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11C-MK-8278 PET as a Tool for Pharmacodynamic Brain Occupancy of Histamine 3 Receptor Inverse Agonists

Autor: Anne Van Hecken, Sandra M. Sanabria-Bohórquez, David P. Mozley, Guy Bormans, Donald Burns, K. Cerchio, Lingling Han, Koenraad Van Laere, Terence G. Hamill, Marleen Depré, Inge De Lepeleire, Richard Hargreaves, John J. Renger, Robert Iannone, Michel Koole, Jan de Hoon, John Plalcza

Publikováno v: Journal of Nuclear Medicine. 55:65-72

The histamine 3 (H3) receptor is a presynaptic autoreceptor in the central nervous system that regulates the synthesis and release of histamine and modulates the release of other major neurotransmitters. H3 receptor inverse agonists (IAs) may be effi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16651dc8a94c52cb65c939f99a07b06f
https://doi.org/10.2967/jnumed.113.122515

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A single supratherapeutic dose of ridaforolimus does not prolong the QTc interval in patients with advanced cancer

Autor: Richard Lush, Michele Trucksis, Keith Orford, Diana Selverian, K. Cerchio, Mark Stroh, John A. Wagner, Nancy G. B. Agrawal, Scot Ebbinghaus, Jacqueline B. McCrea, Marian Iwamoto, Amita Patnaik, Daniel C. Sullivan, Xiaodong Li, Kyriakos P. Papadopoulos, Anthony W. Tolcher

Publikováno v: Cancer Chemotherapy and Pharmacology

Purpose This dedicated QTc study was designed to evaluate the effect of the mammalian target of rapamycin inhibitor, ridaforolimus, on the QTc interval in patients with advanced malignancies. Methods We conducted a fixed-sequence, single-blind, place

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f394bbf5592e421e63b00c24aa966700
https://doi.org/10.1007/s00280-012-1942-7

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Effect of Alendronate and MK-677 (a Growth Hormone Secretagogue), Individually and in Combination, on Markers of Bone Turnover and Bone Mineral Density in Postmenopausal Osteoporotic Women1

Autor: M. G. Murphy, K. Cerchio, Michael R. McClung, Barry J. Gertz, Stuart R. Weiss, J. Connor, Thomas J. Schnitzer, D Krupa

Publikováno v: The Journal of Clinical Endocrinology & Metabolism. 86:1116-1125

GH increases bone turnover and stimulates osteoblast activity. We hypothesized that administration of MK-677, an orally active GH secretagogue, together with alendronate, a potent inhibitor of bone resorption, would maintain a higher bone formation r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ad4120475b65893252274cd406225a87
https://doi.org/10.1210/jcem.86.3.7294

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Oral Administration of the Growth Hormone Secretagogue MK‐677 Increases Markers of Bone Turnover in Healthy and Functionally Impaired Elderly Adults

Autor: K. Cerchio, M. G. Murphy, James A. Bolognese, J. Ng, D Krupa, D. Plotkin, M. A. Bach, Barry J. Gertz

Publikováno v: Journal of Bone and Mineral Research. 14:1182-1188

Growth hormone (GH) stimulates osteoblasts in vitro and increases bone turnover and stimulates osteoblast activity when given to elderly subjects. Probably a major effect of GH on bone is mediated through stimulation of either circulating or locally

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9203f0aab00877f95ad1160e1c119b88
https://doi.org/10.1359/jbmr.1999.14.7.1182

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Treatment with the Oral Growth Hormone Secretagogue MK-677 Increases Markers of Bone Formation and Bone Resorption in Obese Young Males

Autor: Gail Murphy, John-Olov Jansson, Claes Ohlsson, Subburaman Mohan, D. Wyss, Johan Svensson, Barry J. Gertz, K. Cerchio, D Krupa, Bengt-Åke Bengtsson, Polvino William J, David J. Baylink

Publikováno v: Journal of Bone and Mineral Research. 13:1158-1166

The effect of 2 months of treatment with the oral growth hormone (GH) secretagogue MK-677 on markers of bone metabolism was determined in healthy obese male subjects. This was a randomized, double-blind, parallel, placebo-controlled study. Twenty-fou

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a726910318fb39c355d4788a7f5087e6
https://doi.org/10.1359/jbmr.1998.13.7.1158

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Two-Month Treatment of Obese Subjects with the Oral Growth Hormone (GH) Secretagogue MK-677 Increases GH Secretion, Fat-Free Mass, and Energy Expenditure1

Autor: Johan Svensson, D Krupa, Polvino William J, K. Cerchio, Lars Lönn, John-Olov Jansson, Barry J. Gertz, Gail Murphy, B.-Å. Bengtsson, I. Boseaus, D. Wyss, Lars Sjöström

Publikováno v: The Journal of Clinical Endocrinology & Metabolism. 83:362-369

Obesity is associated with blunted GH secretion, unfavorable body composition, and increased cardiovascular mortality. The objective of this study was to investigate the effects of oral treatment with the GH secretagogue MK-677 on GH secretion and bo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8b06a7a3f878e16a934543d502536e11
https://doi.org/10.1210/jcem.83.2.4539

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Oral Administration of Growth Hormone (GH) Releasing Peptide-Mimetic MK-677 Stimulates the GH/Insulin-Like Growth Factor-I Axis in Selected GH-Deficient Adults1

Autor: K. Cerchio, Polvino William J, D Krupa, Ora H. Pescovitz, Michael O. Thorner, Barry J. Gertz, Gail Murphy, Emily H. Skiles, Theresa Treep, Suzan S. Pezzoli, Ian Chapman

Publikováno v: The Journal of Clinical Endocrinology & Metabolism. 82:3455-3463

To determine the effect of the GH releasing peptide (GHRP)-mimetic, MK-677, on the GH/insulin-like growth factor-I (IGF-I) axis in selected GH-deficient adults, we studied nine severely GH-deficient men [peak serum GH concentration in response to ins

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a642c5dd40302400056ab0a3475e9bc0
https://doi.org/10.1210/jcem.82.10.4297

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Effect of L-000845704, an alphaVbeta3 integrin antagonist, on markers of bone turnover and bone mineral density in postmenopausal osteoporotic women

Autor: K. Cerchio, M. G. Murphy, Robert R. Recker, M. Wu, Keith Gottesdiener, S. A. Stoch

Publikováno v: The Journal of clinical endocrinology and metabolism. 90(4)

The αVβ3 integrin (vitronectin receptor) plays a pivotal role in bone resorption. We hypothesized that L-000845704, an αVβ3 integrin antagonist, would potently inhibit bone resorption, thereby increasing bone mass as assessed by bone mineral dens

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7c3cf44ec4e0900d05a2d4b6b235de9
https://pubmed.ncbi.nlm.nih.gov/15814776

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Effects of oral administration of ibutamoren mesylate, a nonpeptide growth hormone secretagogue, on the growth hormone-insulin-like growth factor I axis in growth hormone-deficient children

Autor: K. Cerchio, Alejandra Avila, M. Verónica Mericq, D Krupa, Fernando Cassorla, Ora H. Pescovitz, Gail Murphy, Barry J. Gertz, Johan Svensson, Ethel Codner, Anatoly N. Tiulpakov

Publikováno v: Clinical pharmacology and therapeutics. 70(1)

Ibutamoren mesylate (MK-0677), an orally active nonpeptide growth hormone (GH) secretagogue, stimulates GH release through a pituitary and hypothalamic receptor that is different from the GH-releasing hormone receptor. We evaluated the safety and tol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1198159e326f9f1bce277f1f602cc677
https://pubmed.ncbi.nlm.nih.gov/11452249

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Oral administration of the growth hormone secretagogue MK-677 increases markers of bone turnover in healthy and functionally impaired elderly adults. The MK-677 Study Group

Autor: M G, Murphy, M A, Bach, D, Plotkin, J, Bolognese, J, Ng, D, Krupa, K, Cerchio, B J, Gertz

Publikováno v: Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research. 14(7)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::74d2ff8065b4fc11784a71ddb9edd2c8
https://pubmed.ncbi.nlm.nih.gov/10404019

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