G C Hsieh

Summary

Affiliation: Abbott Laboratories
Country: USA

Publications

  1. ncbi request reprint Effects of selective dopamine receptor subtype agonists on cardiac contractility and regional haemodynamics in rats
    James S Polakowski
    Pharmaceutical Discovery, Global Pharmaceutical R and D, Abbott Laboratories, Abbott Park, Illinois 60064 6119, USA
    Clin Exp Pharmacol Physiol 31:837-41. 2004
  2. doi request reprint Localization of histamine H4 receptors in the central nervous system of human and rat
    Marina I Strakhova
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Department R4MN, Abbott Park, Illinois 60064, USA
    Brain Res 1250:41-8. 2009
  3. ncbi request reprint Central mechanisms regulating penile erection in conscious rats: the dopaminergic systems related to the proerectile effect of apomorphine
    Gin C Hsieh
    Neuroscience Research, Abbott Laboratories, Abbott Park, Illinois 60064 6119, USA
    J Pharmacol Exp Ther 308:330-8. 2004
  4. ncbi request reprint Dual mechanism of action of nicorandil on rabbit corpus cavernosal smooth muscle tone
    G C Hsieh
    Neurological and Urological Diseases Research, Abbott Laboratories, Abbott Park, Illinois 60064 6119, USA
    Int J Impot Res 13:240-6. 2001
  5. pmc Central and peripheral sites of action for CB₂ receptor mediated analgesic activity in chronic inflammatory and neuropathic pain models in rats
    Gin C Hsieh
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Br J Pharmacol 162:428-40. 2011
  6. ncbi request reprint YC-1 potentiates the nitric oxide/cyclic GMP pathway in corpus cavernosum and facilitates penile erection in rats
    Gin C Hsieh
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064 6119, USA
    Eur J Pharmacol 458:183-9. 2003
  7. doi request reprint Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems
    Gin C Hsieh
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Brain Res 1354:74-84. 2010
  8. doi request reprint H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats
    Gin C Hsieh
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    Pharmacol Biochem Behav 95:41-50. 2010
  9. pmc Peripheral and central sites of action for the non-selective cannabinoid agonist WIN 55,212-2 in a rat model of post-operative pain
    C Z Zhu
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Br J Pharmacol 157:645-55. 2009
  10. pmc In vitro and in vivo characterization of A-796260: a selective cannabinoid CB2 receptor agonist exhibiting analgesic activity in rodent pain models
    B B Yao
    Neurological Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Br J Pharmacol 153:390-401. 2008

Detail Information

Publications31

  1. ncbi request reprint Effects of selective dopamine receptor subtype agonists on cardiac contractility and regional haemodynamics in rats
    James S Polakowski
    Pharmaceutical Discovery, Global Pharmaceutical R and D, Abbott Laboratories, Abbott Park, Illinois 60064 6119, USA
    Clin Exp Pharmacol Physiol 31:837-41. 2004
    ..Hence, by comparison, agonism of the D4 receptor has little effect in the cardiovascular system of the rat relative to the other dopamine receptor subtype agonists tested...
  2. doi request reprint Localization of histamine H4 receptors in the central nervous system of human and rat
    Marina I Strakhova
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Department R4MN, Abbott Park, Illinois 60064, USA
    Brain Res 1250:41-8. 2009
    ..Our observations provide evidence of the H(4) presence in both human and rodent CNS and offer some insight into possible role of H(4) in itch and pain...
  3. ncbi request reprint Central mechanisms regulating penile erection in conscious rats: the dopaminergic systems related to the proerectile effect of apomorphine
    Gin C Hsieh
    Neuroscience Research, Abbott Laboratories, Abbott Park, Illinois 60064 6119, USA
    J Pharmacol Exp Ther 308:330-8. 2004
    ..These results suggest that the proerectile action of apomorphine in rats is mediated at supraspinal levels and that this effect is not mimicked by a D2 receptor agonist but associated with activation of D4 receptors...
  4. ncbi request reprint Dual mechanism of action of nicorandil on rabbit corpus cavernosal smooth muscle tone
    G C Hsieh
    Neurological and Urological Diseases Research, Abbott Laboratories, Abbott Park, Illinois 60064 6119, USA
    Int J Impot Res 13:240-6. 2001
    ..The results of the present study indicate that nicorandil can relax rabbit cavernosal tissue in vitro via a mechanism that involves activation of K(ATP) channels and stimulation of soluble guanylate cyclase...
  5. pmc Central and peripheral sites of action for CB₂ receptor mediated analgesic activity in chronic inflammatory and neuropathic pain models in rats
    Gin C Hsieh
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Br J Pharmacol 162:428-40. 2011
    ..The present study was conducted to elucidate the CB₂ receptor expression in 'pain relevant' tissues and the potential sites of action of CB₂ agonism in rats...
  6. ncbi request reprint YC-1 potentiates the nitric oxide/cyclic GMP pathway in corpus cavernosum and facilitates penile erection in rats
    Gin C Hsieh
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064 6119, USA
    Eur J Pharmacol 458:183-9. 2003
    ..These biochemical events may be related to the pro-erectile properties of YC-1 in vivo...
  7. doi request reprint Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems
    Gin C Hsieh
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Brain Res 1354:74-84. 2010
    ..Our data also provide support that selective H(3) antagonists may represent a class of agents for the treatment of pain disorders...
  8. doi request reprint H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats
    Gin C Hsieh
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    Pharmacol Biochem Behav 95:41-50. 2010
    ..Our results demonstrate that selective blockade of H(4) receptors in vivo produces significant anti-nociception in animal models of inflammatory and neuropathic pain...
  9. pmc Peripheral and central sites of action for the non-selective cannabinoid agonist WIN 55,212-2 in a rat model of post-operative pain
    C Z Zhu
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Br J Pharmacol 157:645-55. 2009
    ..However, the effects of CB receptor agonists in post-operative pain remain to be investigated. Here, we characterized the anti-allodynic effects of WIN 55,212-2 (WIN) in a rat model of post-operative pain...
  10. pmc In vitro and in vivo characterization of A-796260: a selective cannabinoid CB2 receptor agonist exhibiting analgesic activity in rodent pain models
    B B Yao
    Neurological Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Br J Pharmacol 153:390-401. 2008
    ..Additionally, its analgesic effects are mu-opioid receptor-dependent. Herein, we describe the in vitro and in vivo pharmacological properties of A-796260, a novel CB2 agonist...
  11. doi request reprint Assessing carrageenan-induced locomotor activity impairment in rats: comparison with evoked endpoint of acute inflammatory pain
    C Z Zhu
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, USA
    Eur J Pain 16:816-26. 2012
    ..Most animal models currently used to evaluate antinociceptive efficacy of analgesics rely on the assessment of evoked pain behaviours as primary endpoints...
  12. ncbi request reprint Activators of soluble guanylate cyclase for the treatment of male erectile dysfunction
    J D Brioni
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    Int J Impot Res 14:8-14. 2002
    ..This type of sGC activators represent a new class of compounds with a different pharmacological profile in comparison to the classical NO-donors and they could be beneficial for the treatment of male erectile dysfunction...
  13. ncbi request reprint 3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator
    S W Djuric
    Immunological Diseases Research, Abbott Laboratories, 200 Abbott Park Road, Abbott Park, Illinois 60064 6217, USA
    J Med Chem 43:2975-81. 2000
    ..Additionally, the BTPs show inhibition of IL-4, IL-5, IL-8, and eotaxin production. Unlike the IL-2 inhibitors, cyclosporine and FK506, the BTPs do not directly inhibit the dephosphorylation of NFAT by calcineurin...
  14. ncbi request reprint Central oxytocinergic and dopaminergic mechanisms regulating penile erection in conscious rats
    Brenda Martino
    Global Neuroscience Research, Global Pharmaceutical Research and Development, Building AP9A, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    Pharmacol Biochem Behav 81:797-804. 2005
    ..Together, these data indicate a possible concomitant role between dopamine and oxytocin in mediating penile erection at both the spinal and supraspinal sites...
  15. doi request reprint Pharmacological modulation of movement-evoked pain in a rat model of osteoarthritis
    Prasant Chandran
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6115, USA
    Eur J Pharmacol 613:39-45. 2009
    ..As the model is clinically relevant, it will further enhance the mechanistic understanding of chronic arthritic joint pain and help in developing newer and better therapeutic strategies to manage osteoarthritis pain...
  16. doi request reprint Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain
    Arturo Perez-Medrano
    Abbott Laboratories, Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Park, Illinois 60064 6101, USA
    J Med Chem 52:3366-76. 2009
    ..These results suggest an important role of P2X(7) receptors in neuropathic pain and therefore a potential use of P2X(7) antagonists as novel therapeutic tools for the treatment of this type of pain...
  17. doi request reprint Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity
    Jennifer M Frost
    Neurological Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, R47W, AP9A, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    J Med Chem 53:295-315. 2010
    ..N1 aromatic side chains also afforded several high affinity CB(2) receptor agonists (61, 63, 65, and 69) but were generally less potent in an in vitro CB(2) functional assay than were nonaromatic side chain analogues...
  18. ncbi request reprint Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction
    Marlon Cowart
    Department of Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60064 6123, USA
    J Med Chem 47:3853-64. 2004
    ..Distinctive structural features were discovered that are associated with D4 selective agonism in this series of analogues...
  19. pmc Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats
    Jorge D Brioni
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Proc Natl Acad Sci U S A 101:6758-63. 2004
    ..The ability of ABT-724 to facilitate penile erection together with the favorable side-effect profile indicates that ABT-724 could be useful for the treatment of erectile dysfunction...
  20. ncbi request reprint A-350619: a novel activator of soluble guanylyl cyclase
    Loan N Miller
    Neuroscience Research, Global Pharmaceutical Research and Development, AP9, Room 1125, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064 6119, USA
    Life Sci 72:1015-25. 2003
    ..Activation of soluble guanylyl cyclase in cavernosum tissue as an alternate method of enhancing the effect of NO may provide a novel treatment of sexual dysfunction...
  21. doi request reprint Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain
    Robert J Altenbach
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6100, United States
    J Med Chem 53:7869-73. 2010
    ..A series of compounds was designed as dual inhibitors of the H(3) receptor and the norepinephrine transporter. Compound 5 (rNET K(i) = 14 nM; rH(3)R K(i) = 37 nM) was found to be efficacious in a rat model of osteoarthritic pain...
  22. doi request reprint cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia
    Huaqing Liu
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6100, USA
    J Med Chem 51:7094-8. 2008
    ..Most interesting was the high potency and efficacy of this compound in blocking pain responses, where it showed an ED(50) of 42 mumol/kg (ip) in a rat post-carrageenan thermal hyperalgesia model of inflammatory pain...
  23. ncbi request reprint A-412997 is a selective dopamine D4 receptor agonist in rats
    Robert B Moreland
    Neuroscience Research, Global Pharmaceutical Research and Development, AP9A Room 219, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois, 60064 6123, USA
    Pharmacol Biochem Behav 82:140-7. 2005
    ..A-412997 is a highly selective dopamine D4 receptor agonist and a useful tool to understand the role of dopamine D4 receptors in rat models of central nervous system processes and disease...
  24. ncbi request reprint 1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction
    Teodozyj Kolasa
    Neuroscience Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6101, USA
    J Med Chem 49:5093-109. 2006
    ..Our results suggest that the oximes provide a novel structural linker for 4-arylpiperazine-based D4 agonists, possessing leadlike quality and with potential to develop a new class of potent and selective dopamine D4 receptor agonists...
  25. ncbi request reprint Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction
    Meena V Patel
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 3500, USA
    J Med Chem 49:7450-65. 2006
    ..The N-oxy-2-pyridinyl moiety not only provided the structural motif required for agonist function but also reduced metabolism rates. The SAR study leading to the discovery of 6b is described herein...
  26. ncbi request reprint 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist
    Masaki Nakane
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Neuropharmacology 49:112-21. 2005
    ..A-381393 inhibited penile erection induced by the selective D4 agonist PD168077 in conscious rats. Thus, A-381393 is a novel selective D4 antagonist that will enhance the ability to study dopamine D4 receptors both in vitro and in vivo...
  27. ncbi request reprint Antidepressant-like effect of D(2/3) receptor-, but not D(4) receptor-activation in the rat forced swim test
    Ana M Basso
    Abbott Laboratories, Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Park, IL 60064, USA
    Neuropsychopharmacology 30:1257-68. 2005
    ..The pharmacological selectivity of the compounds tested suggests that the antidepressant-like effects of quinpirole are most likely mediated mainly by D(2) and to a lesser extent by D(3) but not D(4) receptors...
  28. doi request reprint Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity
    Jennifer M Frost
    Neurological Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    J Med Chem 51:1904-12. 2008
    ..Several agonists were active in the complete Freund's adjuvant model of chronic inflammatory thermal hyperalgesia ( 32, 15)...
  29. doi request reprint Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands
    Robert J Altenbach
    Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6100, USA
    J Med Chem 51:6571-80. 2008
    ....
  30. doi request reprint Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models
    Marlon D Cowart
    Department of Neuroscience Research, Abbott Laboratories, Abbott Park, Illinois 60064 6123, USA
    J Med Chem 51:6547-57. 2008
    ..6 and 1.6 h, oral bioavailability of 37% and 90%) with anti-inflammatory activity (ED 50 = 37 micromol/kg, mouse) and efficacy in pain models (thermal hyperalgesia, ED 50 = 72 micromol/kg, rat)...
  31. pmc Differential effects of cannabinoid receptor agonists on regional brain activity using pharmacological MRI
    C L Chin
    Advanced Technology, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Br J Pharmacol 153:367-79. 2008
    ..To address selectivity in vivo, we describe non-invasive, non-ionizing, functional data that distinguish CB1 from CB2 receptor neural activity using pharmacological MRI (phMRI) in awake rats...