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Topic: Receptor antagonist

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Competitive antagonist

Antipyretic

Morphine

Antagonist

Opioid

Serotonin receptor

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	Receptor Workbook
		An antagonist that binds to the receptor in a reversible mass-action manner is referred to as a competitive antagonist.
		The dose-response curve obtained in the presence of a competitive antagonist is parallel to the dose-response curve obtained in the absence of antagonist.
		In the resting state the receptor is not occupied by an agonist and the G-protein exists as trimer of the alpha, beta and gamma subunits with GDP bound to the alpha subunit.
	www.mc.uky.edu /Pharmacology/instruction/pha824mp/PHA824mp.html (4044 words)

	CNSforum \| Anxiety - Serotonergic receptor systems
		The 5-HT3 receptor is structurally similar to the nicotinic acetylcholine receptor and is composed of 5 subunits.
		The 5-HT1A receptor is coupled to inhibitory G-proteins, which dissociate from the receptor on agonist binding, and inhibit secondary messenger signaling mechanisms.
		The 5-HT2 receptor is coupled to stimulatory G-proteins, which dissociate from the receptor on agonist binding, and initiate secondary messenger signaling mechanisms.
	www.cnsforum.com /imagebank/section/receptor_systems_Serotonergic/default.aspx (1189 words)

	Antagonist \| Encyclopedia of Drugs and Addictive Behavior
		As the concentration of antagonist is increased, the binding of the agonist is progressively inhibited, resulting in a decrease in the physiological response.
		A competitive antagonist, therefore, shifts the dose-response relationship for the agonist to the right, so that an increased concentration of the agonist in the presence of a competitive antagonist is required to produce the same biological response observed in the absence of the antagonist.
		In this case, the binding of the antagonist to the receptor (its affinity) may be so strong that the receptor is unavailable for binding by the agonist.
	www.bookrags.com /research/antagonist-edaa-01 (343 words)

	The Ibogaine Dossier
		Although NMDA receptor antagonists of the phencyclidine (PCP) type are precluded from clinical use because of their psychotomimetic properties, amantadine and memantine have been administered to human patients with idiopathic Parkinson's disease and spasticity for many years without serious adverse effects.
		Thus, neuroprotection targeting glutamate receptors does apparently not have to be associated with prominent psychotogenicity, and the development and evaluation of new neuroprotective drugs will have to performed in consideration both of the relative safety and of the good clinical effect of the already known and established aminoadamantanes.
		Data from binding studies is consistent with differences between three NMDA receptors in the striatum, thalamus and cerebellum with respect to their preferences for agonist or antagonist binding and the modulation of binding by dizocilpine, cations and polyamines.
	www.ibogaine.desk.nl /lit-nmda.html (7184 words)

	Blood Pressure at AllBestRx.com
		Altace Hct - Altace Hct Is An Angiotensin Ii Receptor Antagonist And Thiazide Diuretic Combination Used...
		Atacand - Atacand Is An Angiotensin Ii Receptor Antagonist Used To Treat High Blood Pressure.
		Cozaar - Cozaar Is An Angiotensin Ii Receptor Antagonist Used To Treat High Blood Pressure.
	www.allbestrx.com /pharmacy/Blood_Pressure.htm (616 words)

	Antagonist Summary
		The antagonist is the character (or group of characters, or, sometimes an institution) of a story who represents the opposition against which the heroes and/or protagonists must contend.
		Instead, the antagonist becomes that character, group, or sometimes force which provides the chief obstruction to the protagonist or "main character" of the story.
		Note that the antagonist is not necessarily human; often, the forces of nature or psychological elements provide this element of opposition.
	www.bookrags.com /Antagonist (658 words)

	The Systemically Administered Competitive AMPA Receptor Antagonist, YM872, has Analgesic Effects on Thermal or ...
		Hunter JC, Singh L. Role of excitatory amino acid receptors in the mediation of the nociceptive response to formalin in the rat.
		Kainate GluR5 receptor subtype mediates the nociceptive response to formalin.
		The role of NMDA and non-NMDA excitatory amino acid receptors in the excitation of primate spinothalamic tract neurons by mechanical, chemical, thermal and electrical stimuli.
	www.anesthesia-analgesia.org /cgi/content/full/89/6/1534 (2012 words)

	Serotonin Receptor Subtypes and Ligands
		5-HT is an indolealkylamine that binds to all populations of 5-HT receptors.
		The 5-HT gene is on mouse chromosome 5, whereas the 5-HT gene is on chromosome 1.
		Since any mutation could change receptor structure in a subtle way, the observation that mutation of a specific receptor amino acid leads to a decrease in ligand affinity is not sufficient to indicate that the mutated residue resides in the ligand binding site.
	www.acnp.org /g4/GN401000039/Ch039.html (13714 words)

	Pharmacology of SB-273779, a Nonpeptide Calcitonin Gene-Related Peptide 1 Receptor Antagonist -- Aiyar et al. 296 (3): ...
		Pharmacology of SB-273779, a Nonpeptide Calcitonin Gene-Related Peptide 1 Receptor Antagonist
		Wisskirchen FM, Burt RP and Marshall I (1998) Pharmacological characterization of CGRP receptors mediating relaxation of the rat pulmonary artery and inhibition of twitch responses of the rat vas deferens.
		Wisskirchen FM, Gray DW and Marshall I (1999) Receptors mediating CGRP-induced relaxation in the rat isolated thoracic aorta and porcine isolated coronary artery differentiated by h(alpha) CGRP(8-37).
	jpet.aspetjournals.org /cgi/content/full/296/3/768 (4606 words)

	Addiction Science Network: Agonists and Antagonists
		An agonist is a ligand that binds to a receptor and produces a biological effect (direct acting) or a compound that indirectly produces the same effect of a neurotransmitter (indirect acting).
		An antagonist is a ligand that binds to a receptor but does not produce a biological effect (direct acting) or a compound that indirectly inhibits the effect of a neurotransmitter (indirect acting).
		(It has the physiological/behavioral effect of an antagonist at most doses, but it's still technically an agonist!) Carlson confuses his classification of clonidine by classifying it as an agonist on one table and as an antagonist on another -- it is an agonist with antagonistic actions.
	wings.buffalo.edu /aru/Agonists&Antagonists.html (883 words)

	Efficacy of Administering an Endothelin-receptor Antagonist (SB209670) in Ameliorating Ischemia-Reperfusion Injury in ...
		Endothelin-1 contributes to ischemia/reperfusion injury in isolated rat heart-attenuation of ischemic injury by the endothelin-1 antagonists BQ-123 and BQ610.
		Effects of the endothelin receptor antagonist, SB 209670, on circulatory failure and organ injury in endotoxic shock in the anaesthetized rat.
		Blockade of radiocontrast induced nephrotoxicity by the endothelin receptor antagonist, SB Nephron 72: 629-636
	ajrccm.atsjournals.org /cgi/content/full/157/6/1975 (3461 words)

	The Individualist: Receptor antagonist
		In medicine and biology, a receptor antagonist is a substance that inhibits the normal physiological function of a receptor.
		Antagonists that compete with an agonist for a receptor are competitive antagonists.
		An example of this is the chemical Dimercaprol (antagonist) being used to treat arsenic (agonist) poisoning.
	www.dadamo.com /wiki/wiki.pl/Receptor_antagonist (311 words)

	Allosteric Modulators: The New Generation of Receptor Antagonist -- Kenakin 4 (4): 222 -- Molecular Interventions
		of as a distinct receptor subtype relative to the native (unmodulated)
		receptors are indicated in the absence and presence of saturating concentrations of the allosteric modulator eburnamonine.
		873140 is a synthetic small-molecule (0.6 kDa) non-competitive allosteric antagonist.
	molinterv.aspetjournals.org /cgi/content/full/4/4/222 (3463 words)

	H2-Receptor Antagonist's Effectiveness
		This study was undertaken in order to evaluate the effectiveness of continuous long-term H2 receptor blockade in healing esophageal mucosal disruption in patients with reflux esophagitis.
		In addition to bland diet, elevation of head of bed, and use of antacid as necessary, treatment was begun with the usual dose of H2 receptor antagonists (ranitidine 150mg p.o.
		On subsequent follow up, four patients on the usual dose of H2 receptor antagonists for heartburn developed erosive esophagitis, 2 patients developed Schatzki's Ring and one developed adenocarcinoma of the esophagus.
	www.webgerd.com /Abstract22.htm (396 words)

	Predix Pharmaceuticals Initiates Phase I Clinical Trial of 5-HT2B Receptor Antagonist for Pulmonary Hypertension - ...
		As a selective 5-HT2B antagonist, PRX-008066 has the potential to act both as a vasodilator of pulmonary but not systemic blood vessels, and as a disease-modifying agent to slow the progression of the disease.
		The primary objectives of the Phase I study are to evaluate the safety and tolerability of the compound and to obtain pharmacokinetic data in humans.
		5-HT2B receptor antagonists have the potential to be selective for diseased pulmonary vasculature (i.e., vessels affected by hypoxic conditions) compared to normal pulmonary and systemic vessels.
	www.redorbit.com /news/display?id=147801&source=r_health (530 words)

	Publication in Nature Medicine Highlights Potential of Actelion's Orexin Receptor Antagonist as a Novel Mechanism to ... (Site not responding. Last check: )
		ACT-078573 is the first oral orexin receptor antagonist that penetrates the blood-brain barrier and is capable of inducing a transient and reversible blockade of the two receptors, OX1 and OX2.
		Actelion is currently evaluating safety and efficacy of the OX1/OX2 receptor antagonist ACT-078573 in a Phase II program to assess the role of this compound in the treatment of sleep disorders.
		Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.
	press.arrivenet.com /business/article.php/910489.html (1094 words)

	An oral ETA-selective endothelin receptor antagonist for contrast nephropathy? -- Haylor and Morcos 16 (7): 1336 -- ...
		Brooks DP, DePalma PD. Blockade of radiocontrast-induced nephrotoxicity by the endothelin antagonist, SB 209670.
		VII: Binding characteristics of [3H] SB 209670, a novel nonpeptide antagonist of endothelin receptors.
		Bosentan, an orally active endothelin antagonist: effect on the renal response to contrast media.
	ndt.oxfordjournals.org /cgi/content/full/16/7/1336 (1255 words)

	SUPPRESSING EFFECT OF THE CANNABINOID CB1 RECEPTOR ANTAGONIST, SR147778, ON ALCOHOL INTAKE AND MOTIVATIONAL PROPERTIES ...
		Colombo, G., Vacca, G., Serra, S., Carai, M. and Gessa, G. (2004) Suppressing effect of the cannabinoid CB receptor antagonist, SR141716, on alcohol's motivational properties in alcohol-preferring rats.
		Hungund, B. akall, I., Adam, A., Basavarajappa, B. and Vadasz, C. (2003) Cannabinoid CB1 receptor knockout exhibit markedly reduced voluntary alcohol consumption and lack alcohol-induced dopamine release in the nucleus accumbens.
		Wang, L., Liu, J., Harvey-White, J., Zimmer, A. and Kunos, G. (2003) Endocannabinoid signaling via cannabinoid receptor 1 is involved in ethanol preference and its age-dependent decline in mice.
	alcalc.oxfordjournals.org /cgi/content/full/40/1/46 (5014 words)

	A Potent and Selective Histamine H4 Receptor Antagonist with Anti-Inflammatory Properties -- Thurmond et al. 309 (1): ...
		A, effects of histamine receptor antagonists on the histamine-mediated calcium increase.
		Histamine (fl bars) and the various histamine receptor antagonists (all 10 µM) were added to the cells 10 min prior to the calcium measurements.
		B, effects of histamine receptor antagonists on histamine-induced mast cell chemotaxis.
	jpet.aspetjournals.org /cgi/content/full/309/1/404 (5466 words)

	Definition of endothelin-1 protein receptor antagonist - NCI Dictionary of Cancer Terms
		Definition of endothelin-1 protein receptor antagonist - NCI Dictionary of Cancer Terms
		A substance that blocks the binding of the endothelin-1 protein to its receptor.
		endoscopy, endosonography, endostatin, endothelial cell, endothelin receptor antagonist
	www.nci.nih.gov /Templates/db_alpha.aspx?CdrID=256551 (68 words)

	IUPHAR RECEPTOR DATABASE \| HISTAMINE RECEPTORS \| H2
		receptor antagonist and impromidine is also an H
		A number of neuroleptic and antidepressant drugs (e.g.
		chlorpromazine, amitriptyline) appear to be very potent antagonists of H
	www.iuphar-db.org /GPCR/ReceptorDisplayForward?receptorID=2305 (163 words)

	Drug Development Technology - Vesicare - Oral Selective Muscarinic Receptor Antagonist for Overactive Bladder (OAB)
		Vesicare (solifenacin succinate) is an oral selective muscarinic receptor antagonist developed by Yamanouchi, Japan's third largest pharmaceutical company.
		It is indicated for the treatment of urinary frequency, urgency and incontinence associated with OAB.
		Yamanouchi's investigational muscarinic antagonist solifenacin succinate is thought to act primarily on muscarinic receptors in the smooth muscle of the bladder.
	www.drugdevelopment-technology.com /projects/solifenacin (755 words)

	BAY36-7620: A Potent Non-Competitive mGlu1 Receptor Antagonist with Inverse Agonist Activity. -- Carroll et al. 59 (5): ...
		BAY36-7620: A Potent Non-Competitive mGlu1 Receptor Antagonist with Inverse Agonist Activity.
		antagonists have been described, few are selective for a single
		The C Terminus of the Metabotropic Glutamate Receptor Subtypes 2 and 7 Specifies the Receptor Signaling Pathways
	molpharm.aspetjournals.org /cgi/content/abstract/59/5/965 (858 words)

	Definition of endothelin receptor antagonist - NCI Dictionary of Cancer Terms
		Definition of endothelin receptor antagonist - NCI Dictionary of Cancer Terms
		It may also prevent the growth and spread of other types of cancer, including colorectal cancer.
		endothelin-1 protein receptor antagonist, endpoint, enema, energy balance, English lavender
	www.nci.nih.gov /Templates/db_alpha.aspx?CdrID=44821 (62 words)

	Interleukin 1 receptor antagonist, Homo sapiens - UniGene Hs.81134
		Interleukin 1 receptor antagonist, Homo sapiens - UniGene Hs.81134
		Homo sapiens interleukin 1 receptor antagonist (IL1RN), transcript variant 4, mRNA
		H.sapiens mRNA for intracellular IL-1 receptor antagonist type II EST sequences (10 of 228) [Show all sequences]
	www.ncbi.nlm.nih.gov /UniGene/clust.cgi?ORG=Hs&CID=81134 (331 words)

	Eplerenone: A Selective Aldosterone Receptor Antagonist for Patients with Heart Failure -- Barnes and Howard 39 (1): 68 ...
		Eplerenone: A Selective Aldosterone Receptor Antagonist for Patients with Heart Failure -- Barnes and Howard 39 (1): 68 -- The Annals of Pharmacotherapy
		receptor antagonist, heart failure, myocardial infarction, left-ventricular dysfunction,
		aldosterone receptor antagonist spironolactone is lack of binding
	www.theannals.com /cgi/content/abstract/39/1/68 (396 words)

	NEJM -- Montelukast, a Leukotriene-Receptor Antagonist, for the Treatment of Mild Asthma and Exercise-Induced ...
		Currie, G. P., Lipworth, B. Bronchoprotective Effects of Leukotriene Receptor Antagonists in Asthma* : A Meta-analysis.
		FIGUEROA, D. Expression of the Cysteinyl Leukotriene 1 Receptor in Normal Human Lung and Peripheral Blood Leukocytes.
		BISGAARD, H., NIELSEN, K. Bronchoprotection with a Leukotriene Receptor Antagonist in Asthmatic Preschool Children.
	content.nejm.org /cgi/content/abstract/339/3/147 (1905 words)

	H2 Receptor antagonists poisoning Medical Information
		H2 receptor antagonist poisoning is an overdose of a medication typically used for reducing stomach acid.
		Note: This list may not be all inclusive.
		H2 receptor antagonist medications are available over-the-counter and by prescription.
	www.drugs.com /enc/h2_receptor_antagonists.html (297 words)

	IL1RN - interleukin 1 receptor antagonist
		IRAP; IL1F3; IL1RA; ICIL-1RA; MGC10430; intracellular IL-1 receptor antagonist type II Gene Product
		Four alternatively spliced transcript variants encoding distinct isoforms have been reported.
		Shu KH, Lee SH, Cheng CH, Wu MJ, Lian JD Impact of interleukin-1 receptor antagonist and tumor necrosisfactor-alpha gene polymorphism on IgA nephropathy.
	www.ucsf.edu /urogene/kgdb/gene/95.html (146 words)

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