摘要:
Described herein are pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 individually mean a hydrogen atom or a lower alkyl group, R.sub.3 denotes an azabicyclo group containing a tertiary nitrogen atom, and Y stands for --O-- or --NH--, or salts thereof. Their preparation process and serotonin receptor antagonists containing them as active ingredients are also described.
摘要:
A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkoxy or halogen, and A is lower alkylene, or a pharmacologically acceptable salt thereof, has sympatholytic .alpha.-receptor blocking activity and is useful for the treatment of hypertension.
摘要:
A compound of the formula ##STR1## wherein Z is N or NH, is a single or double bond, R.sub.1 is hydrogen, C.sub.1-20 alkyl or optionally substituted phenyl, A is lower alkylene, R is carboxyl, lower alkoxycarbonyl, ##STR2## or 1-cycloalkyl-tetrazole-5-yl, R.sub.2 is lower alkyl, hydroxy-lower alkyl or optionally substituted phenyl-lower alkyl, R.sub.3 is lower alkyl or cycloalkyl, or R.sub.2 and R.sub.3 together constitute ##STR3## and R.sub.5 and R.sub.6 are hydrogen or optionally substituted phenyl, or a pharmacologically acceptable salt thereof, has platelet aggregation inhibitory activity and/or cyclic AMP/phosphodiesterase inhibitory activity.
摘要:
A screening tool for an antiplatelet agent wherein the tool is a human ADP receptor P2TAC protein, a variation functionally equivalent thereto, or a homologous protein thereof, and a screening tool for an antiplatelet agent wherein the tool is a transformant which is transformed with an expression vector comprising a DNA encoding the protein and is expressing the polypeptide are disclosed. Further, a method for detecting an ADP receptor P2TAC ligand, antagonist, or agonist by using the screening tool for an antiplatelet agent, and a method for screening an antiplatelet agent by the detecting method are disclosed.
摘要:
This invention belongs to the genetic engineering field, and provides novel G protein-coupled receptor family proteins SREB1, SREB2 and SREB3 expressed in the central nervous system, genes coding for these proteins, screening methods using these proteins and so on. As one of the methods for obtaining the G protein-coupled receptor proteins of the present invention, RT-PCR is carried out using mRNA extracted from human or rat brain tissue or brain-derived cells as the template and using two primers interposing the entire portion or a part of the G protein-coupled receptor protein translation region, thereby obtaining cDNA corresponding to the G protein-coupled receptor protein or a part thereof, and the cDNA is integrated into an appropriate expression vector and expressed in a host cell.
摘要:
A convenient screening tool and a convenient screening method for obtaining an agent for treating diabetes, a pharmaceutical composition for treating diabetes, and a process for manufacturing the pharmaceutical composition are disclosed. The screening tool is a G protein-coupled receptor, a variation functionally equivalent thereto, or a homologous polypeptide thereof which promotes insulin secretion under a high glucose concentration by activation, or cells transformed with an expression vector comprising a polynucleotide encoding the above polypeptide and expressing the polypeptide.
摘要:
The invention relates to a convenient screening tool for identifying an agent for treating diabetes. The screening tool is a G protein-coupled receptor, a variant of the G protein-coupled receptor, or a homolog of the G protein-coupled receptor, which promotes insulin secretion under a high glucose concentration by activation. The invention also relates to cells transformed with an expression vector comprising a polynucleotide encoding and expressing the screening tool. The invention provides a convenient screening method for identifying an agent for treating diabetes, pharmaceutical compositions comprising the agent, and a process for manufacturing the pharmaceutical composition.
摘要:
The present invention provides a prophylactic, therapeutic or ameliorative medicament for chronic obstructive pulmonary disease (COPD), cystic fibrosis or pulmonary hypertension. More specifically, the present invention provides: (1) a prophylactic, therapeutic or ameliorative medicament for chronic obstructive pulmonary disorder (COPD), cystic fibrosis or pulmonary hypertension, having an NF-κB decoy as the active ingredient thereof; (2) the NF-κB decoy is an oligonucleotide containing the binding sequence GGGRHTYYC (where R represents either A or G; Y represents either C or T; and H represents either A, C or T); (3) an oligonucleotide wherein the NF-κB binding sequence is GGGATTTCCC or GGGACTTTCC; (4) an oligonucleotide wherein the NF-κB decoy is represented by SEQ ID NO:3; (5) the NF-κB decoy is a double-stranded oligonucleotide; (6) the NF-κB decoy is administered in the form of a fine powder; and (7) the NF-κB decoy fine powder is a dry powder.
摘要:
The invention provides a lipopolysaccharide (LPS) binding protein isolated from horseshoe crab. The LPS binding protein is isolated by (i) extracting the hemocyte membrane fraction of horseshoe crab with a polyethylene glycol ether type nonionic surface active agent in the presence of Ca ions, (ii) combining the extract with immobilized LPS under conditions that permit the LPS binding protein to bind the immobilized LPS to produce an LPS-LPS binding protein complex, and (iii) harvesting the LPS binding protein released from the complex in the presence of a chelating agent. The isolated LPS binding protein has a molecular weight of about 27,000 daltons as determined by SDS polyacrylamide gel electrophoresis and is operative to bind a lipopolysaccharide endotoxin. Accordingly, the isolated LPS binding protein can be used for detecting endotoxin and/or removing endotoxin from an injectable medicine.
摘要:
Antibiotic neplanocin A of the formula ##STR1## is produced by culturing Ampullariella sp. A 11079 FERM-P No. 4494 in a nutrient medium and then separating the neplanocin A thus produced from the culture medium.
摘要翻译:通过培养Ampullariella sp产生式的抗生素neplanocin A。 A 11079FERM-P No.4494在营养培养基中,然后从培养基中分离出由此产生的neplanocin A.