64 results about "P2x7 receptor" patented technology

A recombinant or synthetic antibody or fragment thereof, said antibody or fragment thereof including three complementarity determining regions (CDR1L or H, CDR2L or H and CDR3L or H) for forming an antigen binding site that is capable of binding to a non functional P2X7 receptor but not capable of binding to a functional P2X7 receptor.

The present invention relates to the production of anti non functional P2X7 receptor monoclonal antibodies from hybridoma cell lines.

Pharmaceutical compositions and methods are described comprising at least one Y2 receptor-binding peptide, such as peptide YY(PYY), Neuropeptide Y (NPY) or Pancreatic Peptide (PP) and one or more mucosal delivery-enhancing agents for enhanced nasal mucosal delivery of the peptide YY, for treating a variety of diseases and conditions in mammalian subjects, including obesity.

The present invention relates to the production of anti non functional P2X7 receptor monoclonal antibodies from hybridoma cell lines.

Methods and compositions for the downregulation of P2X7 receptor expression or activity are disclosed. Preferred compositions comprise siNA. The methods and compositions are useful in the treatment of diseases characterised by increased 112X7 receptor activity, such as neuronal degeneration, Alzheimer's disease, inflammatory diseases, and some cancers.

Methods and compositions for the downregulation of P2X7 receptor expression or activity are disclosed. Preferred compositions comprise siNA. The methods and compositions are useful in the treatment of diseases characterised by increased 112X7 receptor activity, such as neuronal degeneration, Alzheimer's disease, inflammatory diseases, and some cancers.

The invention relates to an antigen binding site for binding to a P2X7 receptor, the antigen binding site being defined by general formula 1:FR1-CDR1-FR2-CDR2-FR3-CDR3-FR4

The invention relates to purinergic receptors, to antibodies and related fragments thereof for binding to said receptors, to production of said antibodies and fragments and to use of said antibodies and fragments for cancer detection and therapy. In particular the antibodies described bind specifically to non-functional P2X7 receptors expressed by live cells.

The invention relates to producing humoral response to P2X7 receptors in individuals having cancer, and to minimizing the progression of cancer in said individuals.

The invention relates to a novel epitope on P2X7 receptors, to antibodies for binding to the epitope and to peptides for generating the antibodies.

One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and / or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect.

The invention relates to producing humoral response to P2X7 receptors in individuals having cancer, and to minimizing the progression of cancer in said individuals.

The invention relates to purinergic (P2X) receptors, more specifically to P2X7 receptors, the generation of antibodies and the use of antibodies and immunogens that are capable of selectively binding to a non ATP-binding P2X7 receptor but not to an ATP-binding P2X7 receptor, for the detection and treatment of disease conditions, especially cancer.

Y4 receptor agonist peptide selected from the group consisting of: [Ala30]PP2-36, [Thr30]PP2-36, [Asn30]PP2-36, [Gln30]PP2-36, [Glu10]PP2-36, [Glu10,Leu17,Thr30]PP2-36, [Nle17,Nle30]PP2-36, [Glu10,Nle17,Nle30]PP2-36, their PP1-36 equivalents, and analogues and derivatives thereof as described in the specification, are selective agonists of the Y4 receptor relative to the Y1 and Y2 receptors, and are useful in the treatment, for example, of obesity and overweight, and conditions in which these are considered contributory factors, and in the treatment of diarrhoea and intestinal hypersecretion.

The present invention relates to the treatment or prevention of kidney injury and in particular acute kidney injury, such as acute kidney injury associated with cirrhosis. The invention relates to the treatment or prevention of such injury by administration of an agonist of the P2X7 receptor.

The present invention concerns compounds comprising, within short sequences from a specific regions of the 7TM receptor, that can modulate 7TM receptor-associated signal. The present invention further concerns methods for stimulation angiogenesis by administration of peptides derived from the EDG3 7TM-receptor.

The invention discloses a F-18 tagged P2X7 receptor imaging agent which is a compound 18F-{(2-chloro-3-trifluorophenyl)(1-(pyrimidin-2-yl)-6,7-dihydro-1H-[1,2,3]triazolo[4,5-c]pyridin-5(4H)-yl)methanone shown as formula I. The P2X7 receptor imaging agent is suitable for identifying and diagnosing pulmonary inflammation and tumors.

The invention relates to purinergic receptors, to antibodies and related fragments thereof for binding to said receptors, to production of said antibodies and fragments and to use of said antibodies and fragments for cancer detection and therapy. In particular the antibodies described bind specifically to non-functional P2X7 receptors expressed by live cells.

Methods and compositions for the downregulation of P2X7 receptor expression or activity are disclosed. Preferred compositions comprise siNA. The methods and compositions are useful in the treatment of diseases characterised by increased P2X7 receptor activity, such as neuronal degeneration, Alzheimer's disease, inflammatory diseases, and some cancers.

The invention discloses application of a P2X7 receptor inhibitor in the preparation of drugs for treating radiation brain injuries. Through experimental deep research on pathogenesis of radiation brain injuries and effect of a P2X7 receptor upon occurrence and development of the radiation brain injuries, discovered is that radioactive rays activating microglial cells by the P2X7 receptor cause following inflammatory response, the P2X7 receptor specific inhibitor BBG is effective in inhibiting this response, and nerve cells are thereby protected; the inhibitor is applicable to the treatment of radiation brain injuries.

Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and / or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and / or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.

Unexpectedly, disorders of the cornea and conjunctiva are found to be caused or to be exacerbated, at least in part, by extracellular ATP and P2X7 receptor activation. Therapeutic compositions for topical administration to the eye for the treatment of disorders of the cornea and conjunctiva include an entity that inhibits P2X7 receptor function, reduces the effective concentration of extracellular ATP, or both.

Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and / or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and / or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.

The present invention relates to compounds of the formulawherein R1 and R2 are independently hydrogen, C1–C4 alkyl, C1–C4 substituted alkyl, C1–C4 alkoxy, C1–C4 substituted alkoxy, C1–C4 acyl, halogen, cyano, nitro, amino, alkylamino, or dialkylamino;R3, R4, R5, R6, R7, and R8 are independently CH or nitrogen;R9 is hydrogen or methyl;R10 is C═O or (CH2)n;where n is 0, 1, 2, 3, or 4;R11 and R12 are independently nitrogen or CH; X1 and X2 are independently hydrogen, deuterium, tritium or halogen; and X3 is N; and their pharmaceutically acceptable salts; compositions thereof. Methods of preparing the compounds are also described. The compounds are useful in the treatment of diseases in mammals that are mediated by the action of the P2X7 receptor.

The present invention relates to biological materials against P2X7 and more in particular to polypeptides, nucleic acids encoding such polypeptides; to methods for preparing such polypeptides; to host cells expressing or capable of expressing such polypeptides; to compositions and in particular to pharmaceutical compositions that comprise such polypeptides, for prophylactic, therapeutic or diagnostic purposes. In particular, the biological materials of the present invention inhibit the biological activity of the P2X7 receptor, such as activation by ATP.

The invention discloses a nanosuspension of a P2X7 receptor antagonist employing isoquinoline as a basic skeleton and a preparation method of the nanosuspension, and belongs to the field of medicinal preparations. As a novel P2X7 receptor antagonist, the major indications are labour pains, inflammation, respiratory tract and airway diseases and obstacles and the like. The medicine is extremely difficult to dissolve in water, so that the clinical application is limited. The nanosuspension is prepared by an antisolvent precipitation method combined with a high pressure homogenization method; and the prescription and technology are optimized employing the particle sizes and a polydispersity index as indexes. The result shows that the particle sizes of the medicines in the prepared nanosuspension are 50-500nm; the nanosuspension is round in shape and uniform in distribution; the particle sizes are reduced; increase of the medicine solubility is facilitated; and the in vitro dissolubility is improved.

One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and / or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect.

The present invention provides polynucleotides encoding mutated PYR / PYL receptor polypeptides that are agonized by chemicals, such as bromoxynil, chloroxynil, ioxynil, coumatetralyl, dichlobenil, fenhexamid, benoxacor, and BTH, that do not agonize wild-type PYR / PYL receptor polypeptides, and expression cassettes and plants comprising the polynucleotides. Particular embodiments of the invention provide polynucleotides encoding mutated PYR / PYL receptor polypeptides having a mutation in the ligand-binding pocket of the PYR / PYL receptor polypeptide.