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A case report on the efficacy of vigabatrin analogue (1S, 3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115) in a patient with infantile spasms.
Epilepsy Behav Case Rep
September 2016
New York University School of Medicine, Comprehensive Epilepsy Center, 223 East 34th Street, New York, NY 10016, USA.
West Syndrome is characterized by infantile spasms, a hypsarrhythmic electroencephalogram (EEG) pattern, and a poor neurodevelopmental prognosis. First-line treatments include adrenocorticotrophic hormone (ACTH) and vigabatrin, but adverse effects often limit their use. CPP-115 is a high-affinity vigabatrin analogue developed to increase therapeutic potency and to limit retinal toxicity.
View Article and Find Full Text PDFChronic spinal and oral morphine-induced neuroendocrine and metabolic changes in noncancer pain patients.
Pain Med
April 2015
Department of Neurology, Pain Center and Division of Functional Neurosurgery.
Objective: Interactions between opioid use and hormonal function are documented in the literature. However, it is unclear if therapeutic intrathecal opioid therapy can induce hormonal changes, compared to oral opioid therapy.
Methods: The authors studied hormone and metabolic changes in 22 women (18-60 years) and 38 men (18-45 years) who were referred to a pain center.
Pharmacological characteristics of KP-102 (GHRP-2), a potent growth hormone-releasing peptide.
Arzneimittelforschung
February 2005
Department of Pharmacology, Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., Tokyo, Japan.
KP-102 (D-alanyl-3-(2-naphthyl)-D-alanyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide dihydrochloride, growth hormone-releasing peptide-2, GHRP-2, pralmorelin, CAS 158861-67-7), is a potent synthetic growth hormone (GH) secretagogue. In the present study, the pharmacological characteristics of the GH-releasing property of KP-102 were investigated by means of in vivo and in vitro experiments. In conscious rats, the GH-releasing activity of KP-102 was more potent than that of exogenously injected GH-releasing hormone (GHRH).
View Article and Find Full Text PDFAgouti-related protein (83-132) is a competitive antagonist at the human melanocortin-4 receptor: no evidence for differential interactions with pro-opiomelanocortin-derived ligands.
J Endocrinol
January 2004
School of Biological Sciences, University of Manchester, Stopford Building, Manchester M13 9PT, UK.
Interactions between pro-opiomelanocortin (POMC)-derived peptides, agouti-related protein (AGRP) and the melanocortin-4 receptor (MC4-R) are central to energy homeostasis. In this study we have undertaken comprehensive pharmacological analysis of these interactions using a CHOK1 cell line stably transfected with human MC4-R. Our main objectives were (1) to compare the relative affinities and potencies of POMC-derived peptides endogenously secreted within the hypothalamus, (2) to investigate the potency of AGRP(83-132) antagonism with respect to each POMC-derived peptide and (3) to determine whether AGRP(83-132) and POMC-derived peptides act allosterically or orthosterically.
View Article and Find Full Text PDFCarcinogen-induced impairment of enzymes for replicative fidelity of DNA and the initiation of tumours.
Carcinogenesis
March 2004
Institute of Medical and Veterinary Science, Adelaide, South Australia and Department of Pathology, University of Adelaide, SA 5005, Australia.
Not all carcinogens are mutagens, and many mutagens are not carcinogens. Among related chemicals, small changes of structure can markedly influence carcinogenic potency. Many tumours are genetically unstable, but some, especially 'benign' types, rarely exhibit 'progression' or show other evidence of genetic instability.
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