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7α-和7β-甲基-10β,17β-二乙酰氧基-△4-雌甾烯-3酮(简称7α-和7β-甲-乙氧雌酮)对小鼠抗早孕ED50分别为1.6和5.5 mg/kg。7α-甲-乙氧雌酮在大鼠也有抗早孕作用并使血浆孕酮浓度降低,应用10 μg/ml浓度能抑制离体妊娠大鼠卵巢孕酮合成。7α-和7β-甲-乙氧雌酮与兔子宫胞浆雌二醇受体的相对结合亲和力(RBA)分别为10.8和1.5,与孕酮受体的RBA均<1.7α-和7β-甲-乙氧雌酮都有较弱的雌激素和抗雌激素活性。 相似文献
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We have introduced a carbonyl group at the 11-position and a double bond at the 9-position of norethisterone in order to increase its antifertility potency. The starting material for the preparation of 11-keto-Δ9-noret-histerone(9) was 19-hydroxy-Δ4-androstene-3,17-dione(1), which was converted to the title compound by partial synthesis through the sequence of reactions:(1)→(9).11-Keto-Δ9-norethisterone was found to possess very potent antifertility effect by preliminary screening tests. 相似文献
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珊瑚红球菌944-45选择性降解胆甾醇时,改变生物氧化条件(溶解氧、pH、种量、种龄、无机离子等)及投料方式,可提高雄甾-1,4-二烯-3,17-二酮(简称 ADD)的生成量。当底物浓度为0.25%,转化时间为94h 时,其 ADD 收率(GC 测定)最高约为37%。 相似文献
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为了寻找心血管系统药物,以表雄酮为原料,合成了7个16,17位取代的目标化合物:2β-(4’-甲基-1’-哌嗪基)-3α-羟基-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α-羟基-16α-溴-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-氧-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-肟-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17β-氨基-5α-雄甾烷和2β—(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-16β-氨基-5α-雄甾烷。初步药理试验结果表明它们都有不同程度的抗心律失常活性。 相似文献
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Tahereh Hosseinabadi Hossein Vahidi Bahman Nickavar Farzad Kobarfard 《Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences》2014,22(1)
Background
The biotransformation of steroids by fungal biocatalysts has been recognized for many years. There are numerous fungi of the genus Aspergillus which have been shown to transform different steroid substances. The possibility of using filamentous fungi Aspergillus brasiliensis cells in the biotransformation of androsta-1,4-diene-3,17-dione, was evaluated.Methods
The fungal strain was inoculated into the transformation medium which supplemented with androstadienedione as a substrate and fermentation continued for 5 days. The metabolites were extracted and isolated by thin layer chromatography. The structures of these metabolites were elucidated using 1H-NMR, broadband decoupled 13C-NMR, EI Mass and IR spectroscopies.Results
The fermentation yielded one reduced product: 17β-hydroxyandrost-1,4-dien-3-one and two hydroxylated metabolites: 11α-hydroxyandrost-1,4-diene-3,17-dione and 12β-hydroxyandrost-1,4-diene-3,17-dione.Conclusions
The results obtained in this study show that A. brasiliendsis could be considered as a biocatalyst for producing important derivatives from androstadienedione. 相似文献12.
Synthesis was undertaken of 21-chloro-danazol (Ⅳa) and 21-chloro-6-dehydro-danazol (Ⅳb). The binding ability of these compounds to progesterone receptor were examined and were found to be less active than danazol.Compound (Ⅳa) showed significant activity for eary pregnancy termination effect in Sprague-Dawley rats. 相似文献
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运用“违法传递”概念,根据白念珠菌对寡肽的传送特点,设计并合成了8个含L-4-氧代赖氨酸(以下称I-677)和N3-(4-甲氧基富马酰)-L-2,3-二氨基丙酸(以下称FMDP)的寡肽类似物,均系新化合物。体外抗白念珠菌试验表明:I-677-FMDP-肽(I-677-FMDP,I-677-AA-FMDP,其中AA=Nva,Val,Leu,Phe,Pro,D,L-p-Cl- Phe,D-Pgly)是I-677单体摩尔活性的40~770倍,是FMDP的60~1130倍,其摩尔最低抑菌浓度为6.56×10-9~3.5×10-10mol·disk-1。羧肽酶A存在时化合物I-677-FMDP体外抗菌试验表明,含FMDP的化合物I-677-FMDP能抵抗羧肽酶A的酶解。 相似文献
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Since kainate evokes large non-desensitizing currents at α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, kainate is of limited use in discriminating between AMPA and kainate receptors. Following recent reports that (2S,4R)-4-methylglutamate is a kainate receptor-selective agonist, we have radiolabelled and subsequently characterized the binding of [3H]-(2S,4R)-4-methylglutamate to rabbit whole-brain membranes. [3H]-(2S,4R)-4-methylglutamate binding was rapid, reversible and labelled two sites (KD1 = 3.67 ± 0.50 nM/Bmax1 = 0.54 ± 0.03 pmol/mg protein and KD2 = 281.66 ± 12.33 nM/ Bmax2 = 1.77 ± 0.09 pmol/mg protein). [3H]-(2S,4R)-4-methylglutamate binding was displaced by several non-NMDA receptor ligands: domoate > kainate
-quisqualate
-glutamate > 6-cyano-7-nitroquinoxaline-2, 3-dione (CNQX) (S)-AMPA = (S)-5-fluorowillardiine > NMDA. Neither the metabotropic glutamate receptor agonists (1S,3R)-ACPD or
-AP4, together with the
-glutamate uptake inhibitor
-trans-2,4-PDC, influenced binding when tested at 100 μM. We conclude that [3H]-(2S,4R)-4-methylglutamate is a useful radioligand for labelling kainate receptors. It possesses high selectivity, and possesses a pharmacology similar to that for rat cloned low-affinity (Glu5 and 6) kainate receptor subunits. 相似文献
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本文报道以N-[1-(对-溴苯甲酰甲基)-3-甲基-4-哌啶基]-N-丙酰苯胺(Ⅲ)为前体,以PdO/BaSO4作催化剂,用氚气进行卤—氚置换,氚化还原羰基的反应。反应产物经硅胶纸层析纯化后,用甲基橙比色法定量测定,得到N-{1-[β-羟基-β-氚-β-(对-氚苯基)乙基]-3-甲基-4-哌啶基}-N-丙酰苯胺(Ⅳ,[3H]F-7302),其比放射性为59 Ci/mM,放化纯度为98%。[3H]F-7302与小鼠脑内阿片受体的特异性结合在浓度为4.5×10-9M时达到饱和,解离常数Kd=1.25×10-9M,最大结合量Bmax=93.08×1012M/g蛋白,其特异性结合与非特异性结合比值达10~15。 相似文献
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3, 4-Dichloro-N-methyl-N-[trans-2- (1-△3-pyrrolinyl)-cyclohexyl]-benzenacetamide hydrochloride (K-Ⅱ) was synthesized from N-methyl-7-azabicyclo [4.1.0] heptane by treatment with 2,5-dihydropyrrole to give N-[trans-2(1-△3-pyrrolinyl)-cyclohexyl]-N-methylamine which was amidated with 3,4-dichlorophenyl-acetic acid. K-Ⅱ is an analogue of U-50488 H(K-Ⅰ), a known kappa receptor agonist.The results of animal tests showed that K-Ⅱ is 3 times as potent as K-Ⅰ as an analgesic in the mouse hot plate test and 5 times in the mouse writhing test and that the affinity of K-Ⅱ for kappa receptor may be higher than that of K-Ⅰ. The general behavioural effects of these two agents are similar in mice. 相似文献
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Pertwee RG 《British journal of pharmacology》2008,153(2):199-215
Cannabis sativa is the source of a unique set of compounds known collectively as plant cannabinoids or phytocannabinoids. This review focuses on the manner with which three of these compounds, (-)-trans-delta9-tetrahydrocannabinol (delta9-THC), (-)-cannabidiol (CBD) and (-)-trans-delta9-tetrahydrocannabivarin (delta9-THCV), interact with cannabinoid CB1 and CB2 receptors. Delta9-THC, the main psychotropic constituent of cannabis, is a CB1 and CB2 receptor partial agonist and in line with classical pharmacology, the responses it elicits appear to be strongly influenced both by the expression level and signalling efficiency of cannabinoid receptors and by ongoing endogenous cannabinoid release. CBD displays unexpectedly high potency as an antagonist of CB1/CB2 receptor agonists in CB1- and CB2-expressing cells or tissues, the manner with which it interacts with CB2 receptors providing a possible explanation for its ability to inhibit evoked immune cell migration. Delta9-THCV behaves as a potent CB2 receptor partial agonist in vitro. In contrast, it antagonizes cannabinoid receptor agonists in CB1-expressing tissues. This it does with relatively high potency and in a manner that is both tissue and ligand dependent. Delta9-THCV also interacts with CB1 receptors when administered in vivo, behaving either as a CB1 antagonist or, at higher doses, as a CB1 receptor agonist. Brief mention is also made in this review, first of the production by delta9-THC of pharmacodynamic tolerance, second of current knowledge about the extent to which delta9-THC, CBD and delta9-THCV interact with pharmacological targets other than CB1 or CB2 receptors, and third of actual and potential therapeutic applications for each of these cannabinoids. 相似文献