Behavioural effects of intrathecally injected tachykinins in rats with peripheral nerve transection.

The effect of unilateral sciatic nerve transection on behavioural responses produced by intrathecal administration of substance P (SP), neurokinin A, eledoisin and physalaemin was investigated in the rat. The injection of SP (3 nmol/rat) into the subarachnoid space was followed by reciprocal scratching, biting and licking of the fore- and hind-limbs. There was no observable difference in the behavioural response to SP between rats with nerve transection and sham operated rats at 5 days after operation.

[The effect of nonanoyl vanillylamide on the chemically-induced nociception].

The aim of the present investigation was to determine the effects of a single dose and serial doses of nonanoyl vanillylamide (NVA) administered subcutaneously on responses induced by chemical stimuli in the mouse. The treatment with a single subcutaneous injection produced a significant decrease in the number of abdominal contraction responses produced by intraperitoneal injections of phenylbenzoquinone and in the responsive time of licking induced by plantar injection of formalin. The serial subcutaneous administration of NVA caused a dose related antinociceptive effect against a chemical nociceptive stimulus using the phenylbenzoquinone-induced writhing test, while NVA was ineffective against a chemical stimulus, formalin.

Effect of sodium citrate on the blood disappearance of 67Ga.

The effect of sodium citrate on the blood disappearance of 67Ga was examined in rats. The half life value of the alpha phase and the initial AUC value (0-60 min) were dose-dependently decreased by sodium citrate. The binding of 67Ga to serum proteins was also dose-dependently inhibited by sodium citrate.

Participation of peptide moieties in adhesive behavior of antigenic mannans of Candida albicans to the plastic microtiter plate in enzyme-linked immunosorbent assay.

We report our studies of the mechanism of the adhesion of mannans of Candida albicans NIH A-207 and C. albicans NIH B-792 strains to the surface of a polystyrene microtiter plate being utilized for enzyme-linked immunosorbent assay (EIA) of antigens of this pathogenic yeast species. This binding was manifested predominantly by the peptide moieties of the mannans forming hydrophobic bonds with the plastic molecule.

Involvement of alpha-adrenoceptors in para-hydroxyamphetamine-induced head-twitch response.

The effect of some drugs with a higher selectivity for either the alpha 1- or alpha 2-adrenoceptors on the head-twitches induced by intracerebroventricular administration of p-hydroxyamphetamine (p-OHA) in mice, have been studied. Pretreatment with yohimbine increased the number of head-twitches induced by p-OHA, whereas pretreatment with clonidine or prazosin reduced the number of responses. The decrease in head-twitches produced by clonidine was completely antagonized by pretreatment with yohimbine.

Central hypothermic effects of some analogues of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and 1-methyl-4-phenylpyridinium ion (MPP+).

Effects of some MPTP or MPP+ analogues on mouse body temperature were studied. Of the analogues tested, 4-phenylpyridine (PPY) and 4-phenyl-1,2,3,6-tetrahydropyridine (PTP) given in single i.p.

Behavioural characterization of substance P-induced nociceptive response in mice.

Intrathecal injection of substance P produced a behavioural syndrome, consisting of reciproacal hindlimb scratching and biting or fore- and hind-licking. Pretreatment with either an analogue of substance P, (D-Pro2, D-Trp7,9)-substance P (DPDT-SP) or (D-Arg1, D-Pro2,4, D-Trp7,9, Leu11)-substance P, given intrathecally, reduced the response to substance P in a dose-dependent manner. The behaviour induced by substance P was also inhibited by intrathecal, intracerebroventricular (i.

Utilization of 67Ga-citrate for the measurement of histamine-induced edema in anesthetized rats.

Radioactivity of the histamine-induced paw edema was measured after intravenous injection of 67Ga-citrate in anesthetized rats. The radioactivity was fluctuated almost parallel with the edema rate following subcutaneous injection of histamine. Both the radioactivity and the edema rate were almost equally reduced by pretreatment with chlorpheniramine, an antihistaminic agent.

Synthesis of 16 alpha,19-dihydroxy-4-androstene-3,17-dione and 3 beta,16 alpha,19-trihydroxy-5-androsten-17-one and their 17 beta-hydroxy-16-keto isomers.

3 beta,16 alpha,19-Trihydroxy-5-androsten-17-one and 16 alpha,17-dihydroxy-4-androstene-3,17-dione were synthesized from the 5 alpha-bromo-6 beta,19-epoxy-17-ketone derivative 1, using the bromination at C-16 alpha of the 17-ketone 1 and the controlled alkaline hydrolysis of the 16 alpha-bromo-17-ketones 2 and 11 as key reactions. Zinc dust reductive cleavage of the 6 beta,19-epoxy-16 alpha-hydroxy-17-ketones 4 and 12, produced by controlled hydrolysis, gave the corresponding 19-alcohol derivatives 6 and 14, which were rearranged to the 17 beta-hydroxy-16-ketones 7 and 15 when treated with sodium hydroxide. The 3 beta,16 alpha,17 beta,19-tetrol 8 was obtained from the 16 alpha-ketol 6 by reaction with sodium borohydride.

Evaluation of histamine induced acute inflammation by 67Ga-citrate in conscious rats.

Radioactivity of 67Ga in the paw edema and the edema rate were measured after subcutaneous injection of histamine into the paw of the conscious rat. The radioactivity increased almost parallel with the edema rate following the injection of histamine. The increase in the radioactivity and edema were almost completely prevented by pretreatment with a 10 mg/kg dose of chlorpheniramine, an antihistaminic agent.

Purification and characteristics of glucocorticoid antagonizing factor in endotoxemia.

The present study involved the purification of GAF (glucocorticoid antagonizing factor) released in blood of endotoxemic mice, using the inhibition rate of tryptophan oxygenase (TO) activity in the mice liver as a parameter, to determine if this plays a role in metabolic disorders. GAF-rich serum in zymosan-primed and endotoxin-injected mice was subjected to chromatography on DEAE-Sepharose CL-6B, Blue Sepharose CL-6B and Sephadex G-200 superfine columns. Finally, GAF fractions were purified by chromatography on a DEAE-Sepharose CL-6B column.

Synthesis and evaluation of bromoacetoxy 4-androsten-3-ones as active site-directed inhibitors of human placental aromatase.

2 alpha-Bromoacetoxy (II), 6-bromoacetoxy (VII and X), and 19-bromoacetoxy (XII) derivatives of androstenedione and 17 beta-bromoacetoxy compounds (III, IV, XIII-XVI) were synthesized as potential affinity-labeling reagents for aromatase. 6 alpha-Bromoacetoxy derivative VII was the most potent inhibitor of human placental microsomal aromatase activity among this series. Its inhibitory activity was higher than that of the parent 6 alpha-hydroxy compound V, although other bromoacetates showed weaker inhibition of aromatase than the corresponding alcohols.

Antinociceptive action of morphine and pentazocine on unit activity in the nucleus centralis lateralis, nucleus ventralis lateralis and nearby structures of the cat.

Single neuronal activity has been recorded extracellularly from the nucleus centralis lateralis (CL), ventralis lateralis (VL) and medialis dorsalis (MD) of the cat thalamus. The majority of the CL, VL and MD neurons were excited by nociceptive stimulation such as pinching the skin with serrated forceps and/or intra-arterial injection of bradykinin. The nociceptive neurons were also driven by non-nociceptive stimulation such as tap of deep tissues, bending hairs and an air-puff and/or joint rotation, and their receptive fields were large.