Tadimeti S Rao

Summary

Affiliation: Kalypsys Inc
Country: USA

Publications

  1. doi request reprint Pharmacological characterization of (S)-(2)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine HCl (SIB-1508Y, Altinicline), a novel nicotinic acetylcholine receptor agonist
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Brain Res 1234:16-24. 2008
  2. ncbi request reprint Pharmacological characterization of lysophospholipid receptor signal transduction pathways in rat cerebrocortical astrocytes
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, Building 1, San Diego, CA 92121, USA
    Brain Res 990:182-94. 2003
  3. ncbi request reprint Growth factor pre-treatment differentially regulates phosphoinositide turnover downstream of lysophospholipid receptor and metabotropic glutamate receptors in cultured rat cerebrocortical astrocytes
    Tadimeti S Rao
    Merck Research Laboratories San Diego, 3535 General Atomics Court, Bldg 1, San Diego, CA 92121, USA
    Int J Dev Neurosci 22:131-5. 2004
  4. doi request reprint Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor
    Joseph E Payne
    Department of Chemistry, Kalypsys, Inc, 10420 Wateridge Circle, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 18:6093-6. 2008
  5. ncbi request reprint In vivo pharmacological characterization of (+/-)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol hydrochloride (SIB-1553A), a novel cholinergic ligand: microdialysis studies
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Brain Res 986:71-81. 2003
  6. ncbi request reprint Microglial activation state and lysophospholipid acid receptor expression
    Chui Se Tham
    Molecular Neuroscience Laboratory, Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Int J Dev Neurosci 21:431-43. 2003
  7. doi request reprint Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective
    Joseph E Payne
    Department of Chemistry, Kalypsys, Inc, 10420 Wateridge Circle, San Diego, California 92121, USA
    J Med Chem 53:7739-55. 2010
  8. ncbi request reprint Sphingosine 1-phosphate receptor agonists attenuate relapsing-remitting experimental autoimmune encephalitis in SJL mice
    Michael Webb
    Molecular Neuroscience Laboratory, Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    J Neuroimmunol 153:108-21. 2004
  9. ncbi request reprint Pharmacological characterization of dopamine, norepinephrine and serotonin release in the rat prefrontal cortex by neuronal nicotinic acetylcholine receptor agonists
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Brain Res 990:203-8. 2003
  10. doi request reprint Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models
    Celine Bonnefous
    Department of Chemistry, Kalypsys Inc, 10420 Wateridge Circle, San Diego, CA 92121, USA
    J Med Chem 52:3047-62. 2009

Collaborators

Detail Information

Publications19

  1. doi request reprint Pharmacological characterization of (S)-(2)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine HCl (SIB-1508Y, Altinicline), a novel nicotinic acetylcholine receptor agonist
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Brain Res 1234:16-24. 2008
    ..In summary, the abilities of SIB-1508Y to release multiple neurotransmitters in distinct brain regions may contribute to its behavioral profile...
  2. ncbi request reprint Pharmacological characterization of lysophospholipid receptor signal transduction pathways in rat cerebrocortical astrocytes
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, Building 1, San Diego, CA 92121, USA
    Brain Res 990:182-94. 2003
    ....
  3. ncbi request reprint Growth factor pre-treatment differentially regulates phosphoinositide turnover downstream of lysophospholipid receptor and metabotropic glutamate receptors in cultured rat cerebrocortical astrocytes
    Tadimeti S Rao
    Merck Research Laboratories San Diego, 3535 General Atomics Court, Bldg 1, San Diego, CA 92121, USA
    Int J Dev Neurosci 22:131-5. 2004
    ....
  4. doi request reprint Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor
    Joseph E Payne
    Department of Chemistry, Kalypsys, Inc, 10420 Wateridge Circle, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 18:6093-6. 2008
    ..KD5170 exhibits robust and sustained histone H3 hyperacetylation in HCT-116 xenograft tumors following single oral or i.v. dose and inhibition of tumor growth following chronic dosing...
  5. ncbi request reprint In vivo pharmacological characterization of (+/-)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol hydrochloride (SIB-1553A), a novel cholinergic ligand: microdialysis studies
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Brain Res 986:71-81. 2003
    ..Due to the proposed role of cholinergic pathways in learning and memory, the neurochemical profile of SIB-1553A suggests a potential for it to treat cognitive dysfunction...
  6. ncbi request reprint Microglial activation state and lysophospholipid acid receptor expression
    Chui Se Tham
    Molecular Neuroscience Laboratory, Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Int J Dev Neurosci 21:431-43. 2003
    ..The levels of mRNA of LPA1 and S1P receptors was reduced by overnight exposure to S1P, while the same treatment significantly up-regulated the level of LPA3 mRNA...
  7. doi request reprint Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective
    Joseph E Payne
    Department of Chemistry, Kalypsys, Inc, 10420 Wateridge Circle, San Diego, California 92121, USA
    J Med Chem 53:7739-55. 2010
    ..Further 42 did not affect motor coordination up to doses of 1000 mg/kg, demonstrating a wide therapeutic margin...
  8. ncbi request reprint Sphingosine 1-phosphate receptor agonists attenuate relapsing-remitting experimental autoimmune encephalitis in SJL mice
    Michael Webb
    Molecular Neuroscience Laboratory, Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    J Neuroimmunol 153:108-21. 2004
    ..EAE produced by adoptively transferring lymph node cells from immunized mice to naïve hosts is similarly ameliorated by FTY-P. Treatment with FTY-P is accompanied by a dose-responsive peripheral lymphopoenia...
  9. ncbi request reprint Pharmacological characterization of dopamine, norepinephrine and serotonin release in the rat prefrontal cortex by neuronal nicotinic acetylcholine receptor agonists
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Brain Res 990:203-8. 2003
    ..The differences between nicotinic agonist induced catecholamine and serotonin release suggest involvement of distinct nAChRs...
  10. doi request reprint Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models
    Celine Bonnefous
    Department of Chemistry, Kalypsys Inc, 10420 Wateridge Circle, San Diego, CA 92121, USA
    J Med Chem 52:3047-62. 2009
    ..Following oral dosing, compounds 12 and 42 gave a statistical reduction in pain behaviors in the mouse formalin model, while 12 also statistically reduced neuropathic pain behaviors in the chronic constriction injury (Bennett) model...
  11. ncbi request reprint In vitro pharmacological characterization of (+/-)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A), a nicotinic acetylcholine receptor ligand
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Brain Res 981:85-98. 2003
    ..SIB-1553A did not inhibit rat brain cholinesterase for up to 1 mM. Multiple receptor affinities and release of several neurotransmitters may underlie the cognitive-enhancing effects of SIB-1553A documented in rodent and primate models...
  12. doi request reprint Pharmacological characterization of KLYP961, a dual inhibitor of inducible and neuronal nitric-oxide synthases
    Kent T Symons
    Department of Biology, Kalypsys Inc, San Diego, California, USA
    J Pharmacol Exp Ther 336:468-78. 2011
    ..o.) and a greater potency than gabapentin. In summary, KLYP961 represents an ideal tool with which to probe the physiological role of NO derived from iNOS and nNOS in human pain and inflammatory states...
  13. ncbi request reprint Pharmacological characterization of SIB-1663, a conformationally rigid analog of nicotine
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA
    Brain Res 1003:42-53. 2004
    ..These data indicate that SIB-1663, a conformationally restricted analog of NIC, with distinct nAChR subtype selectivity from NIC exhibits contrasting pharmacology with some of its in vivo actions involving nAChRs...
  14. ncbi request reprint Characterization of lysophosphatidic acid and sphingosine-1-phosphate-mediated signal transduction in rat cortical oligodendrocytes
    Naichen Yu
    Molecular Neuroscience, Merck Research Laboratories, San Diego, California 92121, USA
    Glia 45:17-27. 2004
    ..These results taken together suggest that lysophospholipid receptor activation involves receptor coupling to heterotrimeric Gq subunits with consequent activation of PLC, PKC, and MAPK pathways leading to ERK phosphorylation...
  15. doi request reprint Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors
    Timothy C Gahman
    Department of Medicinal Chemistry, Kalypsys Inc, 10420 Wateridge Circle, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 21:6888-94. 2011
    ....
  16. doi request reprint KLYP956 is a non-imidazole-based orally active inhibitor of nitric-oxide synthase dimerization
    Kent T Symons
    Department of Biology, Kalypsys Inc, San Diego, CA, USA
    Mol Pharmacol 76:153-62. 2009
    ..KLYP956 thus represents the first nonimidazole-based inhibitor of iNOS and nNOS dimerization and provides a novel pharmaceutical alternative to previously described substrate competitive inhibitors...
  17. ncbi request reprint Lysolecithin induces demyelination in vitro in a cerebellar slice culture system
    Eric Birgbauer
    Department of Neurobiology, Merck Research Laboratories, San Diego, California, USA
    J Neurosci Res 78:157-66. 2004
    ..Lysolecithin thus induces demyelination in an in vitro organotypic cerebellar slice culture system, providing a model system for studying myelination, demyelination, and remyelination in vitro...
  18. ncbi request reprint Glutamate-dependent glutamine, aspartate and serine release from rat cortical glial cell cultures
    Tadimeti S Rao
    Merck Research Laboratories, 3535 General Atomics Ct, MRLSDB1, San Diego, CA 92122, USA
    Brain Res 978:213-22. 2003
    ..These results further substantiate coupling between glutamate and glutamine, and shed light on glutamate-dependent release of serine and aspartate, which may further contribute to excitatory neurotransmission...
  19. doi request reprint KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo
    Christian A Hassig
    Kalypsys, Inc, 10420 Wateridge Circle, San Diego, CA 92121, USA
    Mol Cancer Ther 7:1054-65. 2008
    ..The biological and pharmaceutical profile of KD5170 supports its continued preclinical and clinical development as a broad spectrum anticancer agent...