共查询到20条相似文献,搜索用时 78 毫秒
1.
C. Fuganti D. Ghiringhelli P. Grasselli 《Cellular and molecular life sciences : CMLS》1978,34(3):297-298
Summary (1
R) [1-3H,2H1] 3-Phenylpropanol, the key intermediate in the synthesis of (4
R) [4-3H,2H1] D, L-homoserine and of the (4
S)-isomer, is obtained from (1
S) [1-2H1] 3-phenylpropanol and (1
RS) [1-3H] ethanol upon incubation with yeast alcohol dehydrogenase and NAD+; under similar conditions 2-phenylethanol undergoes very small exchange with [1-2H2] ethanol. 相似文献
2.
R. Wiesendanger B. Martinoni T. Boller D. Arigoni 《Cellular and molecular life sciences : CMLS》1986,42(2):207-209
Summary Under the action of the appropriate synthase from ripe tomatoes a 11 mixture of (3S, 4R)-[3,4-2H2] and (3R, 4S)-[3,4-2H2]-(2S)-adenosylmethionine is transformed into a 11 mixture of the two meso forms of [2H2]-1-aminocyclopropanecarboxylic acid, a result which proves the operation of an inversion mechanism and which is consistent with direct nucleophilic displacement of the leaving group in the substrate. 相似文献
3.
Monica Bari Tiziana Bonifacino Marco Milanese Paola Spagnuolo Simona Zappettini Natalia Battista Francesco Giribaldi Cesare Usai Giambattista Bonanno Mauro Maccarrone 《Cellular and molecular life sciences : CMLS》2011,68(5):833-845
The endocannabinoid system and endocannabinoid receptor-driven modulation of glutamate release were studied in rat brain cortex
astroglial gliosomes. These preparations contained the endocannabinoids N-arachidonoylethanolamine (anandamide) and 2-arachidonoylglycerol, as well their major biosynthetic (N-acyl-phosphatidylethanolamines-hydrolyzing-phospholipase D and diacylglycerol-lipase) and catabolic (fatty acid amide-hydrolase
and monoacylglycerol-lipase) enzymes. Gliosomes expressed type-1 (CB1R), type-2 (CB2R) cannabinoid, and type-1 vanilloid (TRPV1)
receptors, as ascertained by Western blotting and confocal microscopy. Methanandamide, a stable analogue of anandamide acting
as CB1R, CB2R, and TRPV1 agonist, stimulated or inhibited the depolarization-evoked gliosomal [3H]d-aspartate release, at lower and higher concentrations, respectively. Experiments with ACEA (arachidonyl-2′-chloroethylamide),
JWH133 ((6aR,10aR)-3-(1,1-dimethylbutyl)-6a,7,10,10a-tetrahydro-6,6,9-trimethyl-6H-dibenzo[b,d]-pyran) and capsaicin, selective
agonists at CB1R, CB2R and TRPV1, respectively, demonstrated that potentiation of [3H]d-aspartate release was due to CB1R while inhibition to CB2R and TRPV1 engagement. These findings were confirmed by using selective
receptor antagonists. Furthermore, CB1R activation caused increase of intracellular IP3 and Ca2+ concentration, suggesting an involvement of phospholipase C. 相似文献
4.
(6R*)-[(2S*)-2-hydroxyheneicos-12-enyl]-5,6-dihydro-2H-pyran-2-one (1) degree is the major constituent of the secretion of freshly dissected Dufour's gland of the urticating ant Tetramorium aculeatum. In solution, compound 1 is slowly transformed into (1S*,5R*,7S*)-7-(nonadec-10-enyl)-2,6-dioxabicyclo[3.3.1] nonan-3-one (2) degrees on standing. The structures of compounds 1 and 2 have been established on the basis of their spectral and chemical properties. Compound 1 could be responsible for the urticating properties of the ant. 相似文献
5.
T. Iso H. Yamauchi H. Suda N. Nakajima K. Nishimura J. Iwao 《Cellular and molecular life sciences : CMLS》1978,34(9):1202-1203
Summary Carrageenin-induced oedema in rats was potentiated by oral administration of (4R)-3-[(2S)-3-mercapto-2-methylpropanoyl]-4-thiazolidinecarboxylic acid (SA291) and related sulfhydryl compounds, and the effect was closely correlated with their potencies as inhibitors of angiotensin-converting enzyme in vivo.Acknowledgment. The authors wish to thank Prof. H. Fujimura, Department of Pharmacology, Gifu University School of Medicine, for his helpful advice. 相似文献
6.
Small nuclear RNAs (snRNAs) from quiescent and serum-stimulated 3T3 cultures, labeled with [3H]uridine [( 3H]U), were electrophoresed in polyacrylamide-urea slab gels and revealed by staining with ethidium bromide and by fluorography. Judged by labeling with [3H]U, synthesis of 7S and U1-U6 RNAs was very low or absent in quiescent cultures. The serum-induced transition of 3T3 cells from a resting to a growing state was accompanied by an early, apparently sequential stimulation of snRNA synthesis; stimulated synthesis of 7S, U1, U2, U3, U4 and U6 RNAs coincided in time with serum-induced stimulation of 45S pre-ribosomal RNA (pre-rRNA) and heterogeneous nuclear RNA (hnRNA) synthesis. 相似文献
7.
V. P. Arya R. S. Grewal C. L. Kaul S. P. Ghate 《Cellular and molecular life sciences : CMLS》1971,27(10):1186-1187
Zusammenfassung 3-[4-(p-Fluorphenyl)-1,2,3,6-te-trahydro-1-pyridyl]-1-[1-(2-hydroxyaethyl)-5-methyl-4-pyrazolyl]-1-propanon (I, CIBA 4416/B-Go) senkt bei normotonischen und hypertonischen Tieren den Blutdruck. Die Drucksenkung kann hauptsächlich auf die periphere Vasodilatation sowie auf die Vasomotorenzentren bezogen werden. Ausserdem wirkt CIBA 4416/B-Go adrenolytisch.
Previous paper:V. P. Arya, R. S. Grewal, C. L. Kaul, S. P. Ghate, D. V. Mehta andT. George, J. Pharm. Sci.58, 432 (1969).Contribution No. 243 from CIBA Research Centre. 相似文献
Previous paper:V. P. Arya, R. S. Grewal, C. L. Kaul, S. P. Ghate, D. V. Mehta andT. George, J. Pharm. Sci.58, 432 (1969).Contribution No. 243 from CIBA Research Centre. 相似文献
8.
Summary Small nuclear RNAs (snRNAs) from quiescent and serum-stimulated 3T3 cultures, labeled with [3H]uridine ([3H]U), were electrophoresed in polyacrylamide-urea slab gels and revealed by staining with ethidium bromide and by fluorography, Judged by labeling with [3H]U, synthesis of 7S and U1-U6 RNAs was very low or absent in quiescent cultures. The serum-induced transition of 3T3 cells from a resting to a growing state was accompanied by an early, apparently sequential stimulation of snRNA synthesis; stimulated synthesis of 7S, U1, U2, U3, U4 and U6 RNAs coincided in time with serum-induced stimulation of 45S pre-ribosomal RNA (pre-rRNA) and heterogeneous nuclear RNA (hnRNA) synthesis. 相似文献
9.
Nonsteroidal antiestrogens reversibly and specifically inhibited the proliferation of two estrogen receptor-negative lymphoid cell lines (EL4 and Raji) in a dose-dependent manner. [3H]Thymidine incorporation of concanavalin A-stimulated primary splenocytes was also inhibited by 10(-6) M clomiphene (1-[4-(2-diethylaminoethoxy)phenyl]-1,2-diphenyl-2-chloroethylene). The antiproliferative effect could be prevented by the simultaneous presence in the growth medium of 10(-5) M linoleic acid or 10(-5) M arachidonic acid but not by 10(-6) M estradiol. Both lymphoid cell lines had high affinity antiestrogen-binding sites whose affinity could be altered by conditions of growth. Growth of EL4 cells in RPMI 1640 medium supplemented with charcoal-pretreated 5% fetal calf serum (charcoal-stripped medium) resulted in significantly higher affinity (Kd 0.54 nM +/- 0.11 nM; n = 6) than growth in medium supplemented with untreated serum (complete medium) (Kd = 1.68 nM +/- 0.48 nM; n = 6) (p less than 0.001). This change in affinity was partly due to removal of fatty acids from the growth medium by charcoal pretreatment, since addition of 10(-5) M linoleic acid or 10(-5) M gamma-linolenic to charcoal-stripped medium decreased the affinity of the antiestrogen-binding protein. In contrast, growth in 10(-5) M stearic acid or 10(-5) M oleic acid did not significantly alter the affinity of the antiestrogen-binding protein, whereas 10(-5) M palmitic acid significantly increased its affinity. The same fatty acids were also tested for their intrinsic effects on EL4 cell proliferation. Oleic, linoleic and gamma-linolenic acids were growth stimulatory while stearic and palmitic acids were not. Thus linoleic and gamma-linolenic acids whose presence in the growth medium was associated with decreased affinity of [3H]tamoxifen (1-[4-(2-dimethylaminoethoxy)phenyl]-1,2-diphenylbut-1(Z)-ene) binding to the intracellular antiestrogen-binding protein were also growth stimulatory. Unsaturated fatty acids have previously been shown to inhibit binding of [3H]tamoxifen to the antiestrogen-binding protein in a cell-free system. The present observations demonstrate that unsaturated fatty acids also modify the affinity of the antiestrogen-binding protein in intact cells. 相似文献
10.
Phospholipase C activation via a GTP-binding protein in tumoral islet cells stimulated by carbamylcholine 总被引:2,自引:0,他引:2
Carbamylcholine and GTP act synergistically in stimulating the production of [3H]inositol-1-phosphate by digitonized tumoral islet cells (RINm5F line) prelabeled with myo-[2-3H(N)]inositol. The response to these two agents is similar to that evoked by GTP gamma S. These findings suggest that a GTP-binding regulatory protein couples the occupancy of muscarinic receptors to activation of phospholipase C in pancreatic islet cells. 相似文献
11.
Carrageenin-induced oedema in rats was potentiated by oral administration of (4R)-3-[(2S)-3-mercapto-2-methylpropanoyl]-4-thiazolidinecarboxylic acid (SA291) and related sulfhydryl compounds, and the effect was closely correlated with their potencies as inhibitors of angiotensin-converting enzyme in vivo. 相似文献
12.
3[H]-(-)-Sulpiride and 3[H]-spiperone binding was compared in rat amygdala, nucleus accumbens and striatum, using (+/-)-sulpiride to define specific binding. 3[H]-(-)-Sulpiride bound to twice as many sites in amygdala and nucleus accumbens as 3[H]-spiperone. 3[H]-(-)-Sulpiride binding was directed to these additional sites by using 1 microM spiperone to mask dopaminergic binding. The binding of 3[H]-(-)-sulpiride to these sites was high affinity, reversible, Na+-dependent, but not stereospecific. Metoclopramide, tiapride and antidepressant medications, but not other neuroleptics, ADTN, or serotonin displaced 3[H]-(-)-sulpiride binding to these sites. These data suggest that 3[H]-(-)-sulpiride labels mesolimbic sites other than dopamine receptors which may mediate antidepressant effects. 相似文献
13.
dl-Erythro-1-phenyl-2-(o-chlorophenyl)-2-[4-(p-methoxybenzyl)-1-piperazinyl] ethanol dihydrochloride showed orally a definite analgesic activity, without producing the significant morphine-like physical dependence liability, and its analgesic potency was about a half that of codeine and far superior to aminopyrine in experimental animals. 相似文献
14.
S. Sakurai T. Ohtaki H. Mori M. Fujiwhara K. Mori 《Cellular and molecular life sciences : CMLS》1990,46(2):220-221
Summary Biological activity of enantiomerically pure juvenile hormones was assayed by topical application on allatectomizedBombyx fourth instar larvae. JHs tested were (10R)-JH I [methyl (2E,6E,10R,11S)-10,11-epoxy-3,11-dimethyl-7-ethyl-2,6-tridecadienoate], (10S)-JH I [methyl (2E, 6E, 10S, 11R)-10,11-epoxy-3,11-dimethyl-7-ethyl-2,6-tridecadienoate], (10R)-JH III [methyl (2E,6E,10R)-10,11-epoxy-3,7,11-trimethyl-2,6-dodecadienoate] and (10S)-JH III [methyl (2E,6E,10S)-10,11-epoxy-3,7,11-trimethyl-2,6-dodecadienoate]. Among these compounds, natural (10R)-JH I was most active and the dose needed to induce 50% larval molting was 0.04 g/larva; it was approximately 12,000 times more active than unnatural (10S)-JH I. Though natural (10R)-JH III showed slight biological activity, it was only one three-thousandth of that of (10R)-JH I. Unnatural (10S)-JH III exhibited no biological activity at the levels assayed. 相似文献
15.
H. Nakamura K. Ishii Y. Yokoyama S. Motoyoshi C. Imazu M. Shimizu 《Cellular and molecular life sciences : CMLS》1979,35(3):369-370
Summary dl-Erythro-1-phenyl-2-(o-chlorophenyl)-2-[4-(p-methoxybenzyl)-1-piperazinyl] ethanol dihydrochloride showed orally a definite analgesic activity, without producing the significant morphine-like physical dependence liability, and its analgesic potency was about a half that of codeine and far superior to aminopyrine in experimental animals. 相似文献
16.
G. F. Weirich J. P. Kochansky E. P. Masler W. R. Lusby M. F. Feldlaufer A. K. Raina J. A. Svoboda 《Cellular and molecular life sciences : CMLS》1995,51(9-10):961-966
The tritium-labeled bis-norleucine analog ofHelicoverpa zea pheromone biosynthesis-activating neuropeptide ([3H]NLPBAN) was incubated in vitro with hemolymph fromManduca sexta orH. zea adult females. The incubations resulted in the formation of several tritium-labeled degradation products. At a [3H]NLPBAN concentration of 0.9 μM the degradation proceeded at a very slow but physiologically plausible rate (2–10 fmol/min/μl hemolymph). The primary [3H]NLPBAN degradation reaction inM. sexta hemolymph was not inhibited by 20 μM leupeptin, 0.1 mM amastatin, 1 mM EDTA, 1 mM EGTA, 1 mM 1,10-phenanthroline, or 2 mM 4-(2-aminoethyl)benzenesulfonyl fluoride; but secondary reactions may have been affected, as some of the inhibitors changed the radio-HPLC profile of the degradation products. It is concluded that hemolymph ofM. sexta andH. zea contains peptidase(s) capable of inactivating circulating PBAN. 相似文献
17.
The effects of serotonin on the formation of inositol phosphates and protein phosphorylation were examined in cultured smooth muscle cells. Serotonin stimulated the formation of [3H]inositol monophosphate, [3H]inositol bisphosphate and [3H]inositol trisphosphate. This effect was prevented by 5-HT2 specific antagonist, 6-methyl-1-(1-methylethyl)ergoline-8-carboxylic acid, 2-hydroxy-1-methylpropyl ester [Z]-2-butenedioate (LY53857). Serotonin stimulated the phosphorylation of many polypeptides, among which a 20 kDa polypeptide was the most prominent. The phosphorylation was also inhibited by LY53857. LY53857 alone produced no effects on protein phosphorylation. The 20 kDa polypeptides were also phosphorylated by the addition of 12-O-tetradecanoylphorbol-13-acetate. These results suggest that serotonin stimulates protein phosphorylation through 5-HT2 receptors and possibly activates protein kinase C in intact vascular smooth muscle cells. 相似文献
18.
2-Halogeno- and 2-methyl-ethanols inhibit alpha-chymotrypsin in the order of their substituted groups: [1] tri- greater than di- greater than mono-, [2] Br- greater than Cl- greater than CH3- greater than F-. The inhibition by the halogeno-ethanols is mediated differently from that by the methyl-ethanols, ethanol, and urea. 相似文献
19.
Inhibition by tetanus and botulinum A toxin of the release of [3H]noradrenaline and [3H]GABA from rat brain homogenate 总被引:2,自引:0,他引:2
E Habermann 《Experientia》1988,44(3):224-226
Rat brain homogenate was preloaded with [3H]noradrenaline or [3H]GABA and stimulated with high K+. Tetanus toxin and botulinum A neurotoxin partially prevent the evoked [3H]noradrenaline release in the same range of toxin concentrations starting below 10(-10) M. In contrast, release of gamma-amino butyric acid (GABA) is much more sensitive to tetanus than to botulinum A toxin. 相似文献
20.
A Malassine S Chaffaux M Breuiller P Laporte F Ferré 《Comptes rendus des séances de l'Académie des sciences. Série D, Sciences naturelles》1980,290(3):231-234
Delta 5, 3 beta hydroxysteroid dehydrogenase activity was studied on mitochondrial and microsomal fractions of human and cat placentas. This activity was assessed by measuring the rate of [3H] progesterone formation from [3H] pregnenolone and of [3H] delta 4-androstenedione from [3H] dehydroepiandrosterone (DHA), by a double isotope dilution method. Specific activities measured under initial velocity conditions were similar in both human and cat placentas. However, the kinetics of the reaction with DHA as substrate exhibit a zoological specificity. 相似文献