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Biomedical subjects

R Nickander

Publications and source records attributed to R Nickander.

13 recordsLinked to original sources
PubMed1985

Picenadol.

Picenadol is a unique opioid mixed agonist-antagonist analgesic currently under clinical evaluation. Structurally, picenadol is a 4-phenylpiperidine derivative and a racemic mixture whose mixed agonist-antagonist properties are a consequence of the d-isomer being a potent opiate agonist, whereas the l-isomer is an opioid antagonist. In the mouse writhing and rat tail heat tests, the analgesic potency of picenadol is estimated to be 1/3 that of morphine. Picenadol itself has weak antagonist activity, whereas the antagonist potency of the l-isomer is approx. 1/10 that of nalorphine. Evaluation of picenadol's affinity for opioid receptors reveals that picenadol, unlike other mixed agonist-antagonists has high affinity for both the mu and delta receptors but a markedly lower affinity for the kappa receptor. Extensive pharmacological investigations show picenadol to have a low potential to produce opiate-like side effects, including a low liability for abuse and physical dependence.

Animals↗
PubMed1982

Comparative effects of benoxaprofen and other anti-inflammatory drugs on bone damage in the adjuvant arthritic rat.

Benoxaprofen, a new nonsteroidal anti-inflammatory agent recently marketed as an an antirheumatic drug, has been reported to suppress leucocyte migration into inflammatory sites, possibly by its reported inhibition of leukotriene synthesis. Benoxaprofen is also a weak to moderate inhibitor of prostaglandin synthesis. The effect of benoxaprofen was examined on adjuvant-induced arthritis in rats by radiographic assessment of bone damage. The effect of benoxaprofen was compared to other nonsteroidal anti-inflammatory agents, considered to act primarily by the inhibition of synthesis and/or release of prostaglandins. Drugs were administered from the 15th to the 30th day after induction of the adjuvant disease ('established adjuvant'). Radiographs of adjuvant rats showed extensive bone damage that was markedly suppressed by 30-40 mg/kg of benoxaprofen. Benoxaprofen exerted a dose-related inhibition of bone damage. There was less suppression of bone damage by comparable doses of phenylbutazone, oxyphenbutazone, ibuprofen, fenbufen, naproxen, tolectin and sulindac. Indomethacin, piroxicam and flurbiprofen were nearly as effective but only in doses that produced adverse effects or death in rats. Benoxaprofen may modify the progression of the experimental arthritic disease through a suppression of leucocyte migration.

Animals↗
PubMed1982

Radiographic studies of the effect of benoxaprofen on bone damage in the adjuvant arthritic rat.

The ability of benoxaprofen to suppress bone damage associated with adjuvant-induced arthritis in rats was studied radiographically over a 49-day period. Benoxaprofen was administered orally at a daily dose of 30 mg/kg. Treated and control groups of rats were examined at seven-day intervals from 14 through 49 days. Benoxaprofen showed significant suppression of bone damage at all time intervals. Benoxaprofen was compared in a radiographic bone study with other nonsteroidal anti-inflammatory agents. Benoxaprofen at doses of 10-40 mg/kg/day orally, administered from days 15 to 39 of the disease, was more effective in suppressing bone damage exhibiting toxic effects than other agents. This modification of the experimental disease process by benoxaprofen may be due in part to its reported ability to suppress monocyte migration into inflammatory sites.

Animals↗
PubMed1977

Propoxyphene and norpropoxyphene: pharmacologic and toxic effects in animals.

alpha-d-Propoxyphene and its principle metabolite, alpha-d-norpropoxyphene, were compared pharmacologically to establish their relative opioid profiles as defined by naloxone reversal. Propoxyphene exhibited opioid activity in the following tests: mouse abdominal constriction and rat tail heat analgesic tests, inhibition of the twitch of the guinea-pig ileum and acute lethality in rodents. Norpropoxyphene also showed opioid activity in the rat tail heat and guinea-pig ileum tests, but exhibited nonopioid activity in the mouse abdominal constriction and acute toxicity studies. Jumping in mice, precipitated by naloxone, suggests the following order for liability to produce physical dependence after repeated administration: morphine greater than codeine greater than propoxyphene greater than norpropoxyphene approximately saline. Propoxyphene and norpropoxyphene depressed axonal conduction in isolated peripheral nerve and were comparable in potency to standard local anesthetic agents. The nonopioid actions of norpropoxyphene might be due in part to its local anesthetic properties.

Analgesics, Opioid↗