Please use this identifier to cite or link to this item:
https://ahro.austin.org.au/austinjspui/handle/1/9304
Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Louis, Simon N S | en |
dc.contributor.author | Jackman, G P | en |
dc.contributor.author | Nero, Tracy L | en |
dc.contributor.author | Iakovidis, D | en |
dc.contributor.author | Louis, William J | en |
dc.date.accessioned | 2015-05-15T22:21:12Z | - |
dc.date.available | 2015-05-15T22:21:12Z | - |
dc.date.issued | 2000-12-01 | en |
dc.identifier.citation | Cardiovascular Drugs and Therapy / Sponsored By the International Society of Cardiovascular Pharmacotherapy; 14(6): 565-77 | en |
dc.identifier.govdoc | 11300357 | en |
dc.identifier.other | PUBMED | en |
dc.identifier.uri | https://ahro.austin.org.au/austinjspui/handle/1/9304 | en |
dc.description.abstract | In vitro lipolysis stimulated by low (-)-isoprenaline concentrations (< or =30 nM) in epididymal white adipocytes from Sprague-Dawley rats was inhibited at least 60-80% by the specific beta1-antagonists LK 204-545 and CGP 20712A (1 microM), suggesting that at these low (10 nM) concentrations of (-)-isoprenaline lipolysis was primarily (80%) but not solely mediated via beta1-adrenergic receptors. Low concentrations (100 nM) of (-)-noradrenaline and formoterol also confirmed a role for beta1-adrenergic receptors in mediating lipolysis at low concentrations of these agonists. At higher agonist concentrations, beta3-adrenergic receptors were fully activated and were the dominant beta-adrenergic receptor subtype mediating the maximum lipolytic response, and the maximum response was not affected by the beta1-antagonists, demonstrating that the beta3-receptor is capable of inducing maximum lipolysis on its own. Studies of lipolysis induced by the relatively beta2-selective agonist formoterol in the presence of beta1-blockade (1 microM CGP 20712A) demonstrated the inability of the beta2-selective antagonist ICI 118-551 to inhibit the residual lipolysis at concentrations of ICI 118-551 < or = 1 microM. Higher concentrations of ICI 118-551 inhibited the residual formoterol-induced lipolysis competetively, but with low affinity (approximately 500-fold lower than its beta2-adrenergic receptor pA2, 7.80 +/- 0.21), suggesting that formoterol was not acting via beta2-adrenergic receptors. These data are consistent with beta1-adrenergic receptors playing an important role in lipolysis at physiological but not pharmacological concentrations of catecholamines and that beta2-adrenergic receptors play no obvious direct role in mediating beta-adrenergic receptor agonist-induced lipolysis in vitro. Finally, racemic-SR 59230A, unlike the pure (S, S)-isomer (a beta3-selective antagonist), was found to be a nonselective antagonist at the three beta-adrenergic receptor subtypes, showing that the other enantiomers have different selectivity. | en |
dc.language.iso | en | en |
dc.subject.other | Adipocytes.drug effects.metabolism | en |
dc.subject.other | Adrenergic beta-Agonists.pharmacology | en |
dc.subject.other | Adrenergic beta-Antagonists.pharmacology | en |
dc.subject.other | Animals | en |
dc.subject.other | Dose-Response Relationship, Drug | en |
dc.subject.other | Female | en |
dc.subject.other | Heart Rate.drug effects | en |
dc.subject.other | In Vitro Techniques | en |
dc.subject.other | Lipolysis.physiology | en |
dc.subject.other | Male | en |
dc.subject.other | Rats | en |
dc.subject.other | Rats, Sprague-Dawley | en |
dc.subject.other | Receptors, Adrenergic, beta.physiology | en |
dc.subject.other | Receptors, Adrenergic, beta-1.physiology | en |
dc.subject.other | Receptors, Adrenergic, beta-2.physiology | en |
dc.subject.other | Receptors, Adrenergic, beta-3.physiology | en |
dc.title | Role of beta-adrenergic receptor subtypes in lipolysis. | en |
dc.type | Journal Article | en |
dc.identifier.journaltitle | Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy | en |
dc.identifier.affiliation | University of Melbourne, Clinical Pharmacology and Therapeutics Unit, Austin and Repatriation Medical Centre, Heidelberg, Victoria, Australia | en |
dc.description.pages | 565-77 | en |
dc.relation.url | https://pubmed.ncbi.nlm.nih.gov/11300357 | en |
dc.type.austin | Journal Article | en |
local.name.researcher | Louis, William J | |
item.openairetype | Journal Article | - |
item.languageiso639-1 | en | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | No Fulltext | - |
item.grantfulltext | none | - |
crisitem.author.dept | Clinical Pharmacology and Therapeutics | - |
Appears in Collections: | Journal articles |
Items in AHRO are protected by copyright, with all rights reserved, unless otherwise indicated.