Darlene Deecher

Summary

Affiliation: Wyeth Research
Country: USA

Publications

  1. ncbi request reprint Understanding the pathophysiology of vasomotor symptoms (hot flushes and night sweats) that occur in perimenopause, menopause, and postmenopause life stages
    D C Deecher
    Women s Health Research, Wyeth Pharmaceuticals, Collegeville, PA 19426, USA
    Arch Womens Ment Health 10:247-57. 2007
  2. ncbi request reprint From menarche to menopause: exploring the underlying biology of depression in women experiencing hormonal changes
    Darlene Deecher
    Wyeth Research, 500 Arcola Rd, RN3164, Collegeville, PA 19426, USA
    Psychoneuroendocrinology 33:3-17. 2008
  3. ncbi request reprint Alleviation of thermoregulatory dysfunction with the new serotonin and norepinephrine reuptake inhibitor desvenlafaxine succinate in ovariectomized rodent models
    Darlene C Deecher
    Women s Health and Musculoskeletal Biology, Wyeth Research N3164, 500 Arcola Road, Collegeville, PA 19426, USA
    Endocrinology 148:1376-83. 2007
  4. ncbi request reprint Characterization of a membrane-associated estrogen receptor in a rat hypothalamic cell line (D12)
    Darlene C Deecher
    Women s Health Research Institute, Wyeth Research, Collegeville, PA 19426, USA
    Endocrine 22:211-23. 2003
  5. ncbi request reprint Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor
    Darlene C Deecher
    Women s Health and Musculoskeletal Biology, Wyeth Research, N3164, 500 Arcola Rd, Collegeville, PA 19426, USA
    J Pharmacol Exp Ther 318:657-65. 2006
  6. ncbi request reprint Physiology of thermoregulatory dysfunction and current approaches to the treatment of vasomotor symptoms
    Darlene C Deecher
    Women s Health Research Institute, Wyeth Pharmaceuticals, Collegeville, PA 19426, USA
    Expert Opin Investig Drugs 14:435-48. 2005
  7. ncbi request reprint Endogenously expressed estrogen receptors mediate neuroprotection in hippocampal cells (HT22)
    Darlene C Deecher
    Women s Health Research Institute, Wyeth Research, Collegeville, Pennsylvania 19426, USA
    J Cell Biochem 95:302-12. 2005
  8. doi request reprint Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors
    Puwen Zhang
    Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 18:6067-70. 2008
  9. ncbi request reprint Pharmacokinetic and pharmacodynamic profiles of the novel serotonin and norepinephrine reuptake inhibitor desvenlafaxine succinate in ovariectomized Sprague-Dawley rats
    Peter D Alfinito
    Women s Health and Musculoskeletal Biology, Wyeth Research, 500 Arcola Road, Collegeville, PA 19425, USA
    Brain Res 1098:71-8. 2006
  10. doi request reprint Simultaneous telemetric monitoring of tail-skin and core body temperature in a rat model of thermoregulatory dysfunction
    Scott Cosmi
    Women s Health and Musculoskeletal Biology, Wyeth Research, Collegeville, PA 19426, USA
    J Neurosci Methods 178:270-5. 2009

Collaborators

Detail Information

Publications36

  1. ncbi request reprint Understanding the pathophysiology of vasomotor symptoms (hot flushes and night sweats) that occur in perimenopause, menopause, and postmenopause life stages
    D C Deecher
    Women s Health Research, Wyeth Pharmaceuticals, Collegeville, PA 19426, USA
    Arch Womens Ment Health 10:247-57. 2007
    ..This review considers the processes and pathways involved in normal temperature regulation and the impact of fluctuating and declining hormones that result in VMS during the menopausal transition...
  2. ncbi request reprint From menarche to menopause: exploring the underlying biology of depression in women experiencing hormonal changes
    Darlene Deecher
    Wyeth Research, 500 Arcola Rd, RN3164, Collegeville, PA 19426, USA
    Psychoneuroendocrinology 33:3-17. 2008
    ..A testable hypothesis will be proposed to advance our understanding of hormonal effects on mood...
  3. ncbi request reprint Alleviation of thermoregulatory dysfunction with the new serotonin and norepinephrine reuptake inhibitor desvenlafaxine succinate in ovariectomized rodent models
    Darlene C Deecher
    Women s Health and Musculoskeletal Biology, Wyeth Research N3164, 500 Arcola Road, Collegeville, PA 19426, USA
    Endocrinology 148:1376-83. 2007
    ..These preclinical studies provide evidence that DVS directly impacts thermoregulatory dysfunction in OVX rats and may have utility in alleviating VMS associated with menopause...
  4. ncbi request reprint Characterization of a membrane-associated estrogen receptor in a rat hypothalamic cell line (D12)
    Darlene C Deecher
    Women s Health Research Institute, Wyeth Research, Collegeville, PA 19426, USA
    Endocrine 22:211-23. 2003
    ..These data support the expression of mER in these brain-derived endothelial cells that is similar to, but biochemically distinguishable from, nuclear ERalpha...
  5. ncbi request reprint Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor
    Darlene C Deecher
    Women s Health and Musculoskeletal Biology, Wyeth Research, N3164, 500 Arcola Rd, Collegeville, PA 19426, USA
    J Pharmacol Exp Ther 318:657-65. 2006
    ..In conclusion, DVS is a new 5-HT and NE reuptake inhibitor in vitro and in vivo that demonstrates good brain-to-plasma ratios, suggesting utility in a variety of central nervous system-related disorders...
  6. ncbi request reprint Physiology of thermoregulatory dysfunction and current approaches to the treatment of vasomotor symptoms
    Darlene C Deecher
    Women s Health Research Institute, Wyeth Pharmaceuticals, Collegeville, PA 19426, USA
    Expert Opin Investig Drugs 14:435-48. 2005
    ..This paper reviews the physiology involved in the underlying thermoregulatory dysfunction that presumably causes VMS and discusses how this physiology relates to current and future VMS treatment options...
  7. ncbi request reprint Endogenously expressed estrogen receptors mediate neuroprotection in hippocampal cells (HT22)
    Darlene C Deecher
    Women s Health Research Institute, Wyeth Research, Collegeville, Pennsylvania 19426, USA
    J Cell Biochem 95:302-12. 2005
    ..In conclusion, HT22 cells express functional ERalpha or a closely related ER enabling this cell line to be used to profile estrogens for neuroprotective properties acting via an ER-dependent mechanism...
  8. doi request reprint Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors
    Puwen Zhang
    Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 18:6067-70. 2008
    ..Several compounds such as 15 and 20 showed good hNET potency. Compounds 15 and 20 also displayed excellent selectivity at hNET that appeared superior to those of reboxetine and atomoxetine (4 and 5)...
  9. ncbi request reprint Pharmacokinetic and pharmacodynamic profiles of the novel serotonin and norepinephrine reuptake inhibitor desvenlafaxine succinate in ovariectomized Sprague-Dawley rats
    Peter D Alfinito
    Women s Health and Musculoskeletal Biology, Wyeth Research, 500 Arcola Road, Collegeville, PA 19425, USA
    Brain Res 1098:71-8. 2006
    ..This work supports the notion that DVS could have utility for treating disorders in menopausal women in which changes in 5-HT and/or NE have been implicated...
  10. doi request reprint Simultaneous telemetric monitoring of tail-skin and core body temperature in a rat model of thermoregulatory dysfunction
    Scott Cosmi
    Women s Health and Musculoskeletal Biology, Wyeth Research, Collegeville, PA 19426, USA
    J Neurosci Methods 178:270-5. 2009
    ..These findings support the use of the new dual temperature transmitters and should enhance the quality and interpretation of data being generated in thermoregulation studies...
  11. doi request reprint 3-(Arylamino)-3-phenylpropan-2-olamines as a new series of dual norepinephrine and serotonin reuptake inhibitors
    An T Vu
    Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 19:2464-7. 2009
    ..A number of analogues displayed significant dual norepinephrine and serotonin reuptake inhibition. Compounds in this class exhibited minimal affinity for the dopamine transporter...
  12. ncbi request reprint Serotonin 2A receptors modulate tail-skin temperature in two rodent models of estrogen deficiency-related thermoregulatory dysfunction
    Kimberly Sipe
    Women s Health Research Institute, Wyeth Research N3151A, 500 Arcola Rd, Collegeville, PA 19426, USA
    Brain Res 1028:191-202. 2004
    ..These results indicate that activation of central 5-HT(2A) receptors restores temperature regulation in two rodent models of ovariectomy-induced thermoregulatory dysfunction...
  13. doi request reprint ICI 182,780 penetrates brain and hypothalamic tissue and has functional effects in the brain after systemic dosing
    Peter D Alfinito
    Women s Health and Musculoskeletal Biology, Wyeth Research, RN 3164, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA
    Endocrinology 149:5219-26. 2008
    ..Thus, ICI crosses the BBB, penetrates into brain and hypothalamic tissues, and has both antiestrogenic and estrogenic-like actions on neuroendocrine-related functions...
  14. ncbi request reprint Effect of calcium channel modulators on temperature regulation in ovariectomized rats
    Liza Leventhal
    Women s Health Research Institute, Wyeth Research RN3164, 500 Arcola Rd, Collegeville, PA 19426, USA
    Pharmacol Biochem Behav 80:511-20. 2005
    ..The present data suggests that gabapentin, verapamil and nifedipine all act to globally alter temperature regulation in steroid-dependent models of thermoregulatory function...
  15. ncbi request reprint Identification and characterization of a selective, nonpeptide follicle-stimulating hormone receptor antagonist
    Brian J Arey
    Women s Health Research Institute and Medicinal Chemistry, Department of Chemical Sciences, Wyeth Research, Collegeville, Pennsylvania 19680, USA
    Endocrinology 143:3822-9. 2002
    ..Compound 1 inhibited ovulation in immature and cycling adult rats. These data provide proof of concept that selective, small molecule antagonists can be designed for glycoprotein hormone receptors...
  16. doi request reprint Structure-activity relationships of the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ol series of monoamine reuptake inhibitors
    Paige E Mahaney
    Chemical Sciences, Wyeth Research, Collegeville, PA 19426, United States
    Bioorg Med Chem Lett 19:5807-10. 2009
    ..This study led to the discovery of compound 20 which inhibited the norepinephrine transporter with an IC50 value of 4 nM while exhibiting 86-fold selectivity over the serotonin transporter...
  17. doi request reprint Estradiol increases catecholamine levels in the hypothalamus of ovariectomized rats during the dark-phase
    Peter D Alfinito
    Women s Health and Musculoskeletal Biology, Wyeth Research, Collegeville, PA 19426, USA
    Eur J Pharmacol 616:334-9. 2009
    ..The estradiol benzoate-induced increases in norepinephrine and dopamine levels in the preoptic area during the dark-phase may play an important role in modulating critical hypothalamic functions...
  18. doi request reprint Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors
    Joseph P Sabatucci
    Chemical Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 20:2809-12. 2010
    ..Synthesis of a variety of heterocycles identified (+)-S-21, a potent NRI efficacious in an animal model for thermoregulatory dysfunction...
  19. doi request reprint Discovery of a new series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols
    Callain Y Kim
    Chemical Sciences, Wyeth Research, Arcola Road, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 19:5029-32. 2009
    ....
  20. doi request reprint Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles
    Gavin D Heffernan
    Chemical Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    Bioorg Med Chem 17:7802-15. 2009
    ..The synthesis and structure-activity relationship (SAR) of this novel series of compounds is also presented...
  21. doi request reprint Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores
    Andrew Fensome
    Pfizer Global Research and Development, 500 Arcola Road, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 20:1555-8. 2010
    ..The 3,4-dihydrosulfostyril series was further tested for microsome stability, and compound 16j, which was optimized for both potency and stability, showed efficacy in an in vivo model of thermoregulatory dysfunction...
  22. doi request reprint 1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as potent and selective norepinephrine reuptake inhibitors
    An T Vu
    Wyeth Research, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA
    J Med Chem 53:2051-62. 2010
    ....
  23. doi request reprint Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors
    Casey C McComas
    Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, S2227A, Collegeville, PA 19426, USA
    Bioorg Med Chem Lett 18:4929-31. 2008
    ....
  24. doi request reprint Effect of 17alpha-ethinyl estradiol on active phase rapid eye movement sleep microarchitecture
    Aaron C Pawlyk
    Women s Health and Musculoskeletal Biology, Wyeth Research, Collegeville, PA 19426, USA
    Eur J Pharmacol 591:315-8. 2008
    ..These results further elucidate 17alpha-EE's effects on REM sleep and provide greater understanding of the mechanisms by which estrogens alter sleep-wakefulness patterns...
  25. ncbi request reprint Discrimination of galanin receptor subtypes in RINm5F cells by structurally different galanin radioligands
    Darlene C Deecher
    Molecular Biology Department, Women s Health Research Institute, Wyeth Research, Collegeville, PA 19426, USA
    Peptides 23:545-53. 2002
    ..Additionally, our data suggests that GALRs exist in a precoupled state with their respective G-proteins prior to interaction with the agonist...
  26. ncbi request reprint A glutathione-S-transferase-FSHalpha subunit hybrid associates with FSHbeta, retains biological activity, and facilitates purification
    Panayiotis E Stevis
    Women s Health and Bone, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    Biochem Biophys Res Commun 319:1026-31. 2004
    ..The use of GST-BV-hFSHalpha provides a novel and efficient method for purifying and studying members of the glycoprotein hormone family derived from the culture supernatant or subcellular fractions of the cell...
  27. ncbi request reprint Analysis of glycoprotein hormone receptor extracellular domain interactions using a solid-phase capture assay
    Panayiotis E Stevis
    Contraception and Reproductive Endocrinology Group, Women s Health and Bone, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA
    Anal Biochem 338:320-5. 2005
    ..This assay format should be applicable to the other receptors of this family...
  28. ncbi request reprint Effects of the 5-HT2A antagonist mirtazapine in rat models of thermoregulation
    Aaron C Pawlyk
    Women s Health and Musculoskeletal Biology, Wyeth Research N3148B, 500 Arcola Rd, Collegeville, PA 19426, USA
    Brain Res 1123:135-44. 2006
    ..These data support the concept that 5-HT(2A) receptors play a role in temperature regulation but that functional blockade of these receptors by mirtazapine is not a likely mechanism for restoring thermoregulatory processes in OVX rats...
  29. ncbi request reprint The role of the selective serotonin reuptake inhibitor fluoxetine in temperature regulation in ovariectomized rat models
    Navin Maswood
    Women s Health and Musculoskeletal Biology, Wyeth Research, Collegeville, PA 19426, USA
    Neuroendocrinology 84:330-8. 2006
    ..c. dose abated the naloxone-induced increase in TST by 55 and 81%, respectively. In summary, FLX affected CBT at all doses, but alleviated thermoregulatory dysfunction only at higher doses that are non-selective for the 5-HT system...
  30. ncbi request reprint Subchronic 17alpha-ethinyl estradiol differentially affects subtypes of sleep and wakefulness in ovariectomized rats
    Aaron C Pawlyk
    Women s Health and Musculoskeletal Biology, Wyeth Research N3129, 500 Arcola Rd, Collegeville, PA 19426, USA
    Horm Behav 53:217-24. 2008
    ....
  31. ncbi request reprint Synthesis of (bis)sulfonic acid, (bis)benzamides as follicle-stimulating hormone (FSH) antagonists
    Jay Wrobel
    Chemical Sciences, Wyeth Research, Inc, 500 Arcola Road, Collegeville, PA 19426, USA
    Bioorg Med Chem 10:639-56. 2002
    ..For instance, while stilbene (bis)sulfonic acid congener 2 was only 10-fold selective for FSHR over TSHR, analogue 50 with an IC(50) value of 0.9 microM in the FSHR-cAMP assay was essentially inactive at 30 microM in the TSHR-cAMP assay...
  32. doi request reprint Structure-activity relationships of the cycloalkanol ethylamine scaffold: discovery of selective norepinephrine reuptake inhibitors
    Paige E Mahaney
    Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA
    J Med Chem 51:4038-49. 2008
    ....
  33. doi request reprint 1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors
    Puwen Zhang
    Chemical Sciences, Wyeth Research, S 2250B, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA
    J Med Chem 52:5703-11. 2009
    ..In addition, compound 20 was also studied in the rat hot plate and spinal nerve ligation (SNL) models of acute and neuropathic pain, respectively, and was orally efficacious at doses of 3-10 mg/kg...
  34. doi request reprint Characterization of ligands for thyroid receptor subtypes and their interactions with co-regulators
    Elizabeth J Koury
    Women s Health and Musculoskeletal Biology, Wyeth Research, RN3164, 500 Arcola Road, Collegeville, PA 19426, United States
    Steroids 74:270-6. 2009
    ..The rank order among TR ligands at either receptor subtype in the biochemical assay correlated with the multiplex assay. These assays can be used to identify new ligands that can provide further insight into TR biology...
  35. doi request reprint Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231)
    David J O'Neill
    Chemical Sciences, Pfizer Global Research and Development, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA
    J Med Chem 53:4511-21. 2010
    ....
  36. ncbi request reprint Desvenlafaxine succinate identifies novel antagonist binding determinants in the human norepinephrine transporter
    John N Mason
    Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee, USA
    J Pharmacol Exp Ther 323:720-9. 2007
    ..In an initial search for molecular features that differentially define antagonist binding determinants, we document that Val148 in hNET transmembrane domain 3 selectively disrupts NIS binding but not that of DVS...