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At least 217 records · Page 12Linked to original sources
PubMed1993

NS-398, a novel non-steroidal anti-inflammatory drug with potent analgesic and antipyretic effects, which causes minimal stomach lesions.

1. NS-398 (N-[2-cyclohexyloxy-4-nitrophenyl] methanesulfonamide) is a new non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic effects. 2. The anti-inflammatory potency of NS-398 in rat carrageenin-induced edema was as potent as that of indomethacin and 8 times more potent than diclofenac. In rat adjuvant arthritis, NS-398 showed a therapeutic effect comparable to that seen with loxoprofen but less than that seen with indomethacin and diclofenac. 3. The analgesic potency of NS-398 in rat adjuvant arthritic pain was much the same as that of indomethacin, and was about 3-5 times higher than that of diclofenac and loxoprofen. In the Randall-Selitto method in rats, NS-398 was 2-7 times as potent as loxoprofen, diclofenac and indomethacin. In acetic acid-induced writhing in mice, NS-398 was equipotent to indomethacin and diclofenac. 4. In LPS-induced fever in rats, NS-398 was 1.5-4.5 times as potent as loxoprofen and indomethacin, but less potent than diclofenac. 5. NS-398 produced little gastric ulceration in doses of up to 1000 mg/kg, while reference drugs produced distinct stomach lesions in doses of 10-30 mg/kg. 6. NS-398 inhibited prostaglandin (PG) endoperoxide synthase from sheep seminal vesicle microsomes less potent than that of ibuprofen.

Animals↗
PubMed1969

The pharmacology of fenclozic acid (2-(4-chlorophenyl)-thiazol-4-ylacetic acid; I.C.I. 54,450; 'Myalex'); a new compound with anti-inflammatory, analgesic and antipyretic activityl.

1. Fenclozic acid (2-(4-chlorophenyl)thiazol-4-ylacetic acid; I.C.I. 54,450; "Myalex") is one representative of a new class of compounds with antiinflammatory, analgesic and antipyretic properties as evidenced by its activity in a variety of tests in rats, mice and guinea-pigs.2. In tests of short duration the potency of fenclozic acid is similar to that of phenylbutazone.3. In tests of longer duration fenclozic acid is more potent than phenylbutazone.4. The activity of fenclozic acid is not mediated by stimulation of the adrenals and the compound is devoid of corticosteroid-like activity.

Adrenal Cortex Hormones↗
PubMed1975

[Anti-inflammatory, analgesic and antipyretic actions of 1-(m-chlorophenyl)-3-N, N-dimethylcarbamoyl-5-methoxypyrazole (PZ-177)].

We have reported that PZ-177 was found to have potent inhibitory activity on acute inflammatory edema. In this paper, the anti-inflammatory, analgesic and antipyretic properties of PZ-177 were assessed by a battery of standard tests. PZ-177 inhibited the increased vascular permeability induced by histamine, xylene and acetic acid. The activity was the same as the anti-edematous one and was more potent than that of mepirizole. PZ-177 did not inhibit ultraviolet erythema in guinea pigs, proliferation of granulation tissue in cotton pellet and granuloma pouch tests of rats and adjuvant arthritis in rats. Wound healing was not prolonged and the agent was weak in ulcerogenic action. PZ-177 did not affect heat denaturation of bovine serum albumin at pH 5.3, but inhibited hyperthermic hemolysis at pH 7.4 and exerted a stabilizing effect on biological membranes. This is considered to be one of the mechanisms of action. When analgesic action was tested by the writhing and Haffner's methods in mice, the compound revealed a more potent activity than did mepirizole and aminopyrine. Utilizing the Randall-Selitto's analgesic method in rats, a significant rise in pain threshold was obtained only at the inflamed foot. The antipyretic action was less than aminopyrine in febrile rabbits. From the above results, PZ-177 may be classified as a potent analgesic and anti-inflammatory agent but has no effect on proliferation of granulation tissue and chronic inflammatory disease.

Analgesics↗
PubMedDate not supplied

[Anti-inflammatory, analgesic and antipyretic activity of pyrimidant].

In experiments on rats with different models of pathology it was demonstrated that a new non-steroidal anti-inflammatory drug pyrimidant exerts pronounced anti-inflammatory, analgesic and antipyretic effects. In some cases its activity exceeds that of indomethacin, brufen, butadione, mefenamic acid, sodium salicylate.

Animals↗
PubMed1975

Some biological properties of flurbiprofen, an anti-inflammatory, analgesic and antipyretic agent.

2-(2-Fluoro-4-biphenyl)propionic acid (flurbiprofen) possesses peripheral analgesic, anti-inflammatory and antipyretic properties. It does not possess glucocorticoid or adrenocortical-stimulating properties. It is a highly potent agent which in acute pharmacological test systems produced a significant pharmacological effect in single oral doses varying from 0.04 to 0.47 mg/kg. The peak plasma concentrations attained after these doses were generally of the order of 1 to 3 mug/ml. Doses of 0.33 mg/kg/day, which gave peak plasma concentrations of 0.6 mug/ml, produced a significant inhibition of rat adjuvant arthritis, both developing and established. The very shallow dose-response curves for flurbiprofen compared with acetylsalicylic acid, especially in the mouse and the rat test systems, are not due to an unreliable or abnormal absorption, which suggests that in these species the mode of action of flurbiprofen is not identical with that of acetylsalicylic acid.

Adrenalectomy↗
PubMed1988

Antiinflammatory, analgesic, and antipyretic activities of methyl 7-butyl-4,5,6,7-tetrahydro-3-methylamino-4,6-dioxo-5-propyl-2H-pyrazol o[3, 4-d]pyrimidine-2-carboxylate (AA-2379), a novel non-acidic agent.

The antiinflammatory, analgesic, and antipyretic activities of methyl 7-butyl-4,5,6,7-tetrahydro-3-methylamino-4,6-dioxo-5-propyl-2H-pyrazolo[ 3, 4-d]pyrimidine-2-carboxylate (AA-2379), a novel non-acidic agent, were examined. 1. AA-2379 had a potent antiinflammatory activity; 3-25 mg/kg, p.o. of the compound inhibited rat carrageenin-, bradykinin-, trypsin-, formalin-, dextran-, and nystatin-induced paw edema; mouse traumatic edema; and rat croton oil pouch inflammation by about 30%. The compound at 25-50 mg/kg, p.o. also inhibited the vascular permeability induced by histamine, serotonin, and bradykinin. 2. AA-2379 had an analgesic activity; the ID50 values in mouse phenylquinone-induced writhing were 10.1 mg/kg, p.o. and the compound at 12.5 mg/kg, p.o. inhibited dog urate arthritis. 3. AA-2379 at 3-10 mg/kg, p.o. showed antipyretic activity in febrile rats and rabbits. 4. AA-2379, at 500 mg/kg, p.o. was not ulcerogenic in rats. 5. These data show that AA-2379 is more active than non-acidic antiinflammatory agents, such as tiaramide and aminopyrine.

Animals↗
PubMed1985

[Anilides with analgesic and antipyretic activity].

Several trimethylcyclopentyl and trimethylcyclopentenyl acetanilides, mono- and di-substituted on the aromatic nucleus as well as the corresponding acyl derivatives from aniline it self and corresponding phenylacetanilides, were prepared and tested as analgesics and antipyretics. Several compounds exhibit considerable activity in some cases superior to that of acetanilide.

Anilides↗
PubMed1982

[Anti-inflammatory, analgesic and antipyretic activities of alpha-(p-thenoylphenyl)-propionic acid (TN-762) (author's transl)].

We reported in our previous paper that TN-762, a potent inhibitor of prostaglandin biosynthesis, has marked inhibitory activity on acute experimental inflammation. In this paper, the anti-inflammatory, analgesic, and antipyretic activities of TN-762 were assessed in animal models, and compared with those of indomethacin, ketoprofen and ibuprofen. TN-762 inhibited the sustained paw edema induced by mustard in rats during administration for 3 days, but after final administration, the inhibitory activity was decreased rapidly and was less then that of ketoprofen and indomethacin. TN-762 also inhibited the proliferation of granuloma induced by means of cotton pellet and granuloma pouch methods, and the adjuvant arthritis in rats. The inhibitory activity of the compound on inflammatory proliferation was more potent than that of ibuprofen, but slightly less than that of ketoprofen and less than about 1/10 times that of indomethacin. Indomethacin markedly inhibited the body weight gain at a high dose, while TN-762 did not affect it. Therefore, TN-762 was proven to have an inhibitory effect on subacute and chronic inflammation at low doses without toxic effects, but the compound appeared to have a less of an inhibitory effect on secondary or late stages of inflammation than on primary stage inflammation. TN-762 inhibited the acute paw edema induced by nystatin, and the inhibitory activity was the same as that of ketoprofen and indomethacin. The pathogenesis of nystatin edema has been considered to be due to lysosomal labilization. This result suggests that TN-762 has a potent membrane stabilizing action which is considered to be one of the necessary mechanisms in anti-inflammatory action. On the other hand, TN-762 showed the same potent analgesic effect as ketoprofen and indomethacin as observed by the acetic acid writhing and modified Haffner's methods in mice and by the Randall-Selitto's method in rats. However the antipyretic effect of TN-762 was significantly less than that of ketoprofen and indomethacin.

Analgesics↗
PubMed1975

[Pharmacological studies of 2-(5H-(1)benzopyrano(2,3-b)pyridin-7-yl)propionic acid (Y-8004). (I) Anti-inflammatory, analgesic and antipyretic actions].

A newly synthesized anti-inflammatory agent, Y-8004 demonstrated a greater inhibition than did indomethacin (IM). on inflammatory response such as ultraviolet erythema in guinea pigs, carrageenin edema, evans blue and carrageenin-induced pleuritis and acetic acid-induced peritonitis in rats. On the other hand, the inhibition of Y-8004 was to the same extent as IM regarding granuloma formation around cotton pellet and the development of adjuvant arthritis in rats, however, Y-8004 was only half as effective as IM regarding exudation in granuloma pouch. In addition, the agent was effective in alleviating established adjuvant arthritis, the anti-inflammatory activity was not mediated by stimulation of the adrenals, and glucocorticoid-like activity could not be demonstrated. Furthermore, analgesic and antipyretic activities were to the degree as seen with IM, and the analgesic property of Y-8004 was considered to be peripheral as is the case with IM. The ulcerogenic activity of Y-8004 was observed to be mainly in the jejunum and ileum of the rat, but compared to IM, there were considerable differences between the ulcerogenic and the effective doses. As Y-8004 has a wider therapeutic margin than IM, this non-steroidal anti-inflammatory agent should be quite applicable for clinical purposes.

Adrenal Cortex↗
PubMed1978

Aspirin and acetaminophen: a comparative view of their antipyretic and analgesic activity.

Aspirin and acetaminophen have excellent and essentially similar antipyretic activity. For the child, lowering of temperature will be indicated for excessively high temperature and when there is a history of febrile seizures. Specific clinical contraindications will often dictate the selection of one drug over the other. Aspirin has some advantage over acetaminophen for analgesia. The need for either drug for analgesia in the pediatric patient, however, will be infrequent; when required, a drug with greater analgesic activity than either aspirin or acetaminophen may be indicated.

Acetaminophen↗