Estimation of Magnitudes of Alternative Metabolic Pathways

Kopin, Irwin J.

doi:10.1002/9780470110294.ch5

Cited by 8 publications

(5 citation statements)

References 25 publications

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“…The fractional norepinephrine spillover of total norepinephrine released varies substantially between different organ systems (kidneys, 1:3; skeletal muscle, 1:12; heart, Ͻ1:20). 59 This should be consid- ered when evaluating the degree of sympathetic neural activation to single organs by the organ norepinephrine spillover technique. 67,68,82 There has been particular interest in cardiac norepinephrine spillover, which contributes only 2-3% (50 -150 pmol/ min) to total norepinephrine spillover under supine resting conditions in healthy, young volunteers.…”

Section: Methods Of Assessment Of Norepinephrine Plasma Concentrationmentioning

confidence: 99%

Sympathetic Nervous System

Neukirchen¹,

Kienbaum²,

Warner³

et al. 2008

Anesthesiology

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For more than 100 yr, scientists have studied the sympathetic nervous system and its cardiovascular control mechanisms. Muscle sympathetic activity is the most important direct and rapidly responding variable for evaluation of sympathetic neural outflow. Because of its significance in response to environmental challenges and its role in cardiovascular control, great attention has been paid to the sympathetic nervous system in both health and disease and, more recently, also during general anesthesia. In fact, general anesthesia can also be considered as an investigational tool to assess mechanisms of cardiovascular regulation. This review evaluates different methods for determination of sympathetic nervous system activity and describes its role in human neurohumoral circulatory control. Furthermore, the effects of general anesthesia on sympathetic nervous system activity and their relevance for clinical anesthesia are discussed.

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Section: Methods Of Assessment Of Norepinephrine Plasma Concentrationmentioning

confidence: 99%

Sympathetic Nervous System

Neukirchen¹,

Kienbaum²,

Warner³

et al. 2008

Anesthesiology

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“…The compound has micromolar activity for the GLP-1 receptor in recombinant cell assays of cAMP [21]. No other studies have been disclosed with this kind of molecule.…”

Section: Low Molecular Weight Glp-1 Receptor Agonistsmentioning

confidence: 99%

“…T-0632 can be considered an allosteric modulator of the GLP-1 receptor. Additionally, there is some evidence indicating the compound behaves as an inverse agonist in a constitutively active GLP-1 receptor system [ 21 ]. Although this compound could be a good tool for in vivo studies considering its physicochemical properties (it passes all of the Lipinski and Veber rules), the weak affinity of T-0632 for the GLP-1 receptor combined with its subnanomolar CCK1 antagonist activity renders it largely inadequate as a research tool to study the GLP-1 receptor.…”

Section: Low Molecular Weight Glp-1 Receptor Antagonistsmentioning

confidence: 99%

“…There have been other efforts aimed at exploring this scaffold. Scientists from the New England Medical Center claimed a series of 2-thiosubstituted quinoxalines, represented by compound 10 ( Figure 2 ( 10 ) 2-(3-methylquinoxalin-2-yl)sulfanyl- N -phenyl-acetamide), as weak GLP-1 receptor agonists [ 21 ]. Zydus also studied analogs of compound 8 but did not show improved activity over this compound in glucose dependent insulin secretion assays using RINmF5 insulinoma cells [ 32 ].…”

Section: Low Molecular Weight Glp-1 Receptor Agonistsmentioning

confidence: 99%

“…A series of pyrazoles represented by compound 19 ( Figure 2 ( 19 ) 4-chloro-2-[[( E) -2-(2,5-dimethyl-4-nitro-pyrazol-3-yl)vinyl]amino]phenol) were identified by Kopin and Beinborn as weak agonists of the GLP-1 receptor [ 21 ]. The compound has micromolar activity for the GLP-1 receptor in recombinant cell assays of cAMP [ 21 ]. No other studies have been disclosed with this kind of molecule.…”

Section: Low Molecular Weight Glp-1 Receptor Agonistsmentioning

confidence: 99%

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Small Molecule Drug Discovery at the Glucagon-Like Peptide-1 Receptor

Willard

Bueno

Sloop

2012

Experimental Diabetes Research

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The therapeutic success of peptide glucagon-like peptide-1 (GLP-1) receptor agonists for the treatment of type 2 diabetes mellitus has inspired discovery efforts aimed at developing orally available small molecule GLP-1 receptor agonists. Although the GLP-1 receptor is a member of the structurally complex class B1 family of GPCRs, in recent years, a diverse array of orthosteric and allosteric nonpeptide ligands has been reported. These compounds include antagonists, agonists, and positive allosteric modulators with intrinsic efficacy. In this paper, a comprehensive review of currently disclosed small molecule GLP-1 receptor ligands is presented. In addition, examples of “ligand bias” and “probe dependency” for the GLP-1 receptor are discussed; these emerging concepts may influence further optimization of known molecules or persuade designs of expanded screening strategies to identify novel chemical starting points for GLP-1 receptor drug discovery.

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Biosynthesis and secretion of steroids by the canine testis

Molen

Eik‐Nes

1971

Biochimica et Biophysica Acta (BBA) - Lipids and Lipid Metaboli

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Estimation of Magnitudes of Alternative Metabolic Pathways

Cited by 8 publications

References 25 publications

Sympathetic Nervous System

Sympathetic Nervous System

Small Molecule Drug Discovery at the Glucagon-Like Peptide-1 Receptor

Biosynthesis and secretion of steroids by the canine testis

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