Charge transfer between O2+ ion and helium at electronvolt energy.
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Biomedical subjects
Publications and source records attributed to Z Fang.
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A series of 5-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines+ ++ (7a-h) was synthesized for biological evaluation as selective agonists for M1 receptors coupled to phosphoinositide (PI) metabolism in the central nervous system. Each ligand bound with high affinity to muscarinic receptors from rat brain as measured by inhibition of [3H]-(R)-quinuclidinyl benzilate ([3H]-(R)-QNB) binding. 5-(3-Methyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine+ ++ trifluoroacetate (CDD-0098-J;7a) displayed high affinity (IC50 = 2.7 +/- 0.69 microM) and efficacy at muscarinic receptors coupled to PI metabolism in the rat cortex and hippocampus. Increasing the length of the alkyl substituent increased affinity for muscarinic receptors yet decreased activity in PI turnover assays. The hippocampal PI response of 7a was blocked by lower concentrations of pirenzepine (8) or by higher concentrations of either AF-DX 116 (9) or p-fluorohexahydrosiladifenidol (10), suggesting that at low concentrations 7a selectively stimulates PI turnover through M1 receptors.
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Identified tract cells in lumbar enlargement were recorded from intact anaesthetized rats. The prolongation of the latency of antidromic action potential was a measure of postsynaptic inhibition. Both ST 36 and SP 6 were stimulated electrically. In EA group (N = 12) EA prolonged the latency for 0.111 +/- 0.022 ms (P < 0.001). In bicuculline group (N = 12) the prolongation of the latency for 0.010 +/- 0.004 ms (P < 0.05) by EA was less than that of EA group with statistical significance. In naloxone group (N = 12) and SP antiserum group (N = 12) EA did not induce a significant prolongation of the latency. It suggested that GABA, opioides and SP might be involved in postsynaptic inhibition induced by EA.
Effects of troxipide (Ku-54) on various experimental gastric ulcers in rats were studied. Ku-54 showed a dose-dependent antiulcerous action at 100, 200 and 300 mg/kg (particularly 300 mg/kg) p.o. in water-immersion stress, pylorus ligated and acetic acid reduced rats. The effect of cimetidine (CIM) (600 mg/kg) on water-immersion stress rats was significantly higher than that of Ku-54(300 mg/kg). On the other hand, the effect of Ku-54 (300 mg/kg) was higher than that of CIM (600 mg/kg) on the pylorus ligated and acetic acid reduced groups. The antiulcerous action of Ku-54 (300 mg/kg) was not related with the content and the pH of gastric juice.
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Experiments were carried out in rats anaesthetized with urethane (1 g/kg). Late discharges of spinal dorsal horn neurons were recorded as noxious responses to strong stimulation of right tibial nerve (a train of 3 pulses, 25V, 1ms). Left St.36 and Sp.6 were stimulated electrically (100Hz, 3V or 6V, 1ms). Left sciatic nerve was exposed and soaked for 15 min in 1.5% capsaicin or vehicle 24 hours before experiment. Left femoral nerve was sectioned. Spinal cord was transected at T4 level in spinal rat. Intact rats: 1) EA group (N = 12). Sciatic nerve was not treated. Late discharges of neuron were reduced to 44.6 +/- 18.3% of control (P less than 0.02) by EA(3v). 2) Capsaicin group (N = 15). Late discharges were reduced to 89.8 +/- 6.0% of control (P greater than 0.05) by EA(3V). 3) Vehicle group (N = 10). Late discharges were reduced to 51.2 +/- 15.6% of control (P less than 0.05) by EA(3V). 4) There was a statistical difference (P less than 0.05) between capsaicin and vehicle group. Spinal rats: 1) EA group. Late discharges of neuron were reduced to 67.6 +/- 10.3% of control (P less than 0.02) in 11 neurons by EA(3V), 72.7 +/- 8.8% (P less than 0.01) in 9 neurons by EA(6V). 2) Capsaicin group. Late discharges were 110 +/- 21.0% of control (P greater than 0.05) in 13 neurons after termination of EA (3V), 90.7 +/- 12.9% (P greater than 0.05) in 10 neurons after EA (6V). 3) Vehicle group. Late discharges were reduced to 67.7 +/- 8.1% of control (P less than 0.02) in 12 neurons by EA (3V), 68.1 +/- 5.0% (P less than 0.01) in 10 neurons by EA (6V). 4) There was a statistical difference (P less than 0.05) between capsaicin and vehicle group for 3V, no statistical difference (P greater than 0.05) for 6V. C fiber of peripheral nerve is main component involved in effect of EA analgesia in intact rats. Both A and C fiber of peripheral nerve involved in effect of EA analgesia in spinal rats.
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Five constituents, 2-furoic acid, succinic acid, ursolic acid, quercetin and daucosterol were isolated and identified from Osbeckia chinensis. All of them are reported to have been found from this plant for the first time.
Tripterine is one of the active components isolated from Tripterygium wilfordii Hook.f. In this study tripterine was shown to inhibit the antibody response of mouse splenocytes to SRBC both in vitro and in vivo either by primary or secondary stimulation. Tripterine was also found to significantly inhibit cotton pellet induced granuloma growth in rats and depress the delayed hypersensitive reaction of mouse skin to dinitrochlorobenzene (DNCB). Besides, it also increased the sleeping time of mouse induced by pentobarbital sodium. From the results stated above, it appears that tripterine might be useful in the treatment of inflammatory diseases or autoimmune diseases.
Mitoxantrone (DHAQ) we studied is a new semisynthetic antitumor drug prepared in China. This paper reports the pharmacokinetic studies of 3H-mitoxantrone in mice by liquid scintillation. The results showed that the decline of radioactivity in the plasma was a biphasic curve after intramuscular and intravenous injection in rats. The adsorption of 3H-DHAQ was ready and complete after intramuscular injection, it was widely distributed in body tissues. The concentration order of various organs was liver greater than intestine greater than kidney greater than lung greater than heart greater than muscles greater than brain. The elimination of the drug was slow, T1/2 was 42.56 h. In 72 h after administration the cumulative excretion of radioactivity in urine was 7% of the total dose, while that in feces was 43%. The main forms of the drug in urine were its metabolites.
The author analyzed 728 cataract extractions performed through 4 mm incisions during January 1972 to January 1987. 230 of the operations were done by phaco-emulsification, 320 by lensectomy, and 178 by aspiration. 580 of the eyes were followed up 1-15 years, when 87.8% of the eyes had corrected vision of 0.06 or over, and 48.8% of 0.6 or over. The technical aspect of cataract extraction through a small incision was evaluated and corneal astigmatism thereof discussed.
This paper reports clinical observations made during experimental Brugia malayi infection in man. This was induced by 52 infective larvae-carrying mosquitoes, Anopheles sinensis. A monkey, Maccaca mulatta, was inoculated with infective larvae from the mosquitoes infected with nocturnally periodic type of B. malayi from patients. Six months later, the monkey became a microfilaria carrier. Nine days later, the subject was experimentally bitten by mosquitoes infected from biting the monkey, with an estimated delivery of over 200 infective larvae. Seven days after the infection, general (but fluctuating) pruritus developed, followed by lymphadenitis and swelling of the hand and forearm, with a mild pyrexia for nearly 3 months. The eosinophil counts continuously increased. There were four separate attacks of lymphangitis. On day 142, microfilaraemia was first detected. After two more weeks, the subject was treated with a total dose of 15 g diethylcarbamazine (DEC) over 30 days. During this period, 28 small tender subcutaneous nodules appeared on his arms. After treatment, microfilaraemia gradually disappeared and the swelling of his arms improved. Three months later, the eosinophil count of his blood returned to normal but some temporary and scattered small pruritic erythematous patches still persisted over his left forearm. Lymphangitis has not recurred.
The synthesis of (-)-ranunculin from mannitol is described. The oxidation of 1,2,5,6-diacetone d-mannitol with NaIO4 or lead tetraacetate gave 2,3-O-isopropylidene-D-glyceraldehyde with the desired alpha-carbon-(R)-configuration. The Wittig reaction of isopropylidene-D-glyceraldehyde with (C6H5)3P = CHCOOCH3 gave a mixture of Z and E methyl-3-(2,2-dimethyl-1,3-dioxo-lan-4-yl)-2-propenoate with a Z:E ratio of 85:15. The dependence of Z:E ratio upon the solvent present was studied. On careful treatment of the cis isomer with 0.1 mol/L HCl, hydrolysis of the ketal took place along with cyclization to give the optically active aglycone with the expected stereochemistry, which was followed by Koenigs-Knorr reaction to give (-)-ranunculin tetraacetate. Since the glycoside is sensitive to acid and base, hydrolysis was carried out with strongly acidic cation exchange resin which yielded (-)-ranunuculin smoothly. The overall yield from mannitol with all the intermediates purified amounted to 15%.
This paper describes a culture system which supports the formation of B cell and some T cell colonies under serum-free conditions in peripheral blood samples of normal individuals and patients with chronic lymphocytic leukemia (CLL) of B cell type. In this system, serum is replaced by bovine serum albumin, transferrin, cholesterol, insulin and catalase or horseradish peroxidase. In addition, it is necessary to add staphylococcus protein A, mitomycin-treated T cells as feeders and phytohemagglutinin leukocyte-conditioned medium as a source of growth factors. The plating efficiency is greatly enhanced when normal cells are incubated with galactose oxidase prior to plating and when CLL cells are exposed sequentially to neuraminidase and galactose oxidase.
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