44 results about "Antagonists drugs" patented technology

An NMDA antagonist (such as ketamine) is administered with a safener (such as clonidine) in patients suffering from neurologic disorders other than pain. The ketamine is adminsitered at a dosage that causes slurred speech, for a span of several days. This treatment enables a patient's nervous system to return to a healthy “set point”, also called an improved stable neural homeostasis, in a manner similar to a broken bone healing itself if protected from jostling and reinjury by a cast. In at least some patients, this treatment can ease problems such as addictions to illegal or pain-killing drugs, nicotine, or alcohol, compulsive or criminal behavioral problems, severe depression, obsessive-compulsive disorders, phobias, etc. It may also provide some relief in some patients for problems such as chronic fatigue, chemical sensitivities, allergies, autoimmune disorders, and diabetes.

A drug that inhibits NMDA receptors (such as ketamine, a surgical anesthetic) is continuously administered to patients suffering from neuropathic pain. Unless the NMDA antagonist drug has inherent safening activity, this treatment requires a “safener” drug to prevent the neurotoxic side effects of NMDA antagonists. One class of safener drugs that increase the efficacy of the treatment include alpha-2 adrenergic agonists, such as clonidine. The treatment lasts for several days and nights, continuously. A maximum tolerated dosage is titered for each patient, such as by observing slurring of speech, and the patient does not lose consciousness except during normal sleep. Magnesium and / or drugs that inhibit ketamine-degrading enzymes can also be used. Patients who suffered for years from chronic intractable pain emerged from this treatment with apparently permanent relief, or with lasting reductions in their levels of pain.

The invention relates to a compound for treating hypertensive, particularly relating to a calcium ion antagonist drug complex with full dissolution, good stability and high bioavailability. The invention is characterized in that the complex contains (A) calcium channel antagonist, (B) alkaline excipient with effective dose and (C) non-ionic surfactant; wherein (A):(B):(C) is ranged from 0.1:1:1 to 10:1:1.

A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and / or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.

The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist. The invention provides methods for treating psychiatric condition or disorder or the symptoms thereof, including acute anxiety and panic comprising administering a pharmaceutical composition consisting essentially of a beta adrenergic receptor antagonist drug and an antiemetic muscarinic receptor antagonist drug in a therapeutically effective amount to stop or reduce the symptoms of anxiety and / or panic. The pharmaceutical compositions are administered as treatments immediately in advance of, at the onset of, or during an acute anxiety and / or panic episode.

The invention relates the method for forecasting the drug-effect. The method measures the polymorphism gene type to forecast the drug-effect of calcium antagonist drug. The method forecasts the drug-effect of calcium antagonist drug by measuring the polymorphism gene type of key enzyme gene on the aminothiopropionic acid metabolism path.; at the mean time, according to the effect, prepare the compound drug which can improve the drug-effect of calcium antagonist by adjusting the preparation of aminothiopropionic acid metabolism path. The invention improves the effective rate of clinical drug therapeutics and the safety of clinical drug, and reduces the drug toxin side effect and cost.

The invention relates to 1,2,3,4-tetrahydroquinoline compound and a synthetic method and application thereof. In a structure formula of the compound, the R1 is nitro or trifluoromethyl or 3-nitrophenylnitrobenzene sulfonyl or cyano, the R2 is hydrogen or methyl, the R3 is methyl formate or butyl formate, and the R4 is methyl. An aromatic ring of the 1,2,3,4-tetrahydroquinoline compound contains a series of electron withdrawing groups. The synthetic method is simple, economical, environment-friendly, easy to operate, easy to control, higher in product purity and yield and good in development prospect in industrial production; in addition, the synthetic method is also a novel synthetic method in atom economy; furthermore, the 1,2,3,4-tetrahydroquinoline compound can serve as intermediate to be used for preparing antagonist medicine.

Prolonged administration of subanesthetic dosages of ketamine, which suppresses activity at NMDA receptors, can provide a damaged central nervous system with an opportunity to use its innate healing processes to “reset” NMDA receptors which were pushed into an unwanted hyper-sensitized state by unusually high activity. However, such treatments can cause permanent brain damage, if the ketamine dosage is too heavy or prolonged. Certain types of “safener” drugs have previously been identified, which can block or at least reduce those unwanted side effects. It is disclosed that if two classes of safener drugs are combined, which will simultaneously suppress activity at both (i) muscarinic acetylcholine receptors, and (ii) the kainate and AMPA classes of glutamate receptors, those safener drug combinations can provide exceptionally potent and reliable safening activity, which can enable the safe use of potent NMDA antagonist drugs for a number of highly beneficial purposes.

The present invention describes novel compounds of the formula:(Q)d-Ln-Ch,useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.

Molecular cloning and expression of a prostaglandin F2alpha receptor which is linked to the signal transduction pathways via guanine nucleotide binding regulatory (G) proteins and measured by, for example, cAMP, IP3 or intracellular calcium. By constructing cell lines that express a prostaglandin F2alpha receptor, the affinities and efficacies of agonist and antagonist drugs with the receptor can be assessed. A recombinant DNA construct includes a vector and a DNA fragment encoding a prostaglandin F2alpha receptor. A host cell is transformed with a recombinant DNA construct, so that the DNA fragment is expressed and a prostaglandin F2alpha receptor is produced. Suitable host systems include eukaryotic and prokaryotic cells, especially mamalian cells such as rat or human. Additionally, for diagnostic purposes, antibodies to a prostaglandin F2alpha receptor can be prepared by producing all or a portion of the receptor protein and injecting these into various types of mammals. Using the resulting antibodies, expression of an F2alpha receptor cDNA, i.e. receptor protein in tissue and cells can be measured.

The invention discloses an application of a compound NSC-156529 in preparation of a T-type calcium channel antagonist. The compound inhibits the T-type calcium channel current in a dose-dependent manner through non-G-protein and non-Akt dependent ways. The T-type calcium channel antagonist drug containing the NSC-156529 structure can be constructed to be used for treating or preventing neuropsychiatric diseases (such as primary tremor, prosopalgia, cancer pain, schizophrenia, epilepsy, Parkinson's disease and depression) and reproductive diseases (such as varicocele infertility and sexual dysfunction) related to T-type calcium channel dysfunction.

The invention relates the method for forecasting the drug-effect. The method measures the polymorphism gene type to forecast the drug-effect of calcium antagonist drug. The method forecasts the drug-effect of calcium antagonist drug by measuring the polymorphism gene type of key enzyme gene on the aminothiopropionic acid metabolism path.; at the mean time, according to the effect, prepare the compound drug which can improve the drug-effect of calcium antagonist by adjusting the preparation of aminothiopropionic acid metabolism path. The invention improves the effective rate of clinical drug therapeutics and the safety of clinical drug, and reduces the drug toxin side effect and cost.

A pharmaceutical composition comprising a therapeutically effective amount of: (a) dipyridamole or a pharmaceutically acceptable salt thereof; (b) acetylsalicylic acid; and (c) an angiotensin II antagonist, kits containing these three compounds, and methods for preventing stroke or reducing the risk of stroke or secondary stroke in a patient in need thereof by administering an effective amount of these compounds to the patient.

The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist. The invention provides methods for treating psychiatric condition or disorder or the symptoms thereof, including acute anxiety and panic comprising administering a pharmaceutical composition consisting essentially of a beta adrenergic receptor antagonist drug and an antiemetic muscarinic receptor antagonist drug in a therapeutically effective amount to stop or reduce the symptoms of anxiety and / or panic. The pharmaceutical compositions are administered as treatments immediately in advance of, at the onset of, or during an acute anxiety and / or panic episode.

The invention relates to the technical field of calcium antagonist medicines, and discloses a composition containing nimodipine, a preparation method and application thereof. The composition containing nimodipine comprises the following components in mass concentration: 0.02-1 percent of nimodipine, and 0.2-3 percent of surfactant, wherein the pH value of the composition containing nimodipine is in a range of 6.5-8.5. Stimulating ethanol is not adopted in the composition containing nimodipine, so that the dosing risk of the composition containing nimodipine can be reduced, and the stability of the composition containing nimodipine can be improved.

The present invention is focused primarily toward pro re nata (“as needed”) treatments for a psychiatric condition or disorder or the symptoms thereof, including the symptoms of acute anxiety and panic in living animals, including humans. The present invention encompasses pharmaceutical compositions as combination therapies containing at least one beta adrenergic receptor antagonist and at least one muscarinic receptor antagonist. The invention provides methods for treating psychiatric condition or disorder or the symptoms thereof, including acute anxiety and panic comprising administering a pharmaceutical composition consisting essentially of a beta adrenergic receptor antagonist drug and an antiemetic muscarinic receptor antagonist drug in a therapeutically effective amount to stop or reduce the symptoms of anxiety and / or panic. The pharmaceutical compositions are administered as treatments immediately in advance of, at the onset of, or during an acute anxiety and / or panic episode.

The invention relates to applications of a chalcone compound in preparation of farnesoid X receptor (FXR) antagonist drugs, and specifically relates to applications of a multi-hydroxy (multi-methoxy) substituted chalcone compound represented by formula I or a pharmaceutically acceptable salt thereof in preparation of farnesoid X receptor (FXR) antagonists and drugs used for preventing and treating diabetes mellitus type 2. The chalcone compound possesses antagonistic action on CDCA (chenodeoxycholic acid and FXR endogenous ligands)-induced farnesoid X receptor activation, is capable of reducing blood glucose and triglyceride of mice, and possesses application potentialities in treating diabetes mellitus type 2.

The invention belongs to the technical field of biology, and particularly relates to a high-affinity peptide for a tumor necrosis factor alpha and an application of the high-affinity peptide. An amino acid sequence of the peptide is as shown in SEQ. ID. NO.1 and SEQ. ID. NO.3 or single or multi-repeated tandem or branched peptide molecular sequences in the SEQ. ID. NO.1 and the SEQ. ID. NO.3 and the amino acid sequence is as shown in SEQ. ID. NO.4; and the peptide can be combined with the tumor necrosis factor alpha at high affinity and is capable of antagonizing the function. An animal is directly injected with the peptide, so that the occurrence degree of inflammation of an animal body can be significantly reduced and the resistivity of the animal body on an inflammatory injury can be improved. The peptide can be used for developing an antagonist drug for the tumor necrosis factor alpha and treating body damages caused by various acute and chronic inflammations, such as autoimmune and stress damages caused by various physical, chemical and biological factors, and has an extremely wide application prospect, small in molecular weight, low in immunogenicity and easy to synthesize, and the side effect and the disadvantages of a traditional monoclonal antibody drug antagonist are avoided.

The present invention provides uses of combined application of a calcium antagonist drug and a 5-HT1A receptor agonist drug in preparation of drugs for treatment and prevention of high blood pressure,and a blood pressure lowering pharmaceutical composition, which comprises a therapeutically effective amount of a calcium antagonist and an active metabolite thereof, a therapeutically effective amount of a 5-HT1A receptor agonist and an active metabolite thereof, and a pharmaceutically acceptable carrier. According to the present invention, through the combined application of the calcium antagonist drug and the 5-HT1A receptor agonist drug, the blood pressure lowering effect can be significantly enhanced, and the side effect of the calcium antagonist can be reduced; and particularly comparedto the combined medication, the application of the compound preparation made of the calcium antagonist and the 5-HT1A receptor agonist as the blood pressure lowering drug can achieve the unexpected blood pressure lowering effect and reduce calcium antagonist induced side effects including constipation and tachycardia.

The invention discloses a GCGR reporter gene stably transfected cell strain and a construction method and application thereof, a cell membrane of the cell strain expresses a GCGR receptor, the cell strain comprises polynucleotide, the polynucleotide has a CRE-bound binding sequence and is connected with a downstream promoter, the promoter is connected with an open reading frame, and the reading frame expresses a reporter gene protein. The inventor constructs a GCGR reporter gene stably transfected cell strain, and develops a biological activity determination method, a biological analysis quantitative method and a neutralizing antibody determination method which are not limited to GCGR agonist and antagonist drugs by using the cell strain. The problems that the detection steps are tedious, the time cost is high, the reagent consumable cost is high, experimental data interpretation is complex, the method is not sensitive enough, the anti-interference capacity is poor, the GCGR activation / antagonism mechanism and effect cannot be completely represented, and is lack of universality.

A portable dual chamber auto-injector configured to store a dry opioid antagonist medicament separately from a liquid component, wherein a user actuated mixing system comprising a movable component to create a fluidic pathway between the first and second chambers and release a portion of energy from a pre-stored energy to drive a displacement mechanism into the first chamber and displace the liquid component into the second chamber and solubilize the opioid antagonist. A needle assembly in fluid communication with the second chamber can be used to transfer the solubilized opioid antagonist.

The invention relates to a dihydroxydibenzo[b,f][1,5]dioxocane compound, a preparation method, a pharmaceutical composition and an application thereof, and belongs to the technical field of chemistry and medicine. The structure of the compound is shown in formula (I): formula (I). The compound is isolated from lichen red snow tea, and can significantly kill and / or inhibit various human cancer cells in vitro. In vivo, it has a significant inhibitory effect on the growth of transplanted tumors in mice. It has synergistic or additive combined anti-tumor effect with clinical anti-tumor drugs. The anticancer effect in vitro has obvious targeting and selectivity. It can affect the cycle distribution, gene expression, signaling pathway and function of cancer cells, and promote the apoptosis of cancer cells. It has no obvious toxicity to animals, and can significantly reduce the toxicity of cisplatin to animals. The compound of formula (I) can be used as a chemotherapeutic drug for human cancer, as a combination drug of other anticancer drugs, a toxicity antagonist drug or a health product for adjuvant cancer treatment.

Provided herein is a sandwich immunoassay for the detection of cross-linked PIIINPs having at least two PIIINP chains linked together by interchain crosslinks, each chain having N protease composed of intact type III procollagen C-terminal neo-epitopes of PIIINP generated by cleavage. A biological sample with cross-linked PIIINP is contacted with a first surface-bound monoclonal antibody, followed by a second monoclonal antibody, both of which are specifically reactive with the neo-epitope in the C-terminal sequence of PIIINP, and then Binding of the second monoclonal antibody was determined. Also provided is a method of assessing the efficacy of an antagonist drug targeting lysyl oxidase by an immunoassay and a kit comprising a solid support bound to a first monoclonal antibody and comprising a second monoclonal antibody.

The invention relates to a compound for treating hypertensive, particularly relating to a calcium ion antagonist drug complex with full dissolution, good stability and high bioavailability. The invention is characterized in that the complex contains (A) calcium channel antagonist, (B) alkaline excipient with effective dose and (C) non-ionic surfactant; wherein (A):(B):(C) is ranged from 0.1:1:1 to 10:1:1.

The invention relates to 1,2,3,4-tetrahydroquinoline compound and a synthetic method and application thereof. In a structure formula of the compound, the R1 is nitro or trifluoromethyl or 3-nitrophenylnitrobenzene sulfonyl or cyano, the R2 is hydrogen or methyl, the R3 is methyl formate or butyl formate, and the R4 is methyl. An aromatic ring of the 1,2,3,4-tetrahydroquinoline compound contains a series of electron withdrawing groups. The synthetic method is simple, economical, environment-friendly, easy to operate, easy to control, higher in product purity and yield and good in development prospect in industrial production; in addition, the synthetic method is also a novel synthetic method in atom economy; furthermore, the 1,2,3,4-tetrahydroquinoline compound can serve as intermediate to be used for preparing antagonist medicine.

The invention relates to the field of new application of known compounds, and particularly discloses an application of a tetrahydroxanthone dimer compound to preparing an alpha1-AR adrenergic receptor antagonist medicine. On the basis of researches, the antagonism effect of the tetrahydroxanthone dimer compound on three adrenoreceptor alpha1-AR subtypes (alpha1A, alpha1B and alpha1D) is found for the first time, wherein the tetrahydroxanthone dimer compound dicerandrol B has the selective antagonism on the adrenoreceptor alpha1B-AR, and can be used for preparing a medicine for blood pressure reduction or benign prostatic hyperplasia treatment.

G protein biosensors comprising mammalian G protein subunits fused to fluorescent proteins emitting a FRET signal expressed in living intact functional cells. The intensity of the FRET signal is strongly responsive to the activation state of the biosensors. The biosensors respond reproducibly to agonist and antagonist drug molecules specific for G protein coupled receptors. The biosensors have utility in identifying and classifying candidate therapeutic drugs as to their therapeutic value.

The invention discloses a process for preparing an intermediate of zafirlukast, and the compound is an important intermediate for preparing the leukotriene antagonist drug zafirlukast. With (5-nitro-1-toluenesulfonyl-1H-indol-3-yl) methyl acetate and 3-methoxybenzoic acid methyl ester as raw materials, under the action of acidified montmorillonite, in an inert solvent In, heat the reaction until the raw materials disappear, filter to obtain 3-methoxy-4-[(5-nitro-1-toluenesulfonyl-1H-indol-3-yl) methyl] methyl benzoate; the above compound Under alkaline conditions, hydrolysis yields the target product. The invention provides a new process route for synthesizing an important intermediate of zafirlukast, which has the technical advantages of simple operation, low reaction cost, high product yield and environmental friendliness, and can meet the demand for large-scale production of pharmaceutical products.

The present invention describes novel compounds of the formula:(Q)d—Ln—Ch,useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.