Search PubMed⌕ Search

Biomedical subjects

E Munekata

Publications and source records attributed to E Munekata.

85 records · Page 5Linked to original sources

Regional distribution of substance P, neurokinin alpha and neurokinin beta in rat central nervous system.

Recently, we have found novel mammalian tachykinins, neurokinin alpha and beta isolated from porcine spinal cord, whose chemical structures are similar to those of substance P or kassinin. In the present study, we describe a specific assay system for neurokinin alpha and beta by combining HPLC and radioimmunoassay. We investigated the regional distribution of tachykinins including substance P in the rat central nervous system using anti-neurokinin alpha antiserum which cross-reacts 25% with neurokinin beta. As a result, it is noted that substance P was the highest in concentration in the rat substantia nigra, the striatum, the cerebellum and the spinal cord, but not in the cerebral cortex in which neurokinin beta was the highest. Concentration of neurokinin alpha was lower than that of substance P and the molar ratio of substance P and neurokinin alpha was fairly constant (2.8-4.0) in all regions. On the other hand, it is noted that the molar ratio of substance P and neurokinin beta was extremely variable and seemed to be specific to tissues.

Animals↗

Effects of taurine on tolerance to [D-Ala2, Met5]enkephalinamide in rats.

Effects of taurine on tolerance to [D-Ala2, Met5]enkephalinamide (DAME) were investigated in rats. Tolerance was produced by five intraventricular administrations of DAME (50 microgram) during 3 consecutive days. The magnitude of developed tolerance to DAME was not uniform for each behavioral parameter; tolerance to analgesia effects developed more intensively and rapidly from the repeated injections of the peptide than that to akinesia effects. Pretreatment with taurine (9.5 X 10(-2) M) which was injected in a volume of 10 microliter intraventricularly 10 min prior to every administration of DAME suppressed the development of tolerance to both analgesia and akinesia effects of this peptide, whereas pretreatment with L-leucine at the same concentration did not. Spontaneous locomotor activity was measured for 1 h after the 90-min behavioral observation period was completed. That activity increased with the number of the peptide injections. Taurine pretreatment inhibited the induction of 'hyper'-locomotor activity. These results support the view that taurine may possess an ability to inhibit development of tolerance to morphine-like peptides in rats.

Analgesia↗

Effects of taurine and gamma-aminobutyric acid on akinesia and analgesia induced by D-Ala2-Met-enkephalinamide in rats.

Effects of taurine or gamma-aminobutyric acid (GABA) on akinesia and analgesia induced by D-Ala2-Met-enkephalinamide were investigated in rats. Administration of taurine (dose range: 2.375 X 10(-2) M-9.5 X 10(-2)-Met-enkephalinamide were investigated in rats. Administration of taurine (dose range: 2.375 X 10(-2) M-9.5 X 10(-2) M/10 microliters) into the left lateral ventricle 10 min prior to the injection of D-Ala2-Met enkephalinamide (50 microgram/10 microliter) produced a dose-dependent reduction in the duration of akinesia and to some extent of analgesia, as estimated at 30 min and 60 min following the enkephalinamide injection; at the first estimation-time (10 min), taurine did not alter the duration of akinesia or that of analgesia. The median effective dose (ED50) for akinesia determined at 60 min after D-Ala2-Met-enkephalinamide was 5 times greater and that for analgesia assessed at the same time was 1.7 times greater in taurine-treated rats than the respective doses in control animals. Administration of GABA under similar experimental conditions produced a dose-dependent reduction in the duration of analgesia from the initial estimation time (10 min) following the injection of D-Ala2-Met-enkephalinamide. The ED50 for analgesia determined at 30 min after D-Ala2-Met-enkephalinamide was 3 times greater in GABA-treated rats than in control animals. Unlike the effects of taurine, GABA did not alter the duration of akinesia. Neither the duration of akinesia nor that of analgesia was modified by taurine or GABA alone in rats tested 9 min after the injection of each amino acid. These findings suggest that taurine may promote a recovery from both akinesia and analgesia, while GABA decreases only the analgesia induced by D-Ala2-Met-enkephalinamide.

Analgesia↗

Structure-activity studies of heptapeptide derivatives related to substance P, neurokinin A, B and other tachykinins on smooth muscles.

Diverse C-terminal heptapeptide derivatives related to substance P, kassinin, physalaemin, neurokinin A and B were synthesized and the contracting activities on the guinea pig ileum as well as rat duodenum were compared. In the partial sequence of C-terminal of tachykinin peptides, -I-II-Phe-III-Gly-Leu-Met-NH2, the combination of amino acid residues at positions I and III have significant roles in contraction of smooth muscle. For the activation of rat duodenal muscle (SP-E), Asp(I) and aliphatic amino acid(III), and for guinea pig ileal muscle(SP-P), Gln(I) and aromatic amino acid(III) are essential. Moreover, guinea pig ileum is sensitive to a full sequence of neurokinin peptides.

Animals↗

Antagonism by GRP(18-27) and substance P analogues on insulin release stimulated by GRP(18-27).

The antagonistic effects of [D-Phe25]gastrin-releasing peptide (GRP)(18-27) and [D-Arg1,D-Pro2,D-Trp7,9,Leu11]substance P (SP) on the stimulation of insulin release by GRP(18-27) from isolated canine pancreas were compared with that of [Ala23]GRP(18-27). The stimulation of insulin release by 1 nM GRP(18-27) was reduced to 24.1% and 15.4% by the prior infusion of 1 microM of [D-Arg1,D-Pro2,D-Trp7,9,Leu11]SP and 10 microM of [D-Phe25]GRP(18-27), respectively. Glucagon release by GRP(18-27) was not affected by these peptides using the above concentrations. The results indicate that these peptides are antagonists of bombesin-like peptide receptors on pancreatic B-cells, although the inhibitory activities are lower than that of [Ala23]GRP(18-27).

Amino Acid Sequence↗

Antibacterial activity and clinical efficacy of sparfloxacin in Mycobacterium avium-intracellulare complex infection.

In Japan the incidence of atypical mycobacteriosis has steadily increased, with Mycobacterium avium-intracellulare complex (MAC) the most common infecting organism. A standard chemotherapy regimen for MAC infection has not been established because of significant resistance to anti-mycobacterial drugs. Sparfloxacin has good antimicrobial activity against several acid-fast bacteria and is expected to be an effective drug for treating mycobacteriosis. We examined the effects of adding sparfloxacin to anti-tuberculotic combination therapy in six patients with MAC pulmonary disease. Drug susceptibility was also assessed using the agar dilution method. The minimum inhibitory concentrations (MICs) for sparfloxacin, levofloxacin, isoniazid, rifampicin, streptomycin, ethambutol and clarithromycin was measured in clinical isolates from all patients; sparfloxacin showed the lowest MIC. Bacteriological and clinical improvements were observed in the four patients who completed the study. Dosing was discontinued in two patients because of pruritic skin eruptions. Sparfloxacin shows promise as an anti-mycobacterial agent for treating MAC pulmonary disease.

Aged↗