摘要:
Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2'-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.
摘要:
A firmness measuring device (10) for non-destructive testing of compliant or soft objects, such as fruit, with rough surfaces is disclosed. The device comprises the following components: a fluid supply means (25) with pressure regulating means (30) that define an impulsive air-jet generating unit (20); a means, including accumulator (35), solenoid valve (40) and nozzle (45) to generate an impulsive jet of a fluid, such as air, aimed at the exposed surface of the object (150) under test; a laser (65) to generate a beam of coherent light (75) aimed at the area (155) on the surface of the object (150) under test when impacted by the fluid jet (not shown); a surface-deformation measuring unit (60) having an optical displacement detector (70) to sense the light (80) reflected off of the surface of the object from the incident laser beam (75); an analyzer unit (120) with means to determine the amount of deformation of the surface caused by the fluid jet, as based on the change of input light signal reaching the detector (70); and a controller unit (100) to coordinate the timed release of the impulsive fluid jet with a triggered active functioning of analyzer means near the moment of maximum surface deformation on object (150).
摘要:
Peptides which exhibit antimicrobial activity comparable to certain known antibiotics are provided. These peptides are related in sequence to amino acid sequences within Cathepsin G. A broad spectrum bactericidal peptide disclosed herein is RPGTLCTVAGWGRVSMRRGT (SEQ ID NO:22). It is active against Pseudomonas aeruginosa, Neisseria gonorrhoeae and Staphylococcus aureus. RRENTQQHITARRAIRHPQY (SEQ ID NO:19) and GKSSGVPPEVFTRFVSSFLPWIRTTMR (SEQ ID NO:26) also exhibited potent activity against P. aeruginosa strains, including clinical isolates. IIGGR (SEQ ID NO:1) and IVGGR (SEQ ID NO:2) act against both gram-negative and gram-positive bacterial strains. HPQYNQR (SEQ ID NO:3) and certain related peptides are also active against both gram-negative and gram-positive bacteria, including, but not limited to, strains of Escherichia coli, Neisseria gonorrhoeae, Staphylococcus aureus, Capnocytophage sputigena and Pseudomonas aeruginosa. The peptides of the present invention will be useful in pharmaceutical compositions useful in the treatment of prophylaxis of infections.
摘要:
Apparatus and method for the automated synthesis of DNA segments utilizing multiple reaction columns (11), all of which are open at the inlet end (13) to the atmosphere of a reaction chamber (10). A moveable reagent supply line outlet (12) is positioned adjacent to the column inlet end (13) to apply reagent to each of the columns (11) according to an input sequence of delivery. The delivery sequence is under processor control. Reagents are removed from all columns (11) simultaneously through the application of vacuum (22) at the outlet end (14) of each column (11). The device enables the parallel synthesis of large numbers of different oligonucleotide sequences of different lengths.
标题翻译:ANTAGONISMUS VON HEILMITTELN DES ZENTRALNERVENSYSTEMS DURCH VERABREICHEN DES 4-AMINOPYRIDINS ALLEIN ODER IN ZUSAMMENHANG MIT SONSTIGEN HEILMITTELN。
摘要:
The use of 4-aminopyridine and congeners or derivatives thereof to antagonize drugs which act at or upon central nervous system receptors, especially dopamine receptors, such as butyrophenones and congeners or derivatives thereof. 4-aminopyridine is used above or in combination with other drugs such as naloxone hydrochloride or yohimbine hydrochloride. The use of 4-aminopyridine overcomes the problems of drug overdoses of drugs which act at or upon central nervous system receptors, especially dopamine receptors by reversing the effects of toxic amounts or toxic dosages.
摘要:
The present invention provides compositions and methods for human neural cell production. More particularly, the present invention provides cellular differentiation methods employing an essentially serum free MEDII conditioned medium for the generation of human neural cells from pluripotent and multipotent human stem cells.