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At least 217 records · Page 12Linked to original sources
PubMedDate not supplied

Mass spectrometric identification of urinary and plasma metabolites of 6-(6'-carboxyhexyl)-7-n-hexyl-1,3-diazaspiro-[4-4]-nonan-2,4-dione, a new cytoprotective agent.

The compound IBI-P-01028, or R,S-cis-6-(6'-carboxyhexyl)-7-trans-n-hexyl-1,3-diazaspiro-[4-4]-nona n-2,4- dione, is a new cytoprotective agent under development. To study the metabolites of this compound in laboratory animals, we administered it to dogs and rats, and analyzed extracts from dog and rat urine, and from dog plasma, by GC-MS. The metabolic profiles were different in the rat and dog. In the dog (plasma and urine), one metabolite was found, and in the rat urine two other metabolites were found. The unmetabolized drug was found only in the dog plasma and urine.

Animals↗
PubMedDate not supplied

Terfenadine (single or associated) treatment of adverse reactions to foods.

Six groups of patients (total 105), affected by cutaneous signs and symptoms related to food ingestion were studied with regards to the clinical efficacy of some pharmacologic treatments: blind placebo, terfenadine alone, terfenadine associated with pirenzepine or rosaprostol or ranitidine or famotidine. Pharmacologic treatment by terfenadine alone showed poor clinical results, similar to placebo, while the associations of terfenadine with both cytoprotective drugs and anti-H2 receptor antagonists revealed significant clinical improvement which is more evident in those patients treated with cytoprotective drugs combination than those who were treated with anti-H2 antagonists.

Adolescent↗
PubMed1988

How the sauna affects the endocrine system.

The sauna induces changes in the secretion of hormones, some similar to changes induced in any other stress situation and others characteristic of exposure to the sauna. Noradrenaline is usually the only catecholamine raised by the sauna in people accustomed to it. The secretion of the antidiuretic hormone is increased and the renin-angiotensin-aldosterone system is activated. The concentrations of the growth hormone and prolactin, in particular, secreted from the anterior pituitary are increased in the circulation. The concentration of the immunoreactive beta-endorphin in blood may also increase which may reflect the feeling of pleasure or, on the other hand, discomfort induced by the sauna. The views on the effects of the sauna on the secretion of the ACTH and cortisol are partly contradictory, probably due to differing ways of taking the sauna bath. In Finnish sauna takers the concentration of cortisol in blood is not usually increased. The changes induced by the sauna in various hormone concentrations in the circulation are, however, normalized within a couple of hours after the heat stress.

Catecholamines↗
PubMedDate not supplied

Prostaglandins and their precursors in rheumatoid arthritis: progress and problems.

Evidence is presented to support the hypothesis that prostaglandins and their precursors, collectively termed prostanoids, have an important role to play in the pathogenesis of joint destruction in arthritis, with particular reference to rheumatoid arthritis. After discussion of the role of prostanoids as mediators of inflammation, evidence is given that prostanoids are present in the joints of patients with rheumatoid arthritis, that these substances are capable of causing joint damage in vitro and in vivo, and that drugs which are able to arrest the progress of the arthritic condition or bring symptomatic relief possess the ability to inhibit prostanoid synthesis in vivo and in vitro.

Animals↗
PubMed1982

A comparison of agents for inducing parturition in mares in the pre-viable and premature periods of gestation.

Various regimens of prostaglandins, alone or followed by oxytocin, were given to induce parturition in mares during the pre-viable and premature periods of gestation and in near-term mares. The most successful method of induction was found to be 2 i.m. injections of 500 micrograms fluprostenol (Equimate: I.C.I.) at a 2-h interval followed (if necessary) by 10-20 i.u. oxytocin injected i.v. in 5 i.u. serial increments every 15-20 min. Peak concentrations of the prostaglandin metabolite (PGFM) in response to the inducing agents were shown to be associated with delivery at, but not before, 320 days of gestation. A radiolabelled study of [14C]fluprostenol distribution showed that fluprostenol was present in placenta, amnion, allantoic and amniotic fluid, and in foal plasma and liver.

Animals↗
PubMed1977

[Synthesis of n-pentanoylmethylenetriphenylphosphorane].

An efficient synthesis of n.pentanoylmethylenetriphenylphosphorane (II), useful intermediate for achievement of prostanoic derivatives, is described. The procedure affords the desired product at a remarkable degree of purity.

Chemical Phenomena↗
PubMed1977

[Synthesis of n-hexanoylmethylene triphenylphosphorane].

An efficient synthesis of n.hexanoylmethylenetriphenylphosphorane (II), a fundamental intermediate for obtaining prostanoic products, is described. The crucial intermediate in the synthesis is the 2-keto-n.heptyltriphenylphosphonium chloride (VII), which is prepared via a very precise procedure.

Chemical Phenomena↗
PubMedDate not supplied

Evidence for the presence of AH 13205-sensitive EP2-prostanoid receptors in the pregnant baboon but not in the pregnant sheep myometrium near term.

OBJECTIVE: Our purposes were to assess the effects of prostaglandin (PG) E2 and PGF2 alpha on myometrial contractility in pregnant sheep and baboons in an in vitro superfusion study, and to characterize further the PGE-sensitive (EP) receptor subtype involved in the myometrial response to PGE2 by using the selective prostanoid EP2 agonist AH 13205. METHODS: Strip preparations of uterine muscle from 15 sheep (107-145 days' gestational age) and ten baboons (158-185 days' gestation) were studied. Cumulative concentration-response curves (CRC) were constructed to oxytocin (4.2 pmol/L to 0.42 mumol/L, PGE2 (0.1 nmol/L to 1 mumol/L), and PGF2 alpha (1 nmol/L to 100 mumol/L), and 50% effective concentration (EC50) values (mean and 95% confidence interval) were calculated. We also tested the hypothesis that PGE2-induced myometrial relaxation in pregnant baboons could be mediated by EP2-prostanoid receptors. Myometrial strips were stimulated by oxytocin (0.42 nmol/L), and CRCs to the EP2-agonist AH 13205 (0.1 nmol/L to 10 mumol/L) were constructed. RESULTS: Prostaglandin F2 alpha stimulated myometrial activity in a concentration-related fashion in all preparations from both sheep and baboons. The EC50 in the sheep myometrium for PGF2 alpha (52 nmol/L, 95% confidence interval [CI] 25-110) was significantly (P < .05) lower than that in baboon myometrium (183 nmol/L, 95% CI 93-355). Oxytocin stimulated myometrial activity in preparations of both sheep (EC50 = 0.29 nmol/L, 95% CI 0.11-0.71) and baboon (EC50 = 0.31 nmol/L, 95% CI 0.18-0.52). In contrast, responses to PGE2 were species-related: PGE2 caused concentration-related stimulation of myometrial activity in sheep tissue (EC50 = 3.2 nmol/L, 95% CI 2.0-5.0), but induced concentration-related inhibition of activity in baboon myometrium (50% inhibitory concentration [IC50] = 21 nmol/L, 95% CI 2.2-203). A concentration-related inhibitory response to AH 13205 (IC50 = 3.56 nmol/L, 95% CI 1.28-5.99) was obtained in the baboon. In contrast, AH 13205 failed to inhibit comparable myometrial strip preparations from pregnant sheep. CONCLUSIONS: The present studies suggest that both sheep and baboon myometrium contain prostanoid receptors that mediate stimulation. In addition, baboon myometrium, like that from the human, contains AH 13205-sensitive EP receptors (EP2 receptors), which mediate inhibition. The pregnant baboon may therefore represent a suitable animal model for investigations into the use of EP2 agonists for the prevention of premature labor in humans.

Animals↗
PubMed1975

The determination of prostaglandin metabolites in human urine.

A method has been developed in which the human urinary prostaglandin metabolites are converted into stable prostanoic and prostanediotic acid homologues. The urine is reduced with sodium borohydride and the organic compounds, isolated with an Amberlite XAD-2 column, are treated with fuming hydrogen iodide, followed by treatment with zinc in methanolic hydrogen chloride, to yield dimethyl tetranorprostanedioate as the major product of human prostaglandin metabolism. This compound is determined by gas chromatography, after a single purification by thin layer chromatography. The excretion of total tetranorprostanedioic acid derivatives in healthy subjects was found to be 0.21 plus and minus 0.08 mg per g of creatinine or 0.3 plus and minus 0.01 mg per 24 hours.

Adult↗