35 results about "Calcium influx" patented technology

Methods are disclosed utilizing the optically pure (-) isomer of amlodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the racemic mixture of amlodipine. The (-) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of (-) amlodipine as a calcium channel antagonist such as cerebral ischemia, cerebral disorders, arrhythmias, cardiac hypertrophy, coronary vasospasm, myocardial infarction, renal impairment and acute renal failure, without the concomitant liability of adverse effects associated with the racemic mixture of amlodipine.

Cosmetic compositions comprising a metal-complexed peptide fraction of stressed yeast extracts and / or a calcium influx inhibitor are disclosed, as well as methods of using such compositions to impart exfoliating, anti-aging, anti-lipid, anti-inflammatory, and / or lightening benefits to the skin; and / or lightening benefits to the hair. These compositions are believed to have modulatory activity against at least one biochemical pathway implicated in skin aging, inflammation, lipid synthesis, and melanin production.

The present invention is based on the discoveries that PAN-811 (1) reduces infarct volume, suppresses brain edema and decreases mortality associated with ischemia; (2) blocks veratridine-induced swelling and neuronal cell death; (3) chelates free calcium and inhibits MMP-9 activity; and (4) blocks calcium-induced neuronal cell death and suppresses glutamate-induced calcium influx into neuronal cells. More particularly, the present invention relates to methods for treating, ameliorating or preventing vasogenic and / or cytotoxic brain edema, by administering to a subject in need thereof certain thiosemicarbazone compounds or pharmaceutically acceptable salts thereof. An example of such a thiosemicarbazone is 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (PAN-811).

The present invention concerns the use of calcium influx inhibitors for treatment of organs and tissues to inhibit damage caused by ischemia / reperfusion events such as transplant, other surgeries, and trauma. It includes methods and apparatuses for achieving stasis in tissue, so as to preserve and / or protect them. In specific embodiments, preservation methods and apparatuses for preserving tissue for transplantation purposes is provided.

The invention relates to sperm motility fluid and a preparation method thereof, belonging to the technical field of human assisted reproduction. The sperm motility fluid is prepared by dissolving ATPsodium salt, dried heparin sodium powder / heparin sodium salt solution into a salt solution containing antibiotics and indicators. The ATP sodium salt and the heparin sodium are added into the sperm motility fluid disclosed by the invention, the ATP sodium salt can provide energy substances for sperm motility and contribute to sperm middle-piece mitochondria capacity, the heparin can activate a receptor-coupled signal transduction system by binding with a receptor on the sperm surface, the capacity function and calcium influx of the sperm mitochondria are gently and effectively improved, and the sperm motility is further improved. Therefore, the sperm motility can be effectively improved, the capacity of the sperm middle-piece mitochondria is wakened and activated, and the success rate of intra-uterine insemination (IUI) is improved. Moreover, a powerful guarantee is provided for the safety of an assisted reproductive technology.

The subjects of the present invention are to provide a method of screening a compound or a polypeptide which inhibits the activity of AST, or inhibits PAR activation, mucus production promotion, cell proliferation, intracellular calcium influx or EGFR pathway activation due to AST, and further to provide a method of assaying AST in vivo and in biological cells or samples. The present invention further includes the following inventions. ASTs whose each is protein comprising the whole amino acid sequence represented by SEQ ID NO: 1 or 2 or a part thereof or a mammalian AST protein having a 66% or more homology with the amino acid sequence represented by SEQ ID NO: 1 and in whose each a propeptide moiety is bound to a trypsin-like protein moiety via a disulfide bond. Nucleic acids encoding the same. Antibodies binding to the same. A method for assaying AST by using these antibodies. Further a method of assaying the inhibitory activity of a compound or a polypeptide to be assayed against AST or PAR activation, mucus production promotion, cell proliferation, intracellular calcium influx or EGFR pathway activation due to the AST.

Transforming growth factor-beta1 (TGF-β1) mediates expression of collagen 1A2 (Col 1A2) gene via a synergistic cooperation between Smad2 / Smad3 and Sp1, both act on the Col 1A2 gene promoter. The present invention discloses a method for inhibiting liver fibrosis via a retinoic acid derivative primarily extracted from the mycelia of Phlellinus linteus. The retinoic acid derivative can antagonize TGF-β-induced liver fibrosis through regulation of ROS and calcium influx, decreasing the promoter activity of Col 1A2, hindering the translocalization of phosphorylated Smad2 / 3-Smad4 complex from cytosol into nucleus and inhibiting Sp1 binding activity.

The invention provides a preparation method and application of radix astragali saponin. The preparation method of radix astragali saponin comprises the following steps: (1) adding water to radix astragali, extracting by decoction, filtering, and concentrating the filtrate; (2) adding ethanol to precipitate, and standing; (3) recovering the ethanol from the supernatant, diluting with water, injecting into macroporous adsorbent resin columns, and sequentially eluting with water, a 20% (volume / volume) ethanol water solution and a 70% (volume / volume) ethanol water solution; and (4) removing the ethanol in the eluent of the 70% (volume / volume) ethanol water solution, and drying to obtain the radix astragali saponin. The research indicates that the radix astragali saponin can activate the vascular endothelial cell NO-cGMP system, inhibit the calcium influx of vascular smooth muscle cells, and open the K[Ca] and K[ATP] channels, thereby relaxing the smooth muscles, especially vascular smoothmuscles; and therefore, the radix astragali saponin has an obvious function of vasodilatation, and is suitable for preventing and treating cardiovascular diseases, such as lowering the blood pressure, resisting angina pectoris and the like.

The present invention provides store operated calcium influx inhibitor compounds, pharmaceutical compositions, and methods of use. The compounds are useful for treating an inflammatory disease or treating an inflammatory reaction. Preferably, compounds, compositions and methods of this invention are used for treatment of inflammatory skin, pulmonary, musculoskeletal, and gastrointestinal diseases, as well as autoimmune disorders, transplantation treatment, and osteoporosis.

A method for treating a mammal comprises administering at least one of a gene, enzyme and pharmaceutical which modulates the concentration of iPLA2β through transcriptional and / or translational regulation or effectively modulate the inhibition of iPLA2β through calmodulin or derivatives thereof.

The present invention pertains to methods to promote outgrowth of, or extension across a substrate of, neuronal cells by inhibiting the interaction between the cytoplasmic tail of the L1-CAM cell surface adhesion molecule and the cytoskeletal protein ankyrin. The invention also pertains to a method to treat diseases characterized by axonal damage such as spinal cord injury, traumatic brain injury, stroke, and neurodegenerative disease by administration of novel peptides that inhibit the binding of the L1-CAM cytoplasmic tail to ankyrin, and to pharmaceutical compositions comprising such peptides. The invention further pertains to a method of blocking calcium flux to protect against neural cell death following stroke or traumatic head injury.

Available evidence indicates that tumor cells exhibit consistent abnormalities in Calcium influx and intracellular storage of sequestered Calcium when compared to normal cells. The present invention provides clinical methods by which such differences are exploited to induce Apoptosis selectively in tumor cells while sparing normal cells. These methods are based upon employing drugs that, acting alone or in synergistic combinations, produce an increase in intracellular Calcium loading such that either or both of two major Apoptotic pathways are triggered to produce selective killing of malignant cells. Since the invention is based upon fundamental cell cycle requirements, to the extent that Calcium handling abnormalities are a general characteristic of the malignant state, the methods presented here are widely applicable regardless of tissue of origin and degree of cellular de-differentiation.

The present invention relates to amantadine nitrate compounds having neural protective effect, and preparation method and medical use thereof. The compounds have the structure of the general formula (I).The compounds have multifunctional mechanisms, including inhibiting NMDA receptors, releasing NO, inhibiting calcium influxes, and having protective effects on cells particularly neurocytes. The compounds can be used in the preparation of medicaments having a cellular protective effect, for prevention or treatment of the diseases related to such as NMDA receptors and elevation of calcium anions in cells, including the diseases related to neurodegeneration such as Alzheimer's disease, Parkinson's disease, cerebral paralysis and glaucoma, and the diseases related to cardio-cerebral-vascular system such as Parkinson's syndrome combined with cerebral arteriosclerosis, as well as respiratory tract infections caused by influenza virus.

The invention discloses a CMKLR1 antagonistic polypeptide and derivatives and application thereof, and particularly relates to analogs of the CMKLR1 antagonistic polypeptide shown in sequences SEQ IDNO.1-21 and derivatives thereof. The derivatives of the binding peptide are products obtained after conventional modification of amino terminals or carboxyl terminals on CMKLR1 binding peptide amino acid side chain groups and CMKLR1 antagonistic polypeptide fragments or products obtained by bonding labels for polypeptide or protein detection or purification with the CMKLR1 antagonistic polypeptide. The binding peptide and the derivatives thereof can be bonded with CMKLR1 in vitro, and by blocking the bond of chemerin / RvE1 and CMKLR1, cAMP concentration increase is promoted, calcium influx caused by chemerin is inhibited, cell chemotaxis caused by chemerin is inhibited, and effective small-molecular treatment drugs are provided for high-expression CMKLR1 receptor diseases such as breast cancer and polycystic ovarian syndrome.

The invention discloses a CMKLR1 antagonistic polypeptide and a derivative and application thereof and particularly relates to a CMKLR1 antagonistic polypeptide shown in SEQ ID No.1-9 and a derivativethereof. The derivative of the binding peptide is a product obtained in the mode that conventional modification is conducted on a CMKLR1 binding peptide amino acid side chain group and an amino terminal or a carboxyl terminal of a CMKLR1 antagonistic polypeptide fragment or a product obtained in the mode that a label for detection or purification of polypeptide or protein is linked to the CMKLR1antagonistic polypeptide. The binding peptide and the derivative thereof can be combined with CMKLR1 in vitro, by stopping combination of chemerin / RvE1 and CMKLR1, the cAMP concentration is changed, the calcium influx caused by chemerin and cell chemotaxis caused by chemerin are inhibited, and effective micromolecule treatment drugs are provided for diseases of high-expression CMKLR1 receptors.

The invention provides a manidipine hydrochloride compound. Manidipine hydrochloride is a lipophilic third generation dihydropyridine calcium channel blocker, and is mainly used for inhibiting calcium influx by inhibiting L type calcium channels on vascular smooth muscle, so as to realize relaxation of vascular smooth muscle and reduce blood pressure.

The invention belongs to the field of health foods, and discloses nutritious fine dried ganoderma-lucidum noodles and a preparation method thereof. The nutritious fine dried ganoderma-lucidum noodlesare prepared from the following raw materials in parts by weight: 70-80 parts of wheat flour, 10-15 parts of soybean powder, 5-8 parts of skimmed milk powder, 4-6 parts of walnut powder, 8-10 parts ofganoderma lucidum liquid, 1-3 parts of red-rooted salvia root extract, 0.5-1 part of eleutheroside, 0.5-1 part of gastrodine, 4-6 parts of eggs, 0.2-0.4 part of CMC , 1-2 parts of edible salt, and 0.1-0.3 part of edible alkali. The soybean powder, the walnut powder and the skimmed milk powder are used as auxiliary materials of the nutritious fine dried ganoderma-lucidum noodles; and functional ingredients, including the gastrodine, the eleutheroside, the red-rooted salvia root extract, the ganoderma lucidum liquid and the like, are added so that the nutritious fine dried ganoderma-lucidum noodles have improved nutritional values, and are capable of regulating content of brain neurotransmitter so as to delay epileptic seizures and reduce degree of attack by blocking calcium influx. And thus, the nutritious fine dried ganoderma-lucidum noodles have certain effects on resisting epilepsy.

The invention discloses a CMKLR1 antagonistic polypeptide and a derivative and application thereof and particularly relates to a CMKLR1 antagonistic polypeptide shown in SEQ ID No.1-24 and a derivative thereof. The derivative of the binding peptide is a product obtained in the mode that conventional modification is conducted on a CMKLR1 binding peptide amino acid side chain group and an amino terminal or a carboxyl terminal of a CMKLR1 antagonistic polypeptide fragment or a product obtained in the mode that a label for detection or purification of polypeptide or protein is linked to the CMKLR1antagonistic polypeptide. The binding peptide and the derivative thereof can be combined with CMKLR1 in vitro, by stopping combination of chemerin / RvE1 and CMKLR1, increase of the cAMP concentrationis promoted, the calcium influx caused by chemerin and cell chemotaxis caused by chemerin are inhibited, proliferation of ovarian carcinoma cells can be inhibited, apoptosis of the ovarian carcinoma cells is promoted, and effective micromolecule treatment drugs are provided for female reproductive diseases such as ovarian cancer.

The present invention relates to methods of inhibiting capillary endothelial (CE) cell migration, the formation of CE networks and angiogenesis, and uses thereof for the purpose of treating angiogenesis-related diseases and disorders, particularly when the diseases or disorders are directly related aberrant angiogenesis. Inhibition is achieved by inhibiting TRPV4 activity, such as the levels of TRPV4 expression, calcium influx through TRPV4, and / or the intracellular signaling from TRPV4 via β1 integrin activation.

The present invention relates to methods of inhibiting capillary endothelial (CE) cell migration, the formation of CE networks and angiogenesis, and uses thereof for the purpose of treating angiogenesis-related diseases and disorders, particularly when the diseases or disorders are directly related aberrant angiogenesis Inhibition is achieved by inhibiting TRPV4 activity, such as the levels of TRPV4 expression, calcium influx through TRPV4, and / or the intracellular signaling from TRPV4 via β1 integrin activation.

The invention discloses a CMKLR1 antagonistic polypeptide and derivatives and application thereof, and particularly relates to analogs of the CMKLR1 antagonistic polypeptide shown in sequences SEQ IDNO.1-17 and derivatives thereof. The derivatives of the binding peptide are products obtained after conventional modification of amino terminals or carboxyl terminals on CMKLR1 binding peptide amino acid side chain groups and CMKLR1 antagonistic polypeptide fragments. The binding peptide and the derivatives thereof can be bonded with CMKLR1 in vitro, and by blocking the bond of chemerin and CMKLR1, cAMP concentration increase is promoted, calcium influx caused by chemerin is inhibited and cell chemotaxis caused by chemerin is inhibited. Besides, proliferation of ovarian cancer cells can be inhibited, the cell cycle is blocked, apoptosis of the ovarian cancer cells is promoted, and effective small-molecular treatment drugs are provided for female reproductive diseases such as ovarian cancer.

The invention provides a TRPV4-His499 protein sensitive to magnetic force, a magnetic regulation tool and application, and relates to the technical field of system nerve science. TRPV4-His499 proteinis capable of sensing magnetic fields and being activated with the aid of functionally modified magnetic nanoparticles, followed by triggering cellular calcium influx for neurocalcium signaling. The specific operation is as follows: inserting a 6*his label at the 499th position amino acid position of the TRPV4 protein to obtain the TRPV4-His499 protein sensitive to magnetic force, transferring theTRPV4-His499 protein into the brain of a mouse by using virus, simultaneously injecting magnetic nanoparticles wrapped by anti-His antibodies, and inducing cell calcium influx under the action of a magnetic field, can be used for conducting nerve calcium signal and regulating mouse behaviors.

The invention belongs to the field of healthcare foods, and discloses glossy ganoderma nutritive fine dried noodles and a preparation method thereof. The fine dried noodles include, by weight, 70-80 parts of wheat flour, 10-15 parts of soybean powder, 5-8 parts of skim milk powder, 4-6 parts of walnut powder, 8-10 parts of glossy ganoderma liquid, 1-3 parts of danshen root extract liquid, 0.5-1 part of eleutheroside, 0.5-1 part of gastrodine, 4-6 parts of eggs, 0.2-0.4 part of CMC, 1-2 parts of table salt, and 0.1-0.3 part of sodium carbonate. The soybean powder, the walnut powder and the skimmilk powder are adopted as auxiliary materials and the gastrodine, the eleutheroside, the danshen root extract liquid, the glossy ganoderma liquid and other functional components are added, and therefore, nutrition value of the noodles is improved, and through regulation of the brain neurotransmitter content, outbreak of epilepsy is delayed by calcium influx blocking and the degree of outbreak isreduced, so that the fine dried noodles have a certain anti-epileptic function.

The invention discloses application of SKF96365 in preparation of a medical composition for treating cerebral angiospasm. According to the invention, a cisterna magna primary blood injection method rat SAH model is adopted to disclose TRPC (Transient Receptor Potential Canonical)1 and TRPC4 expression up-regulation of vascular wall after SAH. The activating level is closely associated with the pathologic change degree of spasm vascular wall in expression time phase, so as to indicate that TRPC1 and TRPC4 participate in occurrence and development of CVS (Cerebral Vascular Spasm). A TRPC channel paralyser SKF96365 is used to prevent and treat cerebral vascular spasm, and the TRPC channel is paralyzed to limit calcium influx of smooth muscle cell, so that the degree of lumen stenosis and lumen thickening can be partially relieved, and a certain treating effect is shown.

The invention provides a preparation method and application of radix astragali saponin. The preparation method of radix astragali saponin comprises the following steps: (1) adding water to radix astragali, extracting by decoction, filtering, and concentrating the filtrate; (2) adding ethanol to precipitate, and standing; (3) recovering the ethanol from the supernatant, diluting with water, injecting into macroporous adsorbent resin columns, and sequentially eluting with water, a 20% (volume / volume) ethanol water solution and a 70% (volume / volume) ethanol water solution; and (4) removing the ethanol in the eluent of the 70% (volume / volume) ethanol water solution, and drying to obtain the radix astragali saponin. The research indicates that the radix astragali saponin can activate the vascular endothelial cell NO-cGMP system, inhibit the calcium influx of vascular smooth muscle cells, and open the K[Ca] and K[ATP] channels, thereby relaxing the smooth muscles, especially vascular smoothmuscles; and therefore, the radix astragali saponin has an obvious function of vasodilatation, and is suitable for preventing and treating cardiovascular diseases, such as lowering the blood pressure, resisting angina pectoris and the like.

The invention discloses a CMKLR1 antagonistic polypeptide and a derivative and application thereof and particularly relates to a CMKLR1 antagonistic polypeptide shown in SEQ ID No.1-15 and a derivative thereof. The derivative of the binding peptide is a product obtained in the mode that conventional modification is conducted on a CMKLR1 binding peptide amino acid side chain group and an amino terminal or a carboxyl terminal of a CMKLR1 antagonistic polypeptide fragment or a product obtained in the mode that a label for detection or purification of polypeptide or protein is linked to the CMKLR1antagonistic polypeptide. The binding peptide and the derivative thereof can be combined with CMKLR1 in vitro, by stopping combination of chemerin / RvE1 and CMKLR1, the cAMP concentration is changed,the calcium influx caused by chemerin and cell chemotaxis caused by chemerin are inhibited, proliferation of ovarian carcinoma cells can be inhibited, apoptosis of the ovarian carcinoma cells is promoted, and effective micromolecule treatment drugs are provided for female reproductive diseases.

The present invention discloses benzimidazolone compounds represented by formula I, or pharmaceutically acceptable salts thereof. Results of citric acid-induced guinea pig cough model effect test, capsaicin-induced mouse cough inhibition test, influences of the benzimidazolone compounds on guinea pig allergic asthma and calcium influx test of vanilloid receptors show that the compounds exhibit good antitussive and antiasthmatic effects by inhibiting vanilloid receptor 1.

The present invention discloses a CMKLR1 antagonistic polypeptide and its derivatives and applications, in particular to the sequence SEQ ID No. 1-8 and its derivatives, wherein the derivatives of the polypeptide are CMKLR1 polypeptide amino acid side chain groups, CMKLR1 antagonistic polypeptides The product obtained by conventional modification of the amino-terminus or carboxyl-terminus of the fragment, or the product obtained by linking a tag used for polypeptide or protein detection or purification on the CMKLR1 antagonistic polypeptide; the polypeptide and its derivatives can bind to CMKLR1 in vitro, and through blocking Breaking the combination of chemerin / RvE1 and CMKLR1 changes cAMP concentration, inhibits calcium influx caused by chemerin, and inhibits cell chemotaxis caused by chemerin, providing an effective small molecule drug for the treatment of diseases with high expression of CMKLR1 receptors, which can be used in medicine and biology. widely used in the field of science.