Receptor agonist - Factbites

Receptor agonist - Factbites
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Topic: Receptor agonist

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	beta 2-Adrenergic Receptor Pharmacogenetics -- LIGGETT 161 (3): 197 -- American Journal of Respiratory and Critical Care Medicine
		Adrenergic receptor haplotypes in mild, moderate and fatal/ near fatal asthma.
		-adrenergic receptor in nocturnal and non-nocturnal asthma: evidence that Gly 16 correlates with the nocturnal phenotype.
		Transfected CHW cells (A) or airway smooth muscle cells (B) expressing the indicated polymorphic receptors were exposed to vehicle or isoproterenol (1 µM) in cell culture for 24 h and receptor density was determined by radioligand binding.
	ajrccm.atsjournals.org /cgi/content/full/161/3/S1/S197

	Online Pharmacy
		beta-Adrenergic receptor subtypes in melanophores of the marine gobies Tridentiger trigonocephalus and Chasmichthys gulosus.
		Beta-1 receptor is the predominant beta-adrenoreceptor on rat brown adipose tissue.
		Increased beta-receptor density and improved hemodynamic response to catecholamine stimulation during long-term metoprolol therapy in heart failure from dilated cardiomyopathy.
	www.hairmillion.com /rx-online-info/metoprolol-online-literature.html

	New Horizons In Asthma: Importance Of b2 Adrenergic Receptor Polymorphisms
		adrenergic receptors are expressed in all cell types comprising the airway including smooth muscle, epithelial cells, blood vessels and cholinergic nerves; they are also expressed in inflammatory cells, and in cells and vessels of the peripheral lung and in circulating lymphocytes.
		adrenergic receptor are not a primary cause of asthma.
		Genetic polymorphisms of the beta 2-adrenergic receptor in nocturnal and nonnocturnal asthma.
	www.dcmsonline.org /jax-medicine/1999journals/nov99/horizons.htm

	Brethine Pharmacology, Pharmacokinetics, Studies, Metabolism - Terbutaline Sulfate - RxList Monographs
		The pharmacologic effects of beta-adrenergic agonists, including terbutaline, are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic 3',5'-adenosine monophosphate (cAMP).
		-adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta
		Increased cAMPlevels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.
	www.rxlist.com /cgi/generic3/terbutaline_cp.htm

	Gi-Dependent Localization of beta 2-Adrenergic Receptor Signaling to L-Type Ca2+ Channels -- Chen-Izu et al. 79 (5): 2547 -- Biophysical Journal
		A plausible determinant of the specificity of receptor signaling is the cellular compartment over which the signal is broadcast.
		Pharmacological characterization of the receptors involved in the beta-adrenoceptor-mediated stimulation of the L-type Ca current in frog ventricular myocytes.
		Compartmentalized structure of the plasma membrane for receptor movements as revealed by a nanometer-level motion analysis.
	www.biophysj.org /cgi/content/full/79/5/2547

	American Pain Foundation
		Foradil is a bronchodilator that belongs to the long-acting beta2-adrenergic receptor agonist class of compounds.
		The pharmacologic effects of beta2 adrenoceptor agonist drugs, including formoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cyclic AMP).
		Adverse reactions to treatment with Foradil are similar to those observed with other selective beta2-adrenoceptor agonists.
	www.centerwatch.com /cgi-bin/cl.pl?p=patient/drugs/dru724.html&h=painfoundhead.txt&f=painfoundfoot.txt

	Adrenal Medullary Hormones
		The alpha and beta adrenergic receptors and their subtypes were originally defined by differential binding of various agonists and antagnonists and, more recently, by analysis of molecular clones.
		These receptors are prototypical examples of seven-pass transmembrane proteins that are coupled to G proteins which stimulate or inhibit intracellular signalling pathways.
		The physiologic effects of epinephrine and norepinephrine are initiated by their binding to adrenergic receptors on the surface of target cells.
	arbl.cvmbs.colostate.edu /hbooks/pathphys/endocrine/adrenal/medhormones.html

	Texas Medicaid: Vendor Drug, Aerosolized Agents - Metered-Dose Inhalers: Anticholinergic Drugs - Ipratropium (Atrovent®)
		Combined ipratropium and beta2-adrenergic receptor agonist in acute asthma.
		agonists in some patients to manage more severe acute asthma exacerbations.
		Ipratropium is supplied as a metered dose inhaler which supplies 18 micrograms of active drug with each actuation.
	www.hhsc.state.tx.us /HCF/vdp/Criteria/antichoa.html

	Department of Critical Care Medicine
		Homozygosity for Arginine16 is associated with early onset agonist-mediated desensitization and decreased vascular responsiveness, while homozygosity for Glycine16 is associated with resistance to desensitization and enhanced vascular responsiveness to agonist stimulation regardless of the amino acid present at position 27.
		The results suggest that it is the allele encoding the amino acid at position 16 of the receptor protein that determines vascular responsiveness.
		The subjects were exposed to the same experimental conditions and "treatments" (agonist challenge), and similar "outcome measures" (vasodilation and desensitization) were determined for all groups.
	www.ccm.upmc.edu /education/journal_club/jcwilner.htm

	National ME/FM Action Network
		The beta2-adrenergic receptor agonist terbutaline inhibits tumor necrosis factor-alpha production and enhances interleukin-10 production by monocytes.
		We examined the sensitivity of the immune system to the glucocorticoid agonist dexamethasone and the beta2-adrenergic agonist terbutaline in 15 adolescent girls with CFS and 14 age- and sex-matched controls.
		Our data demonstrate that the capacity of a beta2-adrenergic agonist to regulate the production of these two cytokines is also reduced in CFS patients.
	www.mefmaction.net /default.aspx?page=youthabstract017

	G Protein-Coupled Receptor Kinases 3 and 6 Use Different Pathways to Desensitize the Endogenous M3 Muscarinic Acetylcholine Receptor in Human SH-SY5Y Cells -- Willets et al. 60 (2): 321 -- Molecular Pharmacology
		Regulation of the rate of receptor phosphorylation and dephosphorylation by agonist occupancy and effects on coupling of the receptor to the guanine nucleotide regulatory protein.
		Krupnick JG and Benovic JL (1998) The role of receptor kinases and arrestins in G protein-coupled receptor regulation.
		Sterne-Marr R and Benovic JL (1996) Regulation of G protein-coupled receptors by receptor kinases and arrestins.
	molpharm.aspetjournals.org /cgi/content/full/60/2/321

	Title page for ETD etd-04252005-223842
		We further defined the adrenergic receptor population on bovine neutrophils to be dominated by the beta2-subtype.
		Dysfunction of beta-adrenergic receptors is known to contribute to the pathophysiology of numerous diseases in both people and animals.
		Additional studies that identify the PKC isoform repertoire in bovine neutrophils may illustrate the potential for selective inhibition, and may lead to more specific identification and treatment of beta2-adrenergic receptor mechanism dysfunction.
	scholar.lib.vt.edu /theses/available/etd-04252005-223842

	Peter H. Fishman, Ph.D., Senior Investigator
		The latter consists of G protein-coupled receptors (GPCRs) that bind hormones and neurotransmitters, G proteins that transduce the signal, and a catalyst that generates cAMP, the intracellular second messenger.
		Arrestin both uncouples receptors from G proteins and by binding to clathrin, recruits the receptors into the clathrin-coated pit endocytic pathway.
		One of the signals that targets receptors to lysosomes and proteolytic degradation is ubiquitination.
	neuroscience.nih.gov /Lab.asp?Org_ID=27

	Online Pharmacy, Tramadol, Paxil, antibiotics, amoxicillin, zithromax, Rx Online, pharmaceuticals, DHEA, prescription medications, prescription drugs.
		Activation of the Cl- current by the nonselective beta-receptor agonist isoproterenol (Iso) was not affected by the beta2-receptor antagonist ICI-118,551 (ICI), but it was blocked by the beta1-receptor antagonist atenolol.
		The inability of beta2-receptor stimulation to activate the Cl- current was confirmed by the lack of response to the selective beta2-receptor agonists salbutamol and zinterol.
		To verify that the lack of response to beta2-receptor stimulation was not unique to the Cl- current, the effects of beta2-receptor agonists on the L-type Ca2+ current were also examined.
	www.hairmillion.com /rx-online-info/atenolol-online-rx/atenolol-online-rx.695.html

	Terbutaline - Wikipedia, the free encyclopedia
		-adrenergic receptor agonist, used as a fast-acting bronchodilator and to delay premature labour as a tocolytic.
		This page was last modified 10:17, 3 July 2005.
		The drug Terbutaline (trade names Brethine, Bricanyl, or Brethaire) is a β
	en.wikipedia.org /wiki/Terbutaline

	beta 2-Adrenergic Receptor Haplotypes in Mild, Moderate and Fatal/Near Fatal Asthma -- WEIR et al. 158 (3): 787 -- American Journal of Respiratory and Critical Care Medicine
		A biallelic DNA polymorphism of the human beta-2 adrenergic receptor detected by Ban I Adbr 2.
		Beta agonists and the risk of asthma death in near-fatal asthma.
		Polymorphism in the human beta-2 adrenergic receptor gene detected by restriction endonuclease digestions with Fnu 4HI.
	ajrccm.atsjournals.org /cgi/content/full/158/3/787

	ARDB Reference Detail Information
		We have been testing the hypothesis that genetic manipulation of the myocardial beta-adrenergic receptor (beta-AR) system, which is impaired in HF, can enhance cardiac function.
		Thus, replacement of lost receptors seen in HF may represent novel inotropic therapy.
		Before gene therapy approaches to alter cardiac function can be realized, efficient and reproducible in vivo gene techniques must be established to efficiently transfer transgenes globally to the myocardium.
	ardb.bjmu.edu.cn /detail/ARRef_detail.asp?PubmedID=10393695

	Dynamin-association with agonist-mediated sequestration of beta-adrenergic receptor in single-cell eukaryote Paramecium -- Wiejak et al. 207 (10): 1625 -- Journal of Experimental Biology
		Dynamin-association with agonist-mediated sequestration of beta-adrenergic receptor in single-cell eukaryote Paramecium -- Wiejak et al.
		receptor responsiveness upon agonist stimulation and it is a
		to the appearance of this receptor in unicellular eukaryotes.
	jeb.biologists.org /cgi/content/full/207/10/1625

	NEJM -- The Effect of Common Polymorphisms of the {beta}2-Adrenergic Receptor on Agonist-Mediated Vascular Desensitization
		receptor, one at codon 16 and one at codon 27, on agonist-mediated
		NEJM -- The Effect of Common Polymorphisms of the {beta}2-Adrenergic Receptor on Agonist-Mediated Vascular Desensitization
		Keys, J. R., Zhou, R.-H., Harris, D. M., Druckman, C. A., Eckhart, A. Vascular Smooth Muscle Overexpression of G Protein-Coupled Receptor Kinase 5 Elevates Blood Pressure, Which Segregates With Sex and Is Dependent on Gi-Mediated Signaling.
	content.nejm.org /cgi/content/abstract/345/14/1030

	Advair Diskus Clinical Pharmacology - Salmeterol/Fluticasone - HealthScout
		In vitro assays using human lung cytosol preparations have established fluticasone propionate as a human glucocorticoid receptor agonist with an affinity 18 times greater than dexamethasone, almost twice that of beclomethasone-17-monopropionate (BMP), the active metabolite of beclomethasone dipropionate, and over 3 times that of budesonide.
		These drugs represent 2 classes of medications (a synthetic corticosteroid and a selective, long-acting beta-adrenergic receptor agonist) that have different effects on clinical and physiological indices.
		Although beta2-adrenoceptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-adrenoceptors are the predominant receptors in the heart, there are also beta2-adrenoceptors in the human heart comprising 10% to 50% of the total beta-adrenoceptors.
	www.healthscout.com /rxdetail/1/33/5/main.html

	Pharmacology/Toxicology : College of Pharmacy : UT Austin
		Also, these results have shown important similarities and differences in the structural requirements for agonist affinity at closely related receptors (receptor subtypes and wild type vs. point mutant variants).
		Key results in this area have demonstrated an increase in accuracy and precision of agonist affinity measurements when data from recombinant receptors stably expressed in cell lines are used.
		Key results in this area have demonstrated an improved ability to determine agonist efficacy when studies of second messenger function are used in clonal cell lines stably expressing the receptor.
	www.utexas.edu /pharmacy/divisions/pharmtox/faculty/wilcox.html

	NHLBI Working Group Polymorphisms of the Beta-adrenergic Receptor Gene: Implications for the Pharmacotherapy of Asthma, Executive Summary, NIH, DHHS
		Polymorphisms of the Beta-adrenergic Receptor Gene: Implications for the Pharmacotherapy of Asthma
		Despite major recent advances in the understanding of the structure and function of the beta2 adrenergic receptor (beta2AR), several questions with relevant clinical implications remain to be answered, requiring a stepwise approach.
		Recent findings of a genotyped stratified prospective trial conducted by the NIH Asthma Clinical Research Network (ACRN) prompted the organization of a meeting to examine the role of polymorphisms of the beta-adrenergic receptor gene in relation to asthma treatment as well as to consider new opportunities in the field of asthma pharmacogenetics.
	www.nhlbi.nih.gov /meetings/workshops/pharm_execsum.htm

	美国专利申请公开说明书 20040209860 - Biphenyl derivatives having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity
		The biphenyl derivatives of the invention possess both β2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
		Biphenyl derivatives having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity
		美国专利申请公开说明书 20040209860 - Biphenyl derivatives having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity
	cxp.paterra.com /uspregrant20040209860cn.html

	IngentaConnect Long-acting beta2-adrenergic receptor agonist in pediatric asthma
		2-adrenergic receptor agonist; pediatric asthma; salmeterol; 2-adrenergic receptor agonist">short-acting
		-adrenergic receptor agonists (LABA), a class of agents for the long-term management of childhood bronchial asthma, are recommended for use in combination with steroid inhalation for the treatment of the morning dip in severe childhood asthma.
		IngentaConnect Long-acting beta2-adrenergic receptor agonist in pediatric asthma
	www.ingentaconnect.com /content/bsc/ain/2004/00000053/00000002/art00006

	BodyBuilding4Life - Clenbuterol
		Myocyte-specific necrosis in the heart and soleus muscle of adult male Wistar rats was investigated in response to a single subcutaneous injection of the anabolic beta(2)-adrenergic receptor agonist clenbuterol.
		Methylation of the phospholipids is stimulated by the binding of beta agonists to their receptors.
		However, Beta receptors are embedded in the cell's outer phospholipid membrane.
	www.bodybuilding4life.com /forums/showthread.php?t=5399

	ARDB Reference Detail Information
		Next, the effects of increasing doses of the beta2-adrenergic receptor agonist zinterol on Ca2+ transient amplitudes were examined in ventricular myocytes.
		The cardiomyocyte response to isoproterenol (10(-7) mol/L) in the presence or absence of the selective beta1- (CGP-20712A, 300 nmol/L) or beta2- (ICI 118,551, 100 nmol/L) adrenergic receptor antagonist was also examined.
		§ Beta2-adrenergic receptor antagonists protect against ventricular fibrillation: in vivo and in vitro evidence for enhanced sensitivity to beta2-adrenergic stimulation in animals susceptible to sudden death.
	ardb.bjmu.edu.cn /detail/ARRef_detail.asp?PubmedID=9323081

	Novel Actions of Inverse Agonists on 5-HT2C Receptor Systems -- Berg et al. 55 (5): 863 -- Molecular Pharmacology
		Pranzatelli MR, Murthy JN and Tailor PT (1993) Novel regulation of 5-HTic receptors: Down-regulation induced both by 5-HTic/2 receptor agonists and antagonists.
		Because the action of the inverse agonist to enhance responsiveness of the purinergic receptor system is through its interaction
		Felder CC, Kanterman RY, Ma AL and Axelrod J (1990) Serotonin stimulates phospholipase A2 and the release of arachidonic acid in hippocampal neurons by a type 2 serotonin receptor that is independent of inositolphospholipid hydrolysis.
	molpharm.aspetjournals.org /cgi/content/full/55/5/863

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