Abstract: A pharmaceutical composition and methods of administering the same for treatment of cardiovascular disease comprising a pepducin having a sequence SEQ ID No. 1, wherein said composition stimulates cardiomyocyte contractility and activating the ?2AR/?-arrestin signaling pathway.

Abstract: The present invention relates to a method of inhibiting desensitization of a cell to the effects of a compound. The method comprises contacting the cell with an agent capable of inhibiting phosphorylation, by a protein kinase, of a receptor for the compound present on the surface of the cell. The present invention also relates to a method of screening a compound for its ability to inhibit desensitization.

Abstract: The present invention relates to a method of inhibiting desensitization of a cell to the effects of a compound. The method comprises contacting the cell with an agent capable of inhibiting phosphorylation, by a protein kinase, of a receptor for the compound present on the surface of the cell. The present invention also relates to a method of screening a compound for its ability to inhibit desensitization. The method comprises: i) contacting a receptor specific kinase-containing sample with the compound under conditions such that interaction between receptor specific kinase present in the sample and the compound can occur, and ii) determining the ability of the receptor specific kinase to phosphorylate the receptor for which it is specific.

Abstract: G protein-coupled receptor kinases (GRK) play an important role in phosphorylating and regulating the activity of G protein-coupled receptors. Complementary DNAs (cDNAs)that encode two novel members of the G protein-coupled receptor kinase (GRK) family are provided in the present invention. These cDNAs encode GRK5 (590 amino acids) and GRK6 (576 amino acids) which represent two new members of the GRK family that have distinct tissue distribution and substrate specificity. The availability of the cDNAs enables the generation of reagents to modulate the activity of endogenous kinases. These include dominant negative mutations and antisense oligonucleotides or stably transfected antisense constructs to block expression of the kinase to generate a cell with a reduced ability to desensitize to various agents. Expression of GRK5 and GRK6 also permits identification of specific inhibitors and activators of these two kinases.

Abstract: G protein-coupled receptor kinases (GRK) play an important role in phosphorylating and regulating the activity of G protein-coupled receptors. Complementary DNAs (cDNAs) that encode two novel members of the G protein-coupled receptor kinase (GRK) family are provided in the present invention. These cDNAs encode GRK5 (590 amino acids) and GRK6 (576 amino acids) which represent two new members of the GRK family that have distinct tissue distribution and substrate specificity. The availability of the cDNAs enables the generation of reagents to modulate the activity of endogenous kinases. These include dominant negative mutations and antisense oligonucleotides or stably transfected antisense constructs to block expression of the kinase to generate a cell with a reduced ability to desensitize to various agents. Expression of GRK5 and GRK6 also permits identification of specific inhibitors and activators of these two kinases.

Abstract: The present invention relates to a method of inhibiting desensitization of a cell to the effects of a compound. The method comprises contacting the cell with an agent capable of inhibiting phosphorylation, by a protein kinase, of a receptor for the compound present on the surface of the cell. The present invention also relates to a method of screening a compound for its ability to inhibit desensitization. The method comprises: i) contacting a receptor specific kinase-containing sample with the compound under conditions such that interaction between receptor specific kinase present in the sample and the compound can occur, andii) determining the ability of the receptor specific kinase to phosphorylate the receptor for which it is specific.

Abstract: Immunoassay method and reagent means for determining theophylline in biological fluids such as serum. The antibody employed in the method is prepared from an immunogen comprising theophylline coupled at its 9-position to an immunogenic carrier material.

Abstract: Theophylline immunogens, antibodies prepared therefrom, labeled theophylline conjugates, synthetic intermediates, and the use of such antibodies and labeled conjugates in immunoassays for determining theophylline. The immunogens comprise theophylline coupled at its 9-position to an immunogenic carrier material. Likewise, the labeled conjugates and synthetic intermediates are 9-position derivatives of theophylline or synthetic precursors thereof. The antibody and labeled reagents are particularly useful in homogeneous nonradioisotopic immunoassays for measuring theophylline in biological fluids such as serum.

Abstract: Intermediates in the preparation of 9-position derivatives of theophylline useful in synthesizing theophylline immunogens and labeled conjugates. The labeled conjugates and the antibodies produced against the immunogens are particularly useful in homogeneous nonradioisotopic immunoassay for measuring theophylline in biological fluids such as serum.