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71.
(+)-2,9 alpha-Dimethyl-5-(m-hydroxyphenyl)morphan is the only phenylmorphan analog whose affinity for opioid kappa-receptors is greater than its affinity for opioid mu-receptors. Pharmacologically, the compound is a pure opioid antagonist devoid of agonist activity in in vivo assays of antinociception. The absolute configuration of the compound has been determined to be (1R,5S,9R) from an X-ray crystallographic study of the chloride salt. Thus, the absolute configuration corresponds to that of the atypical opioid agonist (-)-phenylmorphan while the weak atypical agonist (-)-2,9 alpha-dimethyl-5-(m- hydroxyphenyl)morphan corresponds to the potent morphine-like (+)-phenylmorphan. The preferred orientations of the phenyl ring for the two stereoisomers were determined using the molecular mechanics program MM2-87 and found to vary from that of the two parent compounds. The atypical properties of the two 9 alpha-methyl analogs is consistent with an opioid ligand model which proposes that morphine-like properties require a particular range of phenyl orientations. There was good agreement between the structure obtained from X-ray crystallography and computed with the MM2-87 program. 相似文献
72.
V A Frolov G Mall P Rieger Kh Derks Z Antoni 《Biulleten' eksperimental'no? biologii i meditsiny》1987,104(12):739-741
Intensive synthesis of collagen-like substance was revealed in the rabbit myocardium during experimental diphtheria intoxication. It was more marked in the right ventricle 24 hours after the injection of diphtheria toxin. Since similar changes (the substance was mainly formed around blood vessels) have been observed in other cases of toxic myocardial alterations (i.e. ethanol intoxication, injection of pharmacological agents, etc.), it can be assumed that it is a standard protective reaction of the altered heart to the penetration of toxic agents from the blood into the myocardial tissue. 相似文献
73.
N. V. Ozolina E. V. Kolesnikova V. N. Nurminsky I. S. Nesterkina L. V. Dudareva L. I. Donskaya R. K. Salyaev 《Biochemistry (Moscow) Supplemental Series A: Membrane and Cell Biology》2010,4(3):297-301
The changes in transport activity of tonoplast proton pumps under the influence of exogenous NO donator and modulation of
Ca2+ concentration jointly and separately were investigated at different stages of ontogenesis and under hyperosmotic stress.
The results suggest that both exogenous NO donator and Ca2+ ions can influence the activity of transport processes related to tonoplast and this influence is especially evident in the
period of growth and accumulation of metabolites. Under hyperosmotic stress, H+-pyrophosphatase plays a more important role than H+-ATPase: the activity of the former increases 2.3-fold compared to the control osmotic conditions, whereas the activity of
H+-ATPase is practically unchanged. H+-pyrophosphatase was more responsive to the presence of exogenous NO donator and to variations in Ca2+ concentration. The effects of exogenous NO donator on tonoplast proton pumps depended on the concentration of Ca2+, which apparently can mediate NO action. 相似文献
74.
K. Ferrazzoli Devienne M.S. Gonalves Raddi R. Gomes Coelho W. Vilegas 《Phytomedicine》2005,12(5):378-381
Three naturally occurring isocoumarins (paepalantine, paepalantine 9-O-beta-D-glucopyranoside and paepalantine 9-O-beta-D-allopyranosyl(1 --> 6) glucopyranoside) and two semi-synthetic analogues, 9,10-acylated compound and 9-OH-10-methylated compound, structurally similar to paepalantine, were evaluated for antimicrobial activity using a spectrophotometric microdilution technique. The paepalantine was active against S. aureus, S. epidermidis, and E. faecalis while the other four compounds proved ineffective against all microorganisms tested at concentrations of 500 microg/ml. Variations in phenolic substitution at OH-9 and/or OH-10 in the paepalantine molecule resulted in compounds without antimicrobial activity. A combination of structural features, two phenolic groups as cathecolic system, forms an oxygenated system arrangement that may reflect the potentially antimicrobial properties of paepalantine. 相似文献
75.
R Blomhoff W Eskild G M Kindberg K Prydz T Berg 《The Journal of biological chemistry》1985,260(25):13566-13570
The intracellular transport of chylomicron remnants labeled with [3H]retinyl ester was studied in rat liver parenchymal cells by means of subcellular fractionation in Nycodenz and sucrose density gradients. The data presented indicate that endocytosed chylomicron remnant [3H]retinyl ester initially is located in low density endosomes. Radioactivity is subsequently transferred to a denser vesicle. Equilibrium as well as rate zonal centrifugation suggest that this denser [3H] retinoid-containing vesicle may represent endoplasmic reticulum. We have compared the intracellular transport of chylomicron remnant [3H]retinyl ester and 125I-asialofetuin. The receptor-mediated endocytosis of asialoglycoproteins in rat liver parenchymal cells is a thoroughly studied system. Our results suggest that the [3H] retinoid and 125I-asialofetuin follow the same path initially to the endosomes. After transit in endosomes, the intracellular transport differs. While asialofetuin is transported to the lysosomes, the retinoid is probably transferred to the endoplasmic reticulum. 相似文献
76.
V P Andreev 《Biulleten' eksperimental'no? biologii i meditsiny》1985,99(3):370-373
Study of serial semi-thin (0.5 micron) metacrylate and paraffinic (8 microns) of rat kidney sections 6, 12, 24 and 48 h after subcutaneous injection of mercury bichloride at a dose of 0.6 mg/100 g bw has revealed that injury to different parts of the canalicular nephron is of heterogeneous character. The proximal part of the nephron demonstrates both complete and partial necrosis of nephrocyte cytoplasm. The distal parts of the nephron and collecting tubules are characterized by partial necrosis of the apical cytoplasm. Within the period between 12 and 24 h after the mercury bichloride injection, intracellular reparative processes are observed, in addition to destruction, in partially damaged but viable nephrocytes, which is confirmed by the enlargement of the nucleolic size. Regeneration of the tubular epithelium due to cellular restoration was unmarked 24 h after the mercury bichloride injection. 相似文献
77.
A.M. Ageel K.E.H. El-Tahir A.R. Abu-Jayyb 《Prostaglandins & other lipid mediators》1985,30(3):369-381
The effect of bromocriptine mesylate on cyclic nucleotides and PGI2 release by rat aortic and uterine tissues was investigated. Treatment of rats with bromocriptine (10 mg kg−1 I.P. daily for 14 days) increased PGI2 release by the thoracic aorta from 0.67 ± 0.02 to 1.4 ± 0.03 ng/mg wet tissue (P < 0.001; n = 6). This increase was antagonized by treatment with sulpiride (15 mg kg−1). Incubation of the arterial tissue with bromocriptive (50 ug ml−) in vitro also stimulated PGI2 release. Mepacrine (160 μg ml−) significantly decreased both basal and stimulated PGI2 release. Incubation of myometrial tissue from pregnant rats with bromocriptine (50 μg ml−1) in vitro significantly decreased PGI2 release from 1.25 ± 0.07 to 0.60 ± 0.08 ng/mg wet tissue (P < 0.05, n = 6).It also elevated uterine cAMP from 40 ± 2 to 64 ± 3 pmoles/100 mg wet tissue. Both effects were antagonized by sulpiride. Bromocriptine did not affect uterine cGMP or the cyclic nucleotides in the aorta. It is concluded that the increase in aortic PGI2 was mediated via activation of dopamine D-2 receptors that stimulate phospholipase A2 enzyme. The decrease in myometrial PGI2 release may be related to the increase in uterine cAMP resulting from activation of dopamine D-1 receptors. Previous studies suggested a role for PGI2 in implantation in the rat. The results suggest that the inhibitory effèct on uterine PGI2 may underlie the reported inhibition of bromocriptine on implantation. On broad basis, the decrease in uterine PGI2 together with the reported luteolytic effect of bromocriptine point to a potential role for the compound in postcoital contraception. 相似文献
78.
Circumsporozoite protein of Plasmodium berghei: gene cloning and identification of the immunodominant epitopes. 总被引:12,自引:2,他引:10
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D J Eichinger D E Arnot J P Tam V Nussenzweig V Enea 《Molecular and cellular biology》1986,6(11):3965-3972
The gene encoding the circumsporozoite (CS) protein of the rodent malaria parasite Plasmodium berghei was cloned and characterized. A cDNA library made from P. berghei sporozoite RNA was screened with a monoclonal antibody for expression of CS protein epitopes. The resulting cDNA clone was used to isolate the CS protein gene from a lambda library containing parasite blood-stage DNA. The CS protein gene contains a central region encoding two types of tandemly repeated amino acid units, flanked by nonrepeated regions encoding amino- and carboxy-terminal signal and anchorlike sequences, respectively. One of the central repeated amino acid unit types contains the immunodominant epitopes. 相似文献
79.
K N Iarygin A N Kazimirski? G I Kositski? A Iu Rubina V A Vinogradov 《Biulleten' eksperimental'no? biologii i meditsiny》1986,101(6):680-682
The authors studied the anabolic effect of peptide morphogen of the hydra undecapeptide on normal and regenerating rat liver. Ornithine decarboxylase (EC 4.1.1.17) activity served as a marker. Intraperitoneal injection of the peptide into intact animals stimulated ornithine decarboxylase activity in a dose-dependent manner. In partially hepatectomized rats the peptide stimulated ornithine decarboxylase activity in the dose of 20 micrograms/kg body weight while greater doses inhibited the enzyme activity. 相似文献
80.
Immune deficiency in the X-linked lymphoproliferative syndrome. I. Epstein-Barr virus-specific defects 总被引:8,自引:0,他引:8
S Harada K Sakamoto J K Seeley T Lindsten T Bechtold J Yetz G Rogers G Pearson D T Purtilo 《Journal of immunology (Baltimore, Md. : 1950)》1982,129(6):2532-2535
Eleven males with XLP were evaluated for EBV-specific antibodies during periods of 2 to 7 yr. Variable responses to EBV-specific antigens were found. All 11 patients had subnormal anti-EBNA titers, which probably reflected a T cell deficiency. The patients showed four different patterns in their anti-VCA response: 1) two boys who had experienced malignant lymphoma mounted no antibodies at all; 2) two patients showed intermittent anti-VCA titers; 3) four males had persistently elevated anti-VCA titers; and 4) three patients showed normal anti-VCA titers. ADCC against EBV-infected cells was abnormally low in six patients and was elevated in two patients given gamma-globulin. ADCC titers did not correlate with anti-VCA titers. However, most patients with XLP failed to effect regression of autologous EBV-infected lymphoblastoid cell lines, indicating a deficiency in long-lived T cell-mediated immunity to EBV. 相似文献