Abstract: Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

Abstract: Isolated polynucleotides encoding monkey and canine Melanin Concentrating Hormone (MCH) Type 2 receptors and chimeric polypeptides are provided. Vectors and cells for recombinant expression of such MCH receptor polypeptides, and isolated MCH receptor polypeptides are also provided. MCH receptor polynucleotides and polypeptides may be used, for example, to identify agents that specifically interact with MCH receptor. Such agents find use within therapies for humans and animals afflicted with conditions associated with MCH receptor activation.

Abstract: Isolated polynucleotides encoding monkey Melanin Concentrating Hormone (MCH) Type 1 receptors and chimeric polypeptides are provided. Vectors and cells for recombinant expression of such MCH1R polypeptides, and isolated MCH1R polypeptides are also provided. MCH1R polynucleotides and polypeptides may be used, for example, to identify compounds that specifically interact with MCH receptor. Such compounds find use within therapies for humans and animals afflicted with conditions associated with MCH receptor activation.

Abstract: Isolated polynucleotides encoding monkey Melanin Concentrating Hormone (MCH) Type 1 receptors and chimeric polypeptides are provided. Vectors and cells for recombinant expression of such MCH1R polypeptides, and isolated MCH1R polypeptides are also provided. MCH1R polynucleotides and polypeptides may be used, for example, to identify compounds that specifically interact with MCH receptor. Such compounds find use within therapies for humans and animals afflicted with conditions associated with MCH receptor activation.

Abstract: This invention provides novel human capsaicin receptors and the nucleotide sequences encoding these receptors. Also provided are vectors encoding these receptors and mammalian and non-mammalian cells expressing these vectors. Further provided are assays for identifying compounds that modulate capsaicin receptors and diagnostic assays for capsaicin receptor polymorphisms and aberrant capsaicin receptor expression.

Abstract: Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

Abstract: Compositions and methods are provided for the treatment of pain. Compositions and methods are further provided for inhibiting the development of tolerance to addictive therapeutic agents (especially narcotic analgesics) in patients treated with such agents; for minimizing adverse effects (e.g., dependence) resulting from treatment with such addictive agents; and for enhancing pain relief resulting from narcotic analgesic administration. The compositions generally comprise a nontoxic VR1 antagonist, optionally in combination with an addictive therapeutic agent. Patients may be treated with a VR1 antagonist before, during or after administration of the addictive therapeutic agent to prevent, decrease the severity of, delay or treat tolerance and/or other adverse effects of the addictive agent in the patient.

Abstract: Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

Abstract: Compositions and methods for treating diseases that are associated with inflammation are provided. Such diseases include arthritis (particularly rheumatoid arthritis) and other autoimmune disorders, asthma, cardio- and cerebrovascular disease, burns, psoriasis, reperfusion injury, and traumatic CNS and spinal cord injury. The compositions generally comprise at least one C5a antagonist and at least one C5a receptor-inactive therapeutic agent. The methods involve co-administration of at least one C5a antagonist and at least one C5a receptor-inactive therapeutic agent to a patient. The C5a antagonist and C5a receptor-inactive therapeutic agent may be present within the same composition, or may be administered separately to the patient.

Abstract: Isolated polynucleotides encoding monkey and canine Melanin Concentrating Hormone (MCH) Type 2 receptors and chimeric polypeptides are provided. Vectors and cells for recombinant expression of such MCH receptor polypeptides, and isolated MCH receptor polypeptides are also provided. MCH receptor polynucleotides and polypeptides may be used, for example, to identify agents that specifically interact with MCH receptor. Such agents find use within therapies for humans and animals afflicted with conditions associated with MCH receptor activation.

Abstract: Isolated polynucleotides encoding monkey Melanin Concentrating Hormone (MCH) Type 1 receptors and chimeric polypeptides are provided. Vectors and cells for recombinant expression of such MCH1R polypeptides, and isolated MCH1R polypeptides are also provided. MCH1R polynucleotides and polypeptides may be used, for example, to identify compounds that specifically interact with MCH receptor. Such compounds find use within therapies for humans and animals afflicted with conditions associated with MCH receptor activation.

Abstract: This invention provides novel human capsaicin receptors and the nucleotide sequences encoding these receptors. Also provided are vectors encoding these receptors and mammalian and non-mammalian cells expressing these vectors. Further provided are assays for identifying compounds that modulate capsaicin receptors and diagnostic assays for capsaicin receptor polymorphisms and aberrant capsaicin receptor expression.

Abstract: Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

Abstract: Novel chimeric G-protein coupled receptors are provided as isolated polypeptides, membrane preparations containing such chimeric receptors, nucleic acids encoding such chimeric receptors, and cells expressing such receptors. The chimeric receptors are NPY5 receptors with most or all of either one or both of the third cytoplasmic loop domain or the C-terminal intracellular domain of NPY5 replaced with the corresponding region(s) of another NPY receptor, preferably an NPY1 receptor.