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At least 19 recordsLinked to original sources
PubMed1985

Substituted 5H-dibenz[b,g]-1,4-oxazocines and related amino acids with antiinflammatory activity.

During an investigation of the antiinflammatory properties of a number of tetracyclic derivatives of 6,8-dichlorodibenz[b,f]oxepin-10(11H)-one, the ring-expanded 1,3-dichloro-5H-dibenz[b,g]-1,4-oxazocine (9) was prepared and found to be considerable pharmacological interest. It was subsequently found that the corresponding ring-opened amino acid 66, a close analogue of the antiinflammatory agent fenclofenac, also possessed significant antiinflammatory activity, superior both to the dibenzoxazocine and to fenclofenac. These findings prompted extensive synthetic programs in both areas, and a number of derivatives in the amino acid series showed potencies considerably in excess of the standard compound. These phenylacetic acids, however, were significantly more ulcerogenic than fenclofenac whereas the corresponding dibenzoxazocines showed few signs of ulcerogenicity at doses up to 1 g/kg.

Animals↗
PubMedDate not supplied

Investigations of anthelminthic activity and synthesis of new derivatives of perhydroazepine, perhydro-1,4-diazepine, perhydro-1,4-oxazepine and perhydro-1,5-oxazocine.

Anthelminthic activity of new esters of 3,4,5-trimethoxybenzoic acid containing rests of the title heterocyclic amines has been determined. 3-(Perhydroazepinyl)-propyl ester 6 acts on enchytraeids in vitro 56-fold stronger than piperazine adipate, 2-(perhydroazepinyl)-ethyl ester 5 is the most effective in a therapy of mice infested with nematodes.

Animals↗
PubMedDate not supplied

Investigation of the adducts formed by reaction of malondialdehyde with adenosine.

Malondialdehyde (MDA) forms oligomeric adducts with DNA bases. It has been proposed that the 2:1 MDA-guanosine (M2G) and 3:1 MDA-adenosine (M3A) adducts result from sequential addition of MDA molecules to the nucleoside base. Reaction of 1:1 MDA-guanosine (M1G) and 1:1 MDA-adenosine (M1A) adducts with MDA does not produce the multimeric adducts. This suggests they arise by reaction of the nucleoside bases with oligomers of MDA. If so, the proposed structure for M3A is inconsistent with the addition of an MDA trimer to adenosine. Therefore, we investigated the structure of this molecule. Two-dimensional double quantum filtered COSY and hetero-COSY NMR experiments were performed, and a series of insensitive nuclei assignment by polarization transfer (INAPT) NMR spectra were also recorded. The results of these experiments revealed the presence of a propano group and two alpha,beta-unsaturated aldehydes. The UV spectrum of M3A displayed a maximum at 326 nm, similar to that of N6-[3-oxo-1(E)-propenyl]adenosine (M1A). The adducts were reduced with sodium borohydride for comparison of the UV and NMR spectra. On the basis of our results, a new structure for M3A is proposed which is tentatively named 6(5*,7*-diformyl-2*H-3*,6*-dihydro-2*,6*-methano-1*,3*-oxazocin -3*-yl)-9-beta-D-ribofuranosylpurine.

Adenosine↗
PubMed1988

Assessment of the analgesic efficacy of nefopam hydrochloride after upper abdominal surgery: a study using patient controlled analgesia.

A randomized, double-blind, placebo-controlled study was performed to assess the analgesic efficacy of intramuscular nefopam hydrochloride after upper abdominal surgery. Patients received either 20 mg nefopam (n = 23) or matching placebo (n = 26), 90 min before surgery, immediately after surgery, and 6, 12 and 18 h after the end of surgery. The 24-h morphine requirements were measured using a patient-controlled analgesia system delivering on-demand intravenous bolus doses of morphine. Pain was assessed using visual analogue scales. Patients receiving nefopam had a mean (+/- s.e.m.) cumulative morphine consumption of 4.1 +/- 0.8 mg in the first hour, compared with 8.5 +/- 0.8 mg in the control group (P less than 0.01). After 24 h the consumptions were 44.1 +/- 7.2 mg and 62.5 +/- 6.9 mg respectively (P less than 0.05). The pain scores in both groups were similar. This study confirms that nefopam hydrochloride has significant analgesic effects and would be a useful supplement to morphine in the management of postoperative pain.

Abdomen↗
PubMed1975

Respiratory effects of nefopam.

A respiratory study has been done to compare the respiratory effects of a potent new analgesic, nefopam, to morphine. Morphine was a potent respiratory depressant at therapeutic dosage while nefopam was not.

Clinical Trials as Topic↗
PubMed1975

Nefopam and morphine in man.

A new analgesic, nefopam, is chemically distinct and pharmacologically unrelated to any presently known analgesic. A comparison was made of morphine and nefopam in 74 patients who required parenteral analgesia for moderate to severe postoperative and somatic pain, using a single administration, 2-dose level, double-blind design. A significant dose-response curve was obtained with nefopam and with morphine, and there was no significant deviation from parallelism. The time-effect curves for the 2 drugs were similar. The estimated relative potency of nefopam to morphine indicates that 20 mg of nefopam HCl is the approximate analgesic equal of 12 mg of morphine SO4. There were no adverse effects with nefopam and one adverse reaction to morphine.

Adult↗
PubMed1978

Oral nefopam and aspirin.

Analgesia through nefopam (30 mg, 60 mg, 90 mg), aspirin (325 mg, 650 mg), and placebo were compared in 122 hospitalized patients with moderate to severe postoperative, fracture, or other somatic pain. A double-blind noncrossover study design was used, and patients were evaluated for pain intensity and pain relief over a 6-hr period. Based on sum of pain intensity differences (SPID) scores, treatment effects were consistent and indicative of good dose response to both active medications. Pain relief scores were more variable but were generally in accordance with SPID values. Time-effect curves were similar. Estimated relative potency of nefopam to aspirin was 10.4 with a 95% confidence interval of 6.3 to 20.8 for SPID, indicating that the analgesic potency of nefopam, 60 mg, was equivalent to that of aspirin, 650 mg. Side effects were minimal.

Administration, Oral↗