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Biomedical subjects

W Gumułka

Publications and source records attributed to W Gumułka.

14 recordsLinked to original sources
PubMed1978

[Endorphins].

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Amino Acid Sequence↗
PubMed1978

[Enkephalins].

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Animals↗
PubMed1978

Antagonism by morphine and pethidine of the contractile effects of PGE2 on isolated uterus of the rat.

Morphine antagonizes the twitches evoked by administration of PGE2 on spontaneous contractile activity in the isolated uterus of the rat. This action is dose-dependent. Concentrations as low as 2.6 nM completely abolished contractile activity of PGE2 added to the bath at a concentration of 0.5 ng ml-1. In contrast to morphine, pethidine partially antagonized the stimulatory action of PGE2 at much higher concentrations.

Animals↗
PubMedDate not supplied

Lack of habituation of pain evoked potentials after naloxone.

Pain evoked potentials (EPs) were recorded in nucleus caudatus (NC) of rabbits after electric stimulation of the dental pulp. After 50--60 noxious stimuli the decrease in amplitude of evoked potentials occured. Naloxone, 1 mg/kg, temporarily abolished this effect and even after 350 noxious stimuli the habituation was not observed. On the other hand, naloxone did not affect the diminution of monosynaptic transcallosal potentials (TC--EP) evoked by repeated stimulation. It may be suggested that the habituation of EPs elicited by pain stimulation is due to endorphin release.

Animals↗
PubMedDate not supplied

Analgesic activity and opiate receptor affinity of new derivatives of N-butylpiperidine.

The three newly synthesized derivatives of N-butylpiperidine 1-butyl-4-phenyl-4-isonicotinoylaminoethylpiperidine (BG 25), 1-buty-isonicotinoylpiperidine (BG 26) and N-(1-butyl-4-phenyl-4-piperidinoyl) tetrahydropapaverine (BG 9) were evaluated for analgesic activity and opiate receptor affinity. All the three compounds showed analgesic activity both in hot-plate and flinch-squeak-jump test in mice, BG 9 being the most potent. The affinity of the compounds to opiate receptor was moderate (in comparison with pentazocine): the affinity of BG 9 was much greater than that of BG 25 and BG 26. The compounds showed a pronounced inhibitory action in stimulated guinea-pig ileum preparation; this was reversible by naloxone. As evaluated on pA basis, all three investigated compounds showed moderate antagonistic activity. Also in this respect BG 9 was more active than the other two compounds. Cholinolytic and strong spasmolytic properties were observed in isolated rat ileum preparation for BG 9 only.

Analgesics↗
PubMedDate not supplied

Lesion of locus coeruleus: the effect on pethidine and pentazocine analgesia.

Analgesic activity of pethidine and pentazocine in the locus coeruleus lesioned rats was evaluated. Bilateral destruction of locus coeruleus resulted in a marked decrease in noradrenaline content in forebrain but did not change significantly the levels of dopamine. Lesioned animals showed a marked decrease of predrug pain threshold. However, pethidine increased more effectively the nociceptive threshold in lesioned rats. The effect observed after pentazocine was generally similar but the maximal increase in pain threshold in lesioned animals did not differ significantly from the values observed in sham lesioned rats. The action of both analgesics was markedly prolonged after the lesion of the locus coeruleus.

Analgesics↗
PubMedDate not supplied

Esters of cephalosporins. Part I. Permeability of cefuroxime liberated from its 1-acetoxyethyl ester through biological membranes; influence of the form and size of the ester particles.

Concentrations of cefuroxime [II] in blood of rats were measured 30 and 60 min. after administration of amorphous form possessing various particles size (ranging from 0.09 to 0.4 nm) and crystal form of 1-acethoxyethyl ester of cefuroxime [I]. In vitro the concentrations of [II] were measured 15 and 45 min. after application of [I]. HPLC method was used for cefuroxime estimation. Close correlation between the particles size of the amorphous [I] and the concentrations of [II] in vivo as well as in vitro was found, the particles with lover size possessed higher bioavailability. The cefuroxime front the crystal form of ester is poorly absorbed and the concentrations of [II] after its application were similar to those observed after of the bigest particles of amorphous form both in vivo and in vitro.

Animals↗
PubMedDate not supplied

The bioavailability of injectable, amorphous form of aztreonam.

Amorphos injectable form of aztreonam (BIOKTAM) was prepared. It was shown that after intramuscular or intravenous administration there are not any considerable differences in the bioavailability of aztreonam from BIOKTAM and of the drug from AZACTAM.

Adult↗