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Biomedical subjects

Z Fürst

Publications and source records attributed to Z Fürst.

10 recordsLinked to original sources
PubMed1996

PACAP participates in the regulation of the hormonal events preceeding the ovulation.

Pituitary adenylate cyclase activating polypeptide (PACAP) is a member of the secretin family. It was isolated and characterized in 1989. Its neuroendocrine role was demonstrated in vivo and in vitro systems. It seems that in vivo the effect of PACAP on the gonadotrop hormone secretion depends on the route of administration. It was reported that intravenous (i.v.) injection of PACAP elevated, while intra-cerebro-ventricular (i.c.v.) administration depressed plasma LH levels. In the present study it was demonstrated that PACAP, administered i.c.v. before the critical period of the proestrous stage, blocked the ovulation and prevented the proestrous LH surge in rats. The blocking effect of PACAP is not directly mediated by endogenous opioids because the antagonizing effect of Naloxone, an opioid receptor antagonist, was questionable. Under our experimental conditions we could not confirm the stimulating effect of i.v. administered PACAP.

Animals↗
PubMed1993

Highly potent novel opioid receptor agonist in the 14-alkoxymetopon series.

The newly synthesized 14-alkoxymetopon derivatives, 14-methoxymetopon, 14-ethoxymetopon, 14-methoxy-5-methyl-morphinone, exhibit high affinity for the naloxone binding sites in rat brain. A substantial decrease in affinity was observed, in the presence of NaCl indicating a high degree of agonist activity. All three 14-alkoxymetopon derivatives displayed high affinity for [3H][D-Ala2,(Me)Phe4,Gly-ol5]enkephalin ([3H]DAMGO) binding sites, much less potency toward delta sites and were the least effective at kappa sites. Isolated tissue studies using the guinea pig ileum preparation confirmed their high agonist potency. Following administration the new compounds produced naloxone reversible antinociceptive effects and were 130-300 times more potent than morphine in the acetic acid induced abdominal constriction model in the mouse, and the hot plate and tail flick tests in the rat. The compounds also produced dose-dependent muscle rigidity, and potentiated barbiturate-induced narcosis. The in vivo apparent pA2 values for naloxone against 14-ethoxymetopon and morphine were similar in analgesia, suggesting an interaction with the same (mu) receptor site. The dependence liability of 14-alkoxymetopon derivatives in the withdrawal jumping test was less pronounced than that of morphine in either rats or mice, similar to tolerance to the their analgesic action. It is concluded that the 14-alkoxymetopon derivatives studied are selective and potent agonists at mu opioid receptors, with reduced dependence liability.

Analgesics↗
PubMed1993

Synthesis and analgetic activity of nicotinic esters of morphine derivatives.

The synthesis of morphine nicotinates is described using nicotinyl chloride in the presence of pyridine. Isomorphine and isocodeine nicotinates were prepared from the corresponding morphine and codeine derivatives with nicotinic acid in the presence of triphenylphosphine and diethyl azodicarboxylate. Unexpectedly the reaction of 14-hydroxy-dihydromorphinone derivatives was anomalous, enolesters were formed. The analgetic activity of selected compounds was determined.

Analgesics, Opioid↗
PubMed1992

[Radiologic changes in the costovertebral and costotransverse joints and functional changes in the thoracic spine in ankylosing spondylitis].

Radiological, morphological and functional changes of the thoracic spine together with costovertebral and costotransversal joint involvement were studied in patients with ankylosing spondylitis. While radiological changes were found in all patients, in 74% they were of inflammatory origin. Radiological abnormalities were more prominent in patients with a more severe clinical course and a relatively short duration of the disease. As many as 95% of patients exhibited functional impairment of the thoracic spine. No significant difference was observed between the duration of disease and functional impairment of the thoracic spine (t = 1.4, P > 0.05) but there was a highly significant correlation between radiological changes and functional impairment of the thoracic spine (r = 0.577, P < 0.001).

Adult↗
PubMed1983

Septic sacroiliitis. An analysis of 14 patients.

In most joints arthritis is easily diagnosed. This, however, is not the case with infectious sacroiliitis because of the inaccessibility of the sacroiliac joint, due to the anatomic and topographic relations. Fourteen patients with septic sacroiliitis in whom the diagnosis was established between 10 and 90 days after the onset of the disease are reported for a 5-year period. All patients had scintigraphic high uptake and three patients did not show any radiographic changes.

Adolescent↗
PubMedDate not supplied

Endogenous morphine.

This review surveys the discovery of endogenous alkaloids in mammals. The formation of morphine in mammalian brain was assumed in 1970. The existence of morphine was demonstrated by radioimmunoassay. Identification of morphine was performed by spectroscopic methods. The isolation of mammalian morphine raises the question of biosynthesis. Recently, it has been shown that the biosynthetic pathway is similar to that that exists in poppy.

Alkaloids↗