Advertisement

Topics

Antinociceptive effects and toxicity of morphine-6-O-sulfate sodium salt in rat models of pain.

Summary of "Antinociceptive effects and toxicity of morphine-6-O-sulfate sodium salt in rat models of pain."

Mu-opioids (i.e. morphine, oxycodone, hydrocodone) are considered to be the primary drugs for treatment of moderate to severe acute, chronic and cancer pain. Despite their analgesic effectiveness they have several clinically significant side-effects (cognitive, motor, respiratory, cardiovascular, gastrointestinal). They also have a limited spectrum of action, being more effective for nociceptive than neuropathic pain. In an effort to identify other opioid analgesics with greater effectiveness in mixed pain states and with a better side-effect profile compared to the classical mu-opioid agonist, morphine, a relatively little-known morphine derivative, morphine-6-O-sulfate, was characterized using a range of well-established rodent pain models. The present data demonstrated that morphine-6-O-sulfate was efficacious after several routes of administration, including neuroaxial (intrathecal), parenteral (intraperitoneal) and oral in the rat. It showed potent, dose-related, analgesic activities against acute nociceptive pain (the tail flick test), neuropathic pain (chronic constriction nerve injury hyperalgesia and allodynia) and inflammatory pain (formalin test). It had a good separation based on dose (at least 10-fold) between side-effects (incoordination, hypolocomotion, inhibition of gastrointestinal motility) and analgesia in all models of pain tested. In addition, morphine-6-O-sulfate had a more favorable potency ratio for delay of gastrointestinal transit and analgesia when compared to morphine. These preclinical findings suggest that morphine-6-O-sulfate is a potential candidate for development as a novel opioid for management of nociceptive, neuropathic and mixed pain states.

Affiliation

Anesthesiology, College of Medicine, University of Kentucky, 800 Rose Street, Lexington, KY 40536-0293, USA; Pharmaceutical Science, College of Pharmacy, University of Kentucky, 725 Rose Street, Lexington, KY 40536-0082, USA.

Journal Details

This article was published in the following journal.

Name: European journal of pharmacology
ISSN: 1879-0712
Pages:

Links

DeepDyve research library

PubMed Articles [24160 Associated PubMed Articles listed on BioPortfolio]

The Effect of Sodium Sulfate, Ammonium Chloride, Ammonium Nitrate and Salt Mixtures on Aqueous Phase Partitioning of Organic Compounds.

Dissolved inorganic salt(s) influence the partitioning of organic compounds into the aqueous phase. This influence is especially significant in atmospheric aerosol, which usually contains large amount...

Effect of estrogen on morphine- and oxycodone-induced antinociception in a female femur bone cancer pain model.

Although estrous cycle has been reported to influence antiociceptive effect of morphine in several pain conditions, its effect on cancer pain is not well established. We investigated the effect of est...

Relative Contribution of the Dorsal Raphe Nucleus and Ventrolateral Periaqueductal Gray to Morphine Antinociception and Tolerance in the Rat.

The dorsal raphe nucleus (DRN) is embedded in the ventral part of the caudal periaqueductal gray (PAG). Electrical or chemical activation of neurons throughout this region produces antinociception. Th...

CB1 Cannabinoid Agonist (WIN55,212-2) Within the Basolateral Amygdala Induced Sensitization to Morphine and Increased the Level of μ-Opioid Receptor and c-fos in the Nucleus Accumbens.

The basolateral amygdala (BLA) is rich of CB1 cannabinoid receptors (CB1R) and has reciprocal connections with the nucleus accumbens (NAc) which is involved in opioid sensitization. In this study, eff...

Effect of sodium salt on anaerobic digestion of kitchen waste.

The effect of different sodium salt concentration on anaerobic digestion of kitchen waste was investigated. The methane production performance, the corresponding methane production model and sodium sa...

Clinical Trials [5207 Associated Clinical Trials listed on BioPortfolio]

Effect of Solar Salt Diet in Elderly Hypertensive Patients

High sodium intake causes hypertension. Various efforts for reducing salt consumption are proceeding all over the world. Solar salt contains reduced sodium and abundant mineral, such as ca...

Bioequivalency Study of Morphine Sulfate Injection, Solution and Tablet Under Fasted Conditions

Determine the pharmacokinetics and optimize study design for subsequent studies with morphine sulfate tablets and solution.

Dose Proportionality and Food Effect of Morphine Sulfate

Establish the dose proportionality of the 15 mg and 30 mg morphine sulfate tablets and to examine the effect of food on absorption from the 30 mg tablet.

Comparative Evaluation of the Effect on Blood Pressure of an Equivalent Content of Sodium in the Form of Bicarbonate of Sodium and in the Form of Sodium Chloride, on "Sensitive Sodium" Subjects

Many large-scale epidemiological studies have established a link between the average consumption of table salt (sodium chloride) and blood pressure. In France a survey conducted in 2001 sh...

Steady State Study of Codeine Sulfate

Study to characterize the steady-state pharmacokinetics of codeine and its metabolites morphine, morphine-3-glucuronide (M3G), and morphine-6-glucuronide (M6G) after oral administration of...

Medical and Biotech [MESH] Definitions

A pharmaceutical preparation containing a mixture of water-soluble, conjugated estrogens derived wholly or in part from URINE of pregnant mares or synthetically from ESTRONE and EQUILIN. It contains a sodium-salt mixture of estrone sulfate (52-62%) and equilin sulfate (22-30%) with a total of the two between 80-88%. Other concomitant conjugates include 17-alpha-dihydroequilin, 17-alpha-estradiol, and 17-beta-dihydroequilin. The potency of the preparation is expressed in terms of an equivalent quantity of sodium estrone sulfate.

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.

The trihydrate sodium salt of acetic acid, which is used as a source of sodium ions in solutions for dialysis and as a systemic and urinary alkalizer, diuretic, and expectorant.

A sulfate salt of copper. It is a potent emetic and is used as an antidote for poisoning by phosphorus. It also can be used to prevent the growth of algae.

A bile salt formed in the liver by conjugation of deoxycholate with taurine, usually as the sodium salt. It is used as a cholagogue and choleretic, also industrially as a fat emulsifier.

Quick Search
Advertisement
 


DeepDyve research library

Relevant Topics

Nutrition
Within medicine, nutrition (the study of food and the effect of its components on the body) has many different roles. Appropriate nutrition can help prevent certain diseases, or treat others. In critically ill patients, artificial feeding by tubes need t...

Pain
Pain is defined by the International Association for the Study of Pain as “an unpleasant sensory and emotional experience associated with actual or potential tissue damage or described in terms of such damage”. Some illnesses can be excruci...

Head and neck cancers
Cancer can occur in any of the tissues or organs in the head and neck. There are over 30 different places that cancer can develop in the head and neck area. Mouth cancers (oral cancers)  - Mouth cancer can develop on the lip, the tongue, the floor...


Searches Linking to this Article