrates. Enkephalins come in two ... nervous system and sensory receptors Has opioid receptors and shows reduced responses to noxious stimuli when given analgesics ... Naloxone is an μ-opioid receptor antagonist which, in vertebrates and some other invertebrates, negates the effects of opioids ...
Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays. Journal of ... It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor ... Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists. Life Sciences. 1987 Mar 30;40( ... Norbinaltorphimine: antagonist profile at kappa opioid receptors. European Journal of Pharmacology. 1987 Dec 15;144(3):405-8. ...
... effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors". Journal of Pharmacological Sciences. 98 (2 ... and a pure agonist at κ-opioid receptor and antagonist activity at the delta opioid receptor (δ) nalbuphine, κ-agonist/μ- ... Agonist-antagonist opioids that block delta while activating mu opioid receptors produce analgesia without the development of ... agonist at the kappa (κ) and sigma (σ) and has a weak antagonist action at the mu opioid receptor (μ). butorphanol, partial ...
Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays. Journal of ... Norbinaltorphimine: antagonist profile at kappa opioid receptors. European Journal of Pharmacology. 1987 Dec 15;144(3):405-8. ... Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists. Life Sciences. 1987 Mar 30;40( ... Suppression by nor-binaltorphimine of kappa opioid-mediated diuresis in rats. Journal of Pharmacology and Experimental ...
Tao YM, Li QL, Zhang CF, Xu XJ, Chen J, Ju YW, Chi ZQ, Long YQ, Liu JG (April 2008). "LPK-26, a novel kappa-opioid receptor ... LPK-26 is a potent and selective κ-opioid agonist, and has analgesic effects. ...
Particularly, mixed kappa receptor agonist mu receptor antagonist opioid analgesics can cause dose-related psychotomimesis. ... "Psychotomimesis mediated by kappa opiate receptors". Science. 233 (4765): 774-776. doi:10.1126/science.3016896. PMID 3016896. ... Pentazocine and butorphanol fall under this opioid class. There is evidence that cannabinoids are psychotomimetic, especially ... Musacchio JM (1990). "The psychotomimetic effects of opiates and the sigma receptor". Neuropsychopharmacology. 3 (3): 191-200. ...
At kappa-opioid receptors, it acts as an antagonist. Overall, it has a high efficacy as an analgesic. With regards to its ... and kappa-opioid receptors. Dezocine is a mixed agonist/antagonist of opioid receptors. It is related to other benzomorphans ... "Pharmacological profiles of opioid ligands at kappa opioid receptors". BMC Pharmacology. 6: 3. doi:10.1186/1471-2210-6-3. PMC ... Because decozine has mixed agonist/antagonist effects on mu-, delta-, and kappa-opioid receptors, it has a lowered dependence ...
... is a κ-opioid receptor agonist related to pentazocine. It has potent and long-lasting analgesic and diuretic ... Benzomorphan Dortch-Carnes J, Potter DE (2005). "Bremazocine: a kappa-opioid agonist with potent analgesic and other ...
Xin L, Geller EB, Adler MW (April 1997). "Body temperature and analgesic effects of selective mu and kappa opioid receptor ... the peptides do have some affinity for the μ-opioid receptor (MOR), δ-opioid receptor (DOR), and the N-methyl-D-aspartic acid ( ... Other studies have identified a role for dynorphin and kappa opioid receptor stimulation in neuropathic pain. This same group ... Beardsley PM, Howard JL, Shelton KL, Carroll FI (November 2005). "Differential effects of the novel kappa opioid receptor ...
... called the opioid receptor. Opioid Receptors, themselves, are divided into different subunits: kappa (KOR), delta (DOR), and mu ... "Putative Kappa Opioid Heteromers As Targets for Developing Analgesics Free of Adverse Effects." Journal of Medicinal Chemistry ... MOR) receptors. When INTA binds to the receptors, it is actually binding to a heteromer of the receptor. This means that it is ... This experimental drug candidate is under development as a κ-opioid receptor agonist for pain management with fewer adverse ...
Naloxone is an μ-opioid receptor antagonist which, in mammals, negates the analgesic effects of opioids. Both adult and five- ... All four of the main opioid receptor types (delta, kappa, mu, and NOP) are conserved in vertebrates, even in primitive jawless ... "Mu opioid receptor from the zebrafish exhibits functional characteristics as those of mammalian Mu opioid receptor". Zebrafish ... nervous system and sensory receptors Has opioid receptors and shows reduced responses to noxious stimuli when given analgesics ...
Barber A, Gottschlich R (1997). "Novel developments with selective, non-peptidic kappa-opioid receptor agonists". Expert Opin ... opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted ... a selective kappa opioid agonist: comparison with butorphanol and hydromorphone in humans". Psychopharmacology. 157 (2): 151-62 ... Enadoline is a drug which acts as a highly selective κ-opioid agonist. In human studies, it produced visual distortions and ...
August 2014). "Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol". ACS Med Chem Lett. 5 (8): 857-62 ... Pfeiffer A, Brantl V, Herz A, Emrich HM (August 1986). "Psychotomimesis mediated by kappa opiate receptors". Science. 233 (4765 ... it acts as a full agonist of the μ-opioid receptor (Ki = 0.7 nM; EC50 = 1.2 nM; IA = 104%), and δ-opioid receptor (Ki = 18 nM; ... June 2014). "Cebranopadol: a novel potent analgesic nociceptin/orphanin FQ peptide and opioid receptor agonist". J. Pharmacol. ...
... which are receptor antagonists with varying selectivity for mu and kappa opioid receptors. Naltrindole, a delta opioid receptor ... Incarvillateine isolated from Incarvillea sinensis has demonstrated significant analgesic activity when compared to the opiate ... These findings indicate that incarvillateine may possess opioidergic receptor activity, but it is worthy to note that some ... This suggests that incarvillateine's main mechanism of action is mediated through the adenosine receptor. Nakamura, M.; Chi, Y ...
It acts as a kappa opioid receptor agonist and is the first known compound acting on this receptor that is not an alkaloid. ... 2014). "The G-protein biased k-opioid receptor agonist RB-64 is analgesic with a unique spectrum of activities in vivo". J. ... None of these compounds have shown significant (sub-micromolar) affinity at the kappa-opioid receptor, and there is no evidence ... Scheerer JR; Lawrence JF; Wang GC; Evans DA (2007). "Asymmetric synthesis of salvinorin A, a potent kappa opioid receptor ...
... receptor antagonist LY293558 attenuates and reverses analgesic tolerance to morphine but not to delta or kappa opioids. Journal ... In vitro and in vivo antagonism of AMPA receptor activation by (3S, 4aR, 6R, 8aR)-6-[2-(1(2)H-tetrazole-5-yl) ethyl] ... The effect of the AMPA/kainate receptor antagonist LY293558 in a rat model of postoperative pain. Journal of Pain. 2006 Oct;7( ... In vitro and in vivo studies in rats with LY293558 suggest AMPA/kainate receptor blockade as a novel potential mechanism for ...
"A novel series of potent and selective agonists at the opioid kappa-receptor". European Journal of Pharmacology. 151 (3): 475-8 ... ICI-199,441 is a drug which acts as a potent and selective κ-opioid agonist, and has analgesic effects. It is a biased agonist ...
Ko MC, Husbands SM (January 2009). "Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and ... κ2-selective agonists may be useful for preventing the itching which is a common side effect of conventional opioid analgesic ... Naylor A, Judd DB, Lloyd JE, Scopes DI, Hayes AG, Birch PJ (July 1993). "A potent new class of kappa-receptor agonist: 4- ... Ho J, Mannes AJ, Dubner R, Caudle RM (April 1997). "Putative kappa-2 opioid agonists are antihyperalgesic in a rat model of ...
Analgesic and mechanistic evaluation of spiradoline, a potent kappa opioid. Journal of Pharmacology and Experimental ... A review of the properties of spiradoline: a potent and selective kappa-opioid receptor agonist. CNS Drug Reviews. 2003 Summer; ... PMID 2839665 Kunihara M, Ohyama M, Nakano M, Hayashi S. Analgesic activity of spiradoline mesylate (U-62,066E), a kappa opioid ... a kappa opioid receptor agonist. European Journal of Pharmacology. 1989 Jan 31;160(2):229-37. doi:10.1016/0014-2999(89)90495-0 ...
Zhang Z, Chen TY, Kirsch JR, Toung TJ, Traystman RJ, Koehler RC, Hurn PD, Bhardwaj A (December 2003). "Kappa-opioid receptor ... highly selective kappa opioid analgesics". Journal of Medicinal Chemistry. 34 (1): 397-403. doi:10.1021/jm00105a061. PMID ... Peart JN, Gross ER, Gross GJ (March 2004). "Effect of exogenous kappa-opioid receptor activation in rat model of myocardial ... "Neuroprotective kappa-opioid receptor agonist BRL 52537 attenuates ischemia-evoked nitric oxide production in vivo in rats". ...
Pharmacological profiles of opioid ligands at kappa opioid receptors. BMC Pharmacology. 2006 Jan 25;6:3. Shannon HE. ... Metazocine is an opioid analgesic related to pentazocine. While metazocine has significant analgesic effects, mediated through ... Activity of opioid ligands in cells expressing cloned mu opioid receptors. BMC Pharmacology. 2003 Jan 4;3:1. Gharagozlou P, ... use is limited by dysphoric and hallucinogenic effects which are most likely caused by activity at kappa opioid receptors ( ...
... with relatively low affinity for the delta opioid receptor and the kappa opioid receptor. In accordance with these studies, ... AP-237 (1-butyryl-4-cinnamylpiperazine) is an opioid analgesic drug that was widely used in China to treat pain in cancer ... Analgesic and tolerance studies with AP-237, a new analgesic. Arch Int Pharmacodyn Ther. 1975 Jan;213(1):41-57. PMID 1156018 ... subsequent studies have shown AP-237 and similar acyl piperazines to be potent and selective agonists of mu opioid receptor ( ...
The mixed agonists-antagonists drug class exerts their analgesic actions by agonistic activity at opioid kappa ("κ") receptors ... 2006) report that opioid μ-receptors and opioid κ-receptors are located in skin nerves and keratinocytes. Levy et al. (1989) ... Nalbuphine binds with high affinity to the μ-opioid receptor (Ki = 0.89 nM) and κ-opioid receptor (Ki = 2.2 nM), and has ... scale which quantitates the drug's ability to act both as an analgesic (via opioid κ-receptor agonism) as well as an μ-receptor ...
The three known and defined receptors are mu, kappa and delta, with many other receptors reported as well. These receptors are ... but because of the viability of rotating the patient between different opioid analgesics over time. Opioid rotation is ... See also: Opioid#Pharmacology The pharmacology of opioids involves the substance binding to opioid receptors in the nervous ... and opioid receptor down-regulation (internalization of membrane receptors). In opioid-induced hyperalgesia, sensitization of ...
... δ-opioid (delta) and κ-opioid (kappa) receptors. Agonist of the μ-opioid and δ-opioid receptors is largely responsible for the ... strong analgesic and is used clinically in the treatment of pain and also is an active metabolite of the analgesic opioid drug ... 216 Costantino CM, Gomes I, Stockton SD, Lim MP, Devi LA (2012). "Opioid receptor heteromers in analgesia". Expert Rev Mol Med ... is used in scientific research to study binding of the opioid receptors in the nervous system. Dihydromorphine is slightly ...
... opioid, and/or acetylcholine receptor signaling. NK1Rs are stimulated. In turn, a fairly complex reflex is triggered involving ... Azzolina A, Bongiovanni A, Lampiasi N (Dec 2003). "Substance P induces TNF-alpha and IL-6 production through NF kappa B in ... the reasons why NK1RAs have failed as efficacious analgesics in well-conducted clinical proof of concept studies have not yet ... ReceptorEdit. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).[8] It belongs to the ...
It acts at two opioid receptors - the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor ( ... Kappa agonists, Opioid receptor ligands, Drugs acting on the nervous system, Analgesic Categories. ‹ All Categories ... It acts as an antagonist of the μ-opioid receptor (MOR) and as an agonist of the κ-opioid receptor (KOR), and as a result, ... A potent opioid analgesic that was never clinically developed; the codeine analogue of the powerful opioid agonist analgesic ...
It acts at two opioid receptors - the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor ( ... Kappa agonists, Opioid receptor ligands, Drugs acting on the nervous system, Analgesic, Alkenes Categories. ‹ All Categories ... It is related to more well-known opioids such as buprenorphine, which is used as an analgesic and for the treatment of opioid ... is a mixed opioid agonist-antagonist with opioid antagonist and analgesic properties. It was introduced in 1954 and was used as ...
These findings could have implications for the treatment of pain with kappa opioid analgesics. The results may also have an ... PET imaging reveals sex differences in kappa opioid receptor availability in humans, in vivo.. Vijay A1, Wang S2, Worhunsky P1 ... In addition, sex differences have been observed in efficacy of treatment targeting kappa opioid receptors (KOR). Our goal in ... PET imaging reveals sex differences in kappa opioid receptor availability in humans, in vivo ...
Opioid Analgesics: Opioids (Mixed Agonist / Antagonist) may diminish the analgesic effect of Opioid Analgesics. Management: ... Buprenorphine exerts its analgesic effect via high-affinity binding to mu opiate receptors in the CNS; displays partial mu ... agonist and weak kappa antagonist activity. Due to it being a partial mu agonist, its analgesic effects plateau at higher doses ... Diuretics: Opioid Analgesics may enhance the adverse/toxic effect of Diuretics. Opioid Analgesics may diminish the therapeutic ...
The four main opioid receptor types (delta, kappa, mu, and NOP) are found in vertebrates; hey are highly conserved in this ... The endogenous system of opioid receptors is well known for its analgesic potential in vertebrates. Enkephalins come in two ... nervous system and sensory receptors Has opioid receptors and shows reduced responses to noxious stimuli when given analgesics ... Naloxone is an μ-opioid receptor antagonist which, in vertebrates and some other invertebrates, negates the effects of opioids ...
Bremazocine is a κ-opioid receptor agonist related to pentazocine. It has potent and long-lasting analgesic and diuretic ... Benzomorphan Dortch-Carnes J, Potter DE (2005). "Bremazocine: a kappa-opioid agonist with potent analgesic and other ...
... receptor agonists exhibit analgesic effects without activating reward pathways. In the search for nonaddictive opioid ... therapeutics and novel chemical tools to study physiological functions regulated by the KOP receptor, we screened in silico its ... Kappa-opioid (KOP) receptor agonists exhibit analgesic effects without activating reward pathways. In the search for ... Discovery of a novel selective kappa-opioid receptor agonist using crystal structure-based virtual screening J Chem Inf Model. ...
1988) Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays. J Pharmacol Exp ... micro-opioid receptor antagonist in CHO cells expressing the cloned human mu-opioid receptor. Synapse 64:280-288. ... 2011) Analgesic tone conferred by constitutively active mu opioid receptors in mice lacking beta-arrestin 2. Mol Pain 7:24. ... Endogenous opioids acting at the μ-opioid receptor (MOR) serve a pivotal function in reward processing and addictive behaviors ...
... selective kappa opioid receptor (KOPR) agonist with a short duration of action in vivo. Pharmacological properties of a C(2) ... Kappa opioid receptor (KOR) agonists produce analgesic and anti-pruritic effects, but their clinical application was limited by ... Salvinorin A: A Novel and Highly Selective Kappa-Opioid Receptor Agonist F Yan et al. Life Sci 75 (22), 2615-9. 2004. PMID ... A Review of Salvinorin Analogs and Their Kappa-Opioid Receptor Activity JJ Roach et al. Bioorg Med Chem Lett 28 (9), 1436-1445 ...
... exhibiting considerable selectivity in its actions for KOR over other opioid receptors. We previously reported that RGS12-null ... Kappa opioid receptor (KOR) agonists show promise in ameliorating disorders, such as addiction and chronic pain, but are ... The G protein-biased kappa-opioid receptor agonist RB-64 is analgesic with a unique spectrum of activities in vivo. J Pharm Exp ... Kappa opioid receptors on dopaminergic neurons are necessary for kappa-mediated place aversion. Neuropsychopharmacology. 2013; ...
Particularly, mixed kappa receptor agonist mu receptor antagonist opioid analgesics can cause dose-related psychotomimesis. ... "Psychotomimesis mediated by kappa opiate receptors". Science. 233 (4765): 774-776. doi:10.1126/science.3016896. PMID 3016896. ... Pentazocine and butorphanol fall under this opioid class. There is evidence that cannabinoids are psychotomimetic, especially ... Musacchio JM (1990). "The psychotomimetic effects of opiates and the sigma receptor". Neuropsychopharmacology. 3 (3): 191-200. ...
2015) The G protein-biased κ-opioid receptor agonist RB-64 is analgesic with a unique spectrum of activities in vivo. J ... µ-Opioid receptor (MOR), delta opioid receptor, and kappa opioid receptor (KOR) subtypes are expressed by peripheral ... kappa opioid receptor. MOR. µ-opioid receptor. nor-BNI. nor-binaltorphimine dihydrochloride. PBS. phosphate buffered saline. ... Functional Selectivity of Kappa Opioid Receptor Agonists in Peripheral Sensory Neurons. Raehannah J. Jamshidi, Blaine A. Jacobs ...
Available data indicate that opioid substitution treatment can successfully reduce rates of HIV transmission and that patients ... Receptors, Opioid, Kappa. A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind ... A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has ... Receptors, Opioid, Mu. A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in ...
It has high affinity, but only partial agonism at the micro-opioid receptor resulting in a ceiling analgesic effect. At higher ... buprenorphine potentiates antagonism at the kappa-opioid receptor. These properties make buprenorphine an effective maintenance ... Buprenorphine is a mixed opiate receptor agonist-antagonist growing in popularity as an office-based treatment for opioid- ... treatment for opioid-dependent patients. These same properties, however, can interfere with the management of acute pain in ...
Analgesics that target receptors in this pathway, called kappa-opioid receptors, have been reported to work only in women. ... The scientists tested the effects of the kappa-specific analgesic on mutant mice with an inactive variation of Mc1r analogous ... The researchers then tested a clinically used kappa analgesic, pentazocine, on male and female humans with several Mc1r ... "The Melanocortin-1 Receptor Gene Mediates Female-Specific Mechanisms of Analgesia in Mice and Humans," by Jeffrey S. Mogil, ...
Opioid Partial AgonistThe sublingual product is used predominantly for induction dosing followed by maintenance with ... exerts partial agonistic effects at the mu opioid receptor in the CNS and antagonistic effects at the kappa opioid receptor. ... Drugs & Diseases , Psychiatry , Opioid Abuse Q&A Which medications in the drug class Analgesics, Opioid Partial Agonist are ... Prescription opioid analgesics rapidly change the human brain. Pain. 2011 Aug. 152(8):1803-10. [Medline]. [Full Text]. ...
Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays. Journal of ... Norbinaltorphimine: antagonist profile at kappa opioid receptors. European Journal of Pharmacology. 1987 Dec 15;144(3):405-8. ... Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists. Life Sciences. 1987 Mar 30;40( ... Suppression by nor-binaltorphimine of kappa opioid-mediated diuresis in rats. Journal of Pharmacology and Experimental ...
Menthol: Provides pain relief via action at the kappa-opioid receptors located in the skin. ... Topical Analgesics. If you need a modest pain relief preparation without the disruptive nature of NSAIDs, topical analgesics ... Camphor: also provides pain relief via stimulation of the kappa-receptor as well as a mild anaesthetic action. ... Are All Topical Analgesics The Same?. Ingredient wise, they are the same for the most part. Excluding preservatives, the main ...
Menthol has local anesthetic and counterirritant qualities, and it also acts as a weak kappa (κ) opioid receptor agonist. ... Menthols analgesic properties are not fully understood, however they are mediated through a selective activation of κ-opioid ... Menthol acts to chemically trigger the cold-sensitive TRPM-8 receptors in the skin - responsible for the well-known cooling ... This is a topical patch consisting of the topical analgesic, menthol, and the local anesthetic, lidocaine. ...
... with or without analgesics, to induce a state that allows the patient to tolerate unpleasant procedures while maintaining ... The analgesic effect occurs at the mu opioid receptor.. Other opioid receptors (eg, kappa, delta) have been implicated in other ... Opioid analgesics. Opioid analgesic agents are frequently used to control pain. They may be given either alone or in ... Whenever opioid analgesics are used, a reversal agent should be readily available. Naloxone is an opioid reversal agent that ...
1988) Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays. J Pharmacol Exp ... κ opioid receptors. In addition, a tonically active (∼) inhibitory mechanism mediated by μ opioid receptors regulates bladder ... μ opioid receptor inhibition by activating a κ opioid receptor mechanism and in turn decreases bladder capacity. ... Opioid Receptors in Tibial Inhibition of Bladder. Zhaocun Zhang, Richard C. Slater, Matthew C. Ferroni, Brian T. Kadow, Timothy ...
1) Kappa opioid receptor (KOR) agonists are dysphoric. (See Land et al, 2008; Pfeiffer et al., 1986) Ive listened to some ... yet does not induce receptor regulation. Thus, it or something like it may end up being a potent analgesic without the problems ... Really great post! As someone who has spent their post-doc actively investigating the Kappa opioid receptor I find the ban in ... Several large pharmaceutical companies have Kappa-opioid receptor projects ongoing for using KOR as a target for the above ...
They can be divided into 3 classes: Naturally occurring opioids: The following 6 opium alkaloids occur naturally: morphine, ... Types of opioids Opioids are defined by their ability to bind to and influence opiate receptors on cell membranes. ... exerts partial agonistic effects at the mu opioid receptor in the CNS and antagonistic effects at the kappa opioid receptor. ... Opioid analgesics. Class Summary. Two uses for opioid analgesics are as follows: (1) Oral substitution therapy or maintenance ...
The MOR is the target of opioid drugs like morphine and is an important mechanism for pain regulation in the body. The research ... Researchers found initial confirmation that a novel scaffold protein previously unassociated with the mu opioid receptor (MOR) ... For example, activation of the kappa opioid receptor (KOR) signaling cascades for analgesic purposes has been limited because ... Streicher said, this approach has been limited so far, because the signaling complex and regulators of opioid receptors have ...
A kappa opioid receptor agonist. The compound has analgesic action and shows positive inotropic effects on the electrically ...
  • These drugs (such as rofecoxib , celecoxib , and etoricoxib ) are equally effective analgesics when compared with NSAIDs, but cause less gastrointestinal hemorrhage in particular. (wikipedia.org)
  • In one such effort, NIDA-funded researchers recently tested a combination of the prescription analgesic oxycodone and nalfurafine, which is used in Japan to treat itching associated with hemodialysis and chronic liver disease. (drugabuse.gov)
  • Using time-series analysis, we determined whether the addition of long-acting oxycodone to the provincial drug formulary in January 2000 was associated with an increase in opioid-related mortality. (cmaj.ca)
  • We performed a study to determine whether opioid-related mortality increased following the introduction of long-acting oxycodone. (cmaj.ca)
  • There are inpatient facilities and a few, specialized, licensed, outpatient, drug treatment programs that provide opioid detoxification using methadone. (medscape.com)
  • Methadone is a very good medication for opioid use disorders. (painweek.org)
  • Lots of people use methadone as a primary analgesic because it has a long half-life and you don't build as much tolerance. (painweek.org)
  • 6 Lastly, these programs should identify patients with opioid use disorders and engage them in treatment. (woundsresearch.com)