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Topic: Agonist

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Bioavailability

	Agonist - Wikipedia, the free encyclopedia
		An agonist is a substance that binds to a receptor and triggers a response in the cell.
		An agonist is the opposite of an antagonist in the sense that while an antagonist also binds to the receptor, it fails to activate the receptor and actually blocks it from activation by agonists.
		An agonist is a chemical contestant or contender.
	en.wikipedia.org /wiki/Agonist (166 words)

	Lesson 7 (Site not responding. Last check: 2007-11-06)
		Partial agonists by virtue of the occupation of a large number of receptors without eliciting a response, competitively block the effects of agonists of higher intrinsic efficacies or full agonists.
		In contrast, the partial agonist in the presence of concentration of the full agonist that produce responses higher than those of the partial agonist (more than 20%) has antagonistic effects, decreasing the response of the full agonist to the level of the maximal response of the partial agonist (20%).
		The increase in concentrations of the partial agonist required to antagonize the effects of increasingly higher concentrations of full agonist are indicative of the competitive nature of the effect.
	www.med.unc.edu /wrkunits/2depts/pharm/receptor/lesson7.htm (1079 words)

	University of Miami School of Medicine - Glossary - Agonist
		Agonist: A drug that binds to a receptor of a cell and triggers a response by the cell.
		Dopamine agonists mimic the effects of dopamine in the brain by stimulating dopamine receptors with a lower risk of the uncontrollable and irreversible dyskinesias often associated with levodopa therapy.
		For example, LHRH (luteinizing hormone-releasing hormone) agonists are similar to LHRH in structure and are able to mimic the effects of LHRH, a hormone that controls sex hormones in both men and women.
	www.med.miami.edu /glossary/art.asp?articlekey=7835 (206 words)

	World Intellectual Property Organization (Site not responding. Last check: 2007-11-06)
		It is also an object of the invention to provide agonist therapy in which the analgesically effective blood levels of the opioid agonist are maintained during an extended period of time, while also maintaining the pharmacologically effective blood levels of the antagonist for reducing the side effects associated with the opioid treatment.
		comprising opioid agonist and opioid antagonist, wherein the opioid agonist is present in an amount that is analgesically effective when administered to a human, and wherein the opioid antagonist is present in an amount which does not cause a reduction in the level of analgesia provided by the dosage form to a non-therapeutic level.
		are controlled to maintain an analgesically effective amount of the agonist in the blood throughout the dosing period and to maintain the concentration of the opioid antagonist throughout the dosing period sufficient for decreasing the side effects associated with the opioid agonist but not sufficient to negate the analgesic efficacy of the agonist.
	www.wipo.int /ipdl/IPDL-CIMAGES/view/pct/getbykey5?KEY=01/58447.010816&ELEMENT_SET=DECL (9196 words)

	CD Baby: AGONIST: Infinite Resistance
		Agonist started its gradual formation in the summer of 1997.
		This twelve-track freshman effort is mostly an exercise in the heavier side of classic rock with the metal, prog, and psychodelic elements that would later come to define Agonist budding on several tracks throughout the disc.
		After over a year of continued live performance and writing new material, Agonist (newly-renamed) went back into the studio in the spring and summer of 2000 to record "Infinite Resistance," an album which encapsulated much of the band's large scope of musical curiosity and ability.
	www.cdbaby.com /cd/agonist (686 words)

	Physiology Basics: Receptors
		Such antagonism is commonly reversible by increasing the concentration of agonist (competitive antagonism) but sometimes we get lucky and find an antagonist that blocks the receptor by binding at a separate site, and this is not overcome by increasing the concentration of agonist.
		Agonists shifts the equilibrium in the direction of the active form - by binding the active form more avidly, they drive things in the direction of activation.
		Similarly, partial agonists have only a slightly higher affinity for the active receptor than for the inactive form, so they display some agonism, but interfere with the function of a 'full' agonist.
	www.anaesthetist.com /physiol/basics/receptor/receptor.htm (1938 words)

	Dependence of Nicotinic Acetylcholine Receptor Recovery from Desensitization on the Duration of Agonist Exposure -- ...
		Recovery pulses were elicited with the same agonist used for induction of desensitization (ordinate, normalized to the peak current produced during the desensitizing pulse) as a function of time interval between desensitizing and test pulses (abscissa, seconds).
		For mixed agonist experiments, a different agonist was used for the test pulse than for the desensitization pulse.
		1 except that the agonist used for the desensitizing pulse was different from the agonist used in the test pulses during the recovery phase.
	jpet.aspetjournals.org /cgi/content/full/289/2/656 (3829 words)

	The operational model of agonist action
		The EC reflects both the ability of the drug to bind to its receptor (the agonist's affinity) and the ability of the drug to cause a response once it is bound (the agonist's efficacy).
		They then proved mathematically that if agonist binding is hyperbolic and the dose-response curve has a Hill slope of 1.0, the equation linking the concentration of agonist occupied receptors to response must also be hyperbolic.
		Basal is the measured response in the absence of agonist.
	www.curvefit.com /operational_model_.htm (1832 words)

	British Journal of Pharmacology - Roles of threonine 192 and asparagine 382 in agonist and antagonist ... (Site not responding. Last check: 2007-11-06)
		Binding of the endogenous muscarinic agonist acetylcholine (ACh) is initiated by an ion-ion interaction between the negatively charged Asp residue in TM III and the positively charged quaternary amine (Wess et al., 1991; 1992; Blüml et al., 1994).
		Since A9 L cells provide a suitable system for determining muscarinic agonist activities and G-protein coupling interactions (Brann et al., 1987; Messer et al., 1997), mutant receptors were compared to HM (WT) receptors in A9 L cells for their abilities to mediate phosphatidylinositol (PI) metabolism (Figure 3 and Table 4).
		Muscarinic agonists used in functional assays were also tested in inhibition binding assays to determine the effects of mutations on agonist binding interactions (Table 5 and Figures 5 and 6).
	www.nature.com /bjp/journal/v126/n3/full/0702301a.html (5783 words)

	Varenicline: An 42 Nicotinic Receptor Partial Agonist for Smoking Cessation (Site not responding. Last check: 2007-11-06)
		Thus, we anticipated that a partial agonist would be uniquely suited as a treatment for this condition.
		These latter results of combining an agonist and antagonist-essentially creating a partial agonist-suggested that an agent with an optimal partial agonist profile and physicochemical properties could provide improved relief to patients during smoking cessation attempts.
		Partial agonist activity was further demonstrated in vivo by evaluating the antagonist properties of (-)-cytisine, (±)-8, and varenicline (1).
	pubs.acs.org /cgi-bin/jcen?jmcmar/48/i10/html/jm050069n.html (2962 words)

	Partial Agonist Activity of Bucindolol Is Dependent on the Activation State of the Human {beta}1-Adrenergic Receptor -- ...
		Partial Agonist Activity of Bucindolol Is Dependent on the Activation State of the Human {beta}1-Adrenergic Receptor -- Maack et al.
		Effect of agonist and inverse agonist pretreatment on forskolin and isoproterenol sensitivities.
		Human atrial myocardium was pretreated with agonist isoproterenol (1 µmol/L), inverse agonist metoprolol (30 µmol/L), or vehicle for 60 minutes.
	circ.ahajournals.org /cgi/content/full/108/3/348 (2754 words)

	Agonist-antagonists (Site not responding. Last check: 2007-11-06)
		the ability to antagonize an agonist at one of the opioid receptors.
		Butorphanol is popular as an preoperative and postoperative analgesic and has agonist activity at the kappa receptor.
		It seems to have some agonist properties at the mu receptor and antagonist activity at the kappa receptor but the onset of action is rather slow, 20 to 30 minutes.
	cvm.msu.edu /services/aneth/docs/analges/agonist-.htm (230 words)

	[No title] (Site not responding. Last check: 2007-11-06)
		This is because 50 % of the receptors are occupied by a compound which is a partial agonist capable of increasing heart rate by only 50 %.
		Pedigolol must be displaced by the higher intrinsic activity agonist before the actions of isoproterenol can be fully seen.
		This is because all receptors are occupied by the partial agonist.
	www.mc.uky.edu /Pharmacology/instruction/pha824mp/partial.htm (619 words)

	Agonist Watch :
		The Agonist is paying for links on Google, but they may want to reconsider this particular search word combination.
		Agonist pageviews are definately trending down, but I suspect this is part of the normal weekly pattern coupled with lessening interest in the war.
		They hyped the whole warblogger thing (when they needed to fill in some spots) and put the Agonist, Command-Post and others on the map, drawing a whole new audience that didn't know what a blog was two or three weeks ago.
	wcnbdhusicf.blogspot.com (5827 words)

	Induction of an Antigen-Specific CTL Response by a Conformationally Biased Agonist of Human C5a Anaphylatoxin as a ...
		Induction of an Antigen-Specific CTL Response by a Conformationally Biased Agonist of Human C5a Anaphylatoxin as a Molecular Adjuvant -- Ulrich et al.
		the HBsAg CTL epitope and the C5a agonist for CTL induction,
		Decapeptide agonists of human C5a: the relationship between conformation and spasmogenic and platelet aggregatory activities.
	www.jimmunol.org /cgi/content/full/164/10/5492 (4664 words)

	Chronic Treatment with an Agonist of Gonadotropin-Releasing Hormone Enhances Luteal Function in Cattle -- Davis et al. ...
		Antifertility effects of LHRH agonists in the male rat and inhibition of testicular steroidogenesis in man. Int J Fertil 1980 25:157-170
		A cellular and endocrine characterization of the original and induced corpus luteum after administration of a gonadotropin-releasing hormone agonist or human chorionic gonadotropin on day five of the estrous cycle.
		Pituitary function, ovarian follicular growth, and plasma concentrations of 17ß-estradiol and progesterone in prepubertal heifers during and after treatment with the luteinizing hormone-releasing hormone agonist deslorelin.
	www.biolreprod.org /cgi/content/full/69/2/398 (4605 words)

	Copresentation of natural HIV-1 agonist and antagonist ligands fails to induce the T cell receptor signaling cascade -- ...
		APC pulsed with agonistic peptide (GGKKKYKL), partial agonist/antagonist (7R or 7Q), or a natural APL of unknown phenotype (7A) at 40 µM. Cell lysates were electrophoresed and immunoblotted with anti-phosphotyrosine mAb.
		APC pulsed with agonist peptide (SLYNTVATL), strict antagonist (3F, 5A), or partial agonist/antagonist (3C or 3S or 3F, 6I, 8V) at 40 µM. CTL presented with unpulsed APC were used as a control.
		To present peptide, APC were pulsed with 1 nM agonist peptide for 2 hr, washed with RPMI medium 1640, and then either pulsed for a further 2 hr with 1 nM APL (for copresentation) or resuspended in the absence of peptide for 2 hr (for agonist presentation alone).
	www.pnas.org /cgi/content/full/95/8/4527 (4833 words)

	FET without an GnRH Agonist
		In an attempt to increase the predictability of FET cycles, many programs have experimented with using a GnRH agonist (e.g., Lupron) in their protocol, as patients using a GnRH agonist are far less likely to experience a spontaneous LH surge.
		The cost and additional effort required by adding a GnRH agonist, as well as several studies questioning its necessity, however, have raise the question of whether it is possible to increase the predictability of a medicated FET cycle without using a GnRH agonist.
		Based on these results, the authors concluded that, among patients with functioning ovaries, an FET protocol that does not use a GnRH agonist may be appropriate and effective.
	www.inciid.org /article.php?cat=treatment&id=190 (563 words)

	Strong agonist ligands for the T cell receptor do not mediate positive selection of functional CD8+ T cells.
		Strong agonist ligands for the T cell receptor do not mediate positive selection of functional CD8+ T cells.
		In the present study, we have investigated whether low concentrations of the original agonist peptide, or variants that still have a strong agonist activity can also mediate positive selection.
		A strong agonist variant was capable of stimulating the differentiation of TCRhi CD8+ cells, giving the appearance of phenotypic positive selection.
	www.aegis.com /aidsline/1995/nov/M95B0809.html (422 words)

	British Journal of Pharmacology - Abstract of article: Effects of sodium on agonist efficacy for G-protein activation ... (Site not responding. Last check: 2007-11-06)
		S binding stimulated by partial but not full agonists was inhibited by NaCl with a potency that was inversely proportional to agonist efficacy.
		S binding stimulated by the absence of monovalent cations resembled that of agonist-stimulated binding and was blocked by pretreatment of mMOR-CHO cells with pertussis toxin.
		receptor activity and the relative efficacy of partial agonists acting at these receptors are both increased by increases in the stoichiometric ratio of receptors:G-proteins.
	www.nature.com /bjp/journal/v130/n5/abs/0703382a.html (273 words)

	The Agonist Activity of Tamoxifen Is Inhibited by the Short Heterodimer Partner Orphan Nuclear Receptor in Human ...
		The Agonist Activity of Tamoxifen Is Inhibited by the Short Heterodimer Partner Orphan Nuclear Receptor in Human Endometrial Cancer Cells -- Klinge et al.
		The Agonist Activity of Tamoxifen Is Inhibited by the Short Heterodimer Partner Orphan Nuclear Receptor in Human Endometrial Cancer Cells
		ICI 164,384 (14), indicating that TAM agonist activity is ER mediated.
	endo.endojournals.org /cgi/content/full/143/3/853 (8009 words)

	Agonist-Induced Increase in Apparent {beta} -adrenergic Receptor Size -- Limbird and Lefkowitz 75 (1): 228 -- ...
		The properties of digitonin-solubilized ß -adrenergic receptors from frog erythrocyte membranes were studied by gel exclusion chromatography on AcA 34 Ultragel.
		H]hydroxybenzylisoproterenol agonist prior to their solubilization from the membrane leads to an increase in apparent receptor size.
		However, the low concentrations of agonist that are capable of altering apparent receptor size and the sensitivity of this effect to guanyl nucleotides suggest that these phenomena may be intimately involved in eliciting the physiological effects of ß -adrenergic catecholamines at the molecular level.
	www.pnas.org /cgi/content/abstract/75/1/228 (375 words)

	Randomised placebo controlled trial of beta agonist dose reduction in asthma -- Harrison et al. 54 (2): 98 -- Thorax
		Randomised placebo controlled trial of beta agonist dose reduction in asthma -- Harrison et al.
		agonists, often at high doses, contrary to national and international guidelines.
		agonists were converted to an equivalent dose of terbutaline
	thorax.bmjjournals.com /cgi/content/abstract/54/2/98 (346 words)

	University of Miami School of Medicine - Glossary - LHRH agonist
		LHRH agonist: A compound that is similar to LHRH (luteinizing hormone-releasing hormone) in structure and is able to act like it.
		Thus, an LHRH agonist serves in a manner similar to LHRH to control the same sex hormones.
		An agonist achieves a normal action, often mimicking the action of a naturally occurring substance.
	www.med.miami.edu /glossary/art.asp?articlekey=4153 (109 words)

	Palatin Technologies' Small Molecule Melanocortin Agonist..
		Administration of the MC4 receptor-selective agonist on a daily basis resulted in a 12% reduction in body weight by 10 days.
		In addition to its effects in diet-induced obese animals, the MC4 receptor-selective agonist also was effective at reducing the body weight of genetically obese mice that are deficient in leptin, a protein involved in the regulation of food intake and energy expenditure.
		The Company is currently conducting clinical trials with its lead drug candidate, PT-141, an MC receptor agonist, for the treatment of male and female sexual dysfunction.
	www.amex.com /newsDetails/CmnNewsDet.jsp?id=XpressFeed_NewsDetails_1107174654985.html (637 words)

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