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Objective To determine whether a drug detected in the blood or urine of a racing animal could have penetrated through the skin from a topically applied preparation.
Design Blood and urine of dogs and horses were analysed after topical administration of three common nonsteroidal anti-inflammatory preparations.
Experimental method Dimethylsulphoxide was analysed using a gas chromatograph with a flame photometric detector. Phenylbutazone, its metabolites and lignocaine were analysed using a gas chromatograph with a mass selective detector.
Results Dimethylsulphoxide, phenylbutazone and ligno-caine were detected in dog urine after muliple applications of the preparations. The maximum concentration of dimethyl-sulphoxide in dog urine correlated with the concentration of dimethylsulphoxide in the preparation. Phenylbutazone penetrated the skin more effectively from the cream than from the solution or gel preparations. This penetration was independent of the concentration of dimethylsulphoxide.
Conclusion The superior penetration of phenylbutazone from the cream can be explained by it being present as a neutral molecule in an hydrophobic medium. It is proposed that phenylbutazone penetrates the skin of greyhounds most effectively by a hydrophobic lipid route which is likely to be different from the path by which dimethylsulphoxide penetrates the skin. 相似文献
Design Blood and urine of dogs and horses were analysed after topical administration of three common nonsteroidal anti-inflammatory preparations.
Experimental method Dimethylsulphoxide was analysed using a gas chromatograph with a flame photometric detector. Phenylbutazone, its metabolites and lignocaine were analysed using a gas chromatograph with a mass selective detector.
Results Dimethylsulphoxide, phenylbutazone and ligno-caine were detected in dog urine after muliple applications of the preparations. The maximum concentration of dimethyl-sulphoxide in dog urine correlated with the concentration of dimethylsulphoxide in the preparation. Phenylbutazone penetrated the skin more effectively from the cream than from the solution or gel preparations. This penetration was independent of the concentration of dimethylsulphoxide.
Conclusion The superior penetration of phenylbutazone from the cream can be explained by it being present as a neutral molecule in an hydrophobic medium. It is proposed that phenylbutazone penetrates the skin of greyhounds most effectively by a hydrophobic lipid route which is likely to be different from the path by which dimethylsulphoxide penetrates the skin. 相似文献
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Black cohosh acts as a mixed competitive ligand and partial agonist of the serotonin receptor 总被引:6,自引:0,他引:6
Burdette JE Liu J Chen SN Fabricant DS Piersen CE Barker EL Pezzuto JM Mesecar A Van Breemen RB Farnsworth NR Bolton JL 《Journal of agricultural and food chemistry》2003,51(19):5661-5670
Extracts of the rhizome of black cohosh [Actaea racemosa L., formerly called Cimicifuga racemosa (L.) Nutt.] were evaluated for potential mechanisms of action in the alleviation of menopausal hot flashes. Ovariectomized Sprague-Dawley rats were administered a 40% 2-propanol extract of black cohosh [4, 40, and 400 mg/(kg.day)] by gavage for 2 weeks with or without estradiol [50 microg/(kg.day)] to determine if black cohosh could act as an estrogen or antiestrogen on the basis of an increase in uterine weight or vaginal cellular cornification. No effects were observed on uterine weight or on vaginal cellular cornification in rats treated with black cohosh alone or in combination with 17beta-estradiol, indicating this black cohosh extract had no estrogenic or antiestrogenic properties in the ovariectomized rat model. To evaluate other potential pathways by which black cohosh might reduce menopausal hot flashes, serotonin activity was first assessed by the inhibition of radioligand binding to cell membrane preparations containing recombinant human serotonin receptor (5-HT) subtypes. A 40% 2-propanol extract of black cohosh was tested against 10 subtypes of the serotonin receptor, revealing the presence of compounds with strong binding to the 5-HT(1A), 5-HT(1D), and 5-HT(7) subtypes. Subsequent binding studies were carried out using 5-HT(1A) and 5-HT(7) receptors because of their association with the hypothalamus, which has been implicated in the generation of hot flashes. The black cohosh 40% 2-propanol extract inhibited [(3)H]lysergic acid diethylamide (LSD) binding to the human 5-HT(7) receptor (IC(50) = 2.4 +/- 0.4 microg/mL) with greater potency than binding of [(3)H]-8-hydroxy-2-(di-N-propylamino)tetralin to the rat 5-HT(1A) receptor (IC(50) = 13.9 +/- 0.6 microg/mL). Analysis of ligand binding data indicated that components of a black cohosh methanol extract functioned as a mixed competitive ligand of the 5-HT(7) receptor. In addition, a black cohosh methanol extract elevated cAMP levels in 293T-5-HT(7)-transfected HEK cells, suggesting the extract acted as a partial agonist at the receptor. The elevation in cAMP mediated by the black cohosh extract could be reversed in the presence of the antagonist methiothepin, indicating a receptor-mediated process. These data suggest that reductions in hot flashes in some women taking black cohosh may not be due to estrogenic properties. This study identifies other possible biological targets of black cohosh that could account for reported biological effects. 相似文献
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Sialomucin Complex (Muc4) Expression in Porcine Endometrium During the Oestrous Cycle and Early Pregnancy 总被引:1,自引:0,他引:1
The non‐invasive type of implantation in the pig is characterized by the maintenance of a thick glycocalyx coating on the uterine epithelial surface microvilli. Present study investigated the alteration in the sialomucin complex (Muc4) expression during the oestrous cycle and early pregnancy in the pig. Endometrial tissue samples were immunostained with the primary antibody to the Muc4 transmembrane subunit ASGP‐2. Muc4 immunostaining increased in the surface and glandular epithelia between days 5 and 10 of oestrous cycle. Immunostaining continued to increase on day 12 with the greatest intensity of uterine Muc4 immunostaining detected on day 15 of the oestrous cycle and early pregnancy. Endometrial Muc4 expression in cyclic gilts decreased dramatically during early proestrous but continued to remain abundant in the surface and glandular epithelium of pregnant gilts during the period of conceptus attachment to the uterine surface. 相似文献