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11.
Y Masuo H Wang D Pélaprat Z Q Chi W Rostène 《Chemical & pharmaceutical bulletin》1992,40(9):2520-2524
We have recently demonstrated that [3H]ohmefentanyl, a non-peptidergic opioid ligand which was suggested to cross the blood brain barrier in contrast to other peptidergic opioid ligands, bound not only to mu opioid receptor sites but also to sigma sites. In order to examine whether [3H]ohmefentanyl can be used as a marker for mu sites, we investigated the effects of brain lesions on [3H]ohmefentanyl binding site densities, as compared with [3H][D-Ala2, MePhe4, Gly-ol5]enkephalin ([3H]DAGO), a selective mu ligand. These binding site densities were measured by quantitative autoradiography in the rat striatum and substantia nigra, two brain structures known to contain a high density of mu receptors, following lesions of the nigro-striatal dopaminergic pathway and striatal intrinsic neurons. Following unilateral nigral lesion with 6-hydroxydopamine, [3H]ohmefentanyl binding site densities were decreased in the patches (-35%) and matrix (-20%) of the ipsilateral striatum and in the lesioned substantia nigra pars compacta (-49%). Unilateral striatal lesion with quinolinic acid induced 72%, 61% and 50% decreases in [3H]ohmefentanyl binding in the patches and matrix of the lesioned striatum and in the ipsilateral substantia nigra pars reticulata, respectively. Similar results were obtained in the binding of [3H]DAGO. Indeed, a significant linear correlation was observed between [3H]ohmefentanyl and [3H]DAGO binding site densities. Therefore, mu opioid receptors may be mainly located on intrinsic neurons in the striatum, dopaminergic cell bodies in the substantia nigra pars compacta and nerve terminals of striatal efferents in the substantia nigra pars reticulata.(ABSTRACT TRUNCATED AT 250 WORDS) 相似文献
12.
Let G: (0, ∞) → (0, ∞) be logarithmically concave on a neighbourhood of ∞ and suppose limx→∞ G(x + δ)/G(x) = 1 for some δ > 0. Then, the functional equation $$g(x+1)=G(x)\cdot g(x),\ \ \ x\in (0,\infty),$$ admits, up to a multiplicative constant, at most one solution g: (0, ∞) → (0, ∞), geometrically convex on a neighbourhood of ∞. Sufficient conditions on G are given, for which also such a unique geometrically convex solution of (D) exists. This result improves the classical theorems of Bohr-Mollerup type and gives a new characterization of the gamma function and the q-gamma function for q ∈ (0, 1). 相似文献
13.
Detlef Gronau 《Results in Mathematics》1993,23(1-2):49-54
Let IK be either IR or ? and D an open set of IK containing 0 and starlike with respect to 0 (i.e. an open interval containig 0 in the case IK = IR). If f: D » IK is a continuous function with fixed point 0, then under certain conditions stated below we can prove for the kn- th iterates of f the following asymptotic formula: 1 $$f^{(kn)}\bigg({x \over n}\bigg )=\sum_{i-1}^r{1\over (nk)^i}\ f_i(kx)+o \bigg({1\over n^r}\bigg),$$ for n » ∞, k, n and r beeing positive integers and x close enough to 0. The functions f i are continuous and uniquely determined by f. In particular (1) holds for any function holomorphic on a neighbourhood of zero, having a convergent power series expansion of the form $$f(z)=z+a_2z^2+\cdots=\sum_{j=1}^\infty\ a_jz^j,\ a_j\in {\cal C},a_1=1,$$ and for any integers k, r with r > 0. 相似文献
14.
Detlef Gabel Claudia Bauer Mohamed E. El-Zaria Afaf R. Genady Udo Drfler 《Journal of organometallic chemistry》2003,680(1-2):23-26
The preparation and properties of the R1R2NH---B8H11NHR cluster are described. The cluster is stable to aqueous solutions and can be made water-soluble by the introduction of a few hydrophilic groups. This makes the cluster a good candidate as the boron moiety in compounds for boron neutron capture therapy. The chemistry of the cluster preparation, the stability of the cluster, and conditions for reactions of the organic moieties are reviewed. Pyridine derivatives of the cluster show electronic interaction between the cluster and the pyridine. 相似文献
15.
The microwave-assisted synthesis of 5-amino-3-aralkoxy(methoxy)amino-1,2,4-oxadiazoles starting from N1-aralkoxy-(methoxy)-N3-cyano-O-phenylisoureas and hydroxylamine is described. N1-Aralkoxy(methoxy)-N3-cyano-O-phenylisoureas are readily accessible by treatment of diphenyl N-cyanimidocarbonate with O-substituted hydroxylamines. 相似文献
16.
Wilfried A. Knig Detlef Icheln Torsten Runge Ingo Pforr Adolf Krebs 《Journal of separation science》1990,13(10):702-707
Transferring the site of specific substitution of dipentylated cyclodextrins with methyl or acyl residues from the secondary 3-hydroxyl group to the primary 6-hydroxyl group was expected to provide new information on the mechanism of chiral recognition. The 3-position points towards and the 6-position points away from the cyclodextrin cavity which via inclusion complex formation is supposed to play a major role in chiral separation. The “inverse” 6-O-acyl-2,3-di-O-pentyl-cyclodextrins displayed almost no enantioselectivity but the corresponding 6-O-methyl derivatives are a versatile supplement to the chiral capillary GC phases nowadays available. Among the compounds that could be enantiomerically resolved are alcohols, amino acids, alkyl halides, bicyclic ethers, acetals, olefins, other hydrocarbons and chiral pharmaceuticals. 相似文献
17.
Dalvit C Mongelli N Papeo G Giordano P Veronesi M Moskau D Kümmerle R 《Journal of the American Chemical Society》2005,127(38):13380-13385
NMR-based binding and functional screening performed with FAXS (fluorine chemical shift anisotropy and exchange for screening) and 3-FABS (three fluorine atoms for biochemical screening) represents a potential alternative approach to high-throughput screening for the identification of novel potential drug candidates. The major limitation of this method in its current status is its intrinsic low sensitivity that limits the number of tested compounds. One approach for overcoming this problem is the use of a cryogenically cooled (19)F probe that reduces the thermal noise in the receiver circuitry. Sensitivity improvement in the two screening techniques achieved with the novel cryogenic (19)F probe technology permits an increased throughput, detection of weaker binders and inhibitors (relevant in a fragment-based lead discovery program), detection of slow binders, and reduction in protein and substrate consumption. These aspects are analyzed with theoretical simulations and experimental quantitative performance evaluation. Application of 3-FABS combined with the cryogenic (19)F probe technology to rapid screening at very low enzyme concentrations and the current detection limits reached with this approach are also presented. 相似文献
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Pentafluorethyl Sulfurtrifluoride: Synthesis and Reactions By oxidation of (C2F5S?)2 ( 1 ) with AgF2 at 0°C a mixture of C2F5SF3 ( 2 ) and C2F5SF5 ( 3 ) besides C2F5S(O)F ( 4 ) is formed. With elemental fluorine only 3 is isolated, an intermediate in this reaction is (C2F5SF4?)2 ( 5 ). At ?40 to ?30°C the mixture of 2, 3 and 4 was reacted with TASF and AsF5, to give TAS+ C2F5SF4? ( 6 ), TAS+ C2F5S(O)F2? ( 7 ) and C2F5SF2+AsF6? ( 8 ), respectively. While 6 and 7 decompose rapidly in solution even at low temperatures, of thermally stable 8 the solid state structure was determined by x-ray diffraction. 相似文献