Physiological antagonists

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Topic: Physiological antagonists

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	Ranitidine Online Literature
		H2 antagonists in the treatment of reflux oesophagitis: can physiological studies predict the response?
		The effect of aspirin and anti-ulcer drugs on gastric mucosal prostaglandin E. Effects of three H2 antagonists on the isolated perfused rat liver.
		The antisecretory profile of action of the H2-receptor antagonists, famotidine, loxtidine, ranitidine and L-643,441 on the rat isolated gastric mucosa.
	twinpharm.com /ref-ranitidine-9/ranitidine-9-refs.html

	Inverse, protean, and ligand-selective agonism: matters of receptor conformation -- KENAKIN 15 (3): 598 -- The FASEB Journal
		Antagonist: produces no physiological response but rather blocks the response to endogenous or exogenous agonists.
		drug development were full and partial agonists and antagonists.
		However, the lack of depression of basal responses to some antagonists
	www.fasebj.org /cgi/content/full/15/3/598

	Receptor antagonist - Wikipedia, the free encyclopedia
		Antagonists that compete with an agonist for a receptor are competitive antagonists.
		In medicine and biology, a receptor antagonist is a substance that inhibits the normal physiological function of a receptor.
		Antagonists stop agonists from acting on certain receptors by blocking them.
	en.wikipedia.org /wiki/Receptor_antagonist (211 words)

	Receptor antagonist - Wikipedia, the free encyclopedia
		Antagonists that compete with an agonist for a receptor are competitive antagonists.
		In medicine and biology, a receptor antagonist is a substance that inhibits the normal physiological function of a receptor.
		Antagonists that antagonize by other means are non-competitive antagonists.
	en.wikipedia.org /wiki/Receptor_antagonist (215 words)

	British Journal of Pharmacology - Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery
		Inverse agonists may be beneficial here, since they would decrease the high basal activity induced by the mutation, while antagonists would have no effect.
		A prerequisite for considering the physiological relevance of inverse agonism, is its study in experimental conditions that are as close to physiological as possible.
		The physiological relevance of inverse agonism is not only becoming clearer, but is slowly taking a place and establishing a role in drug therapy.
	www.nature.com /bjp/journal/v130/n1/full/0703311a.html (215 words)

	Tolerance, physical dependence and addiction: definitions, clinical relevance and misconceptions
		Physical dependence is the physiological adaptation of the body to the presence of an opioid.
		It is incorrect to use the term 'physical dependence' (a physiological state) to describe addiction (a dysfunctional psychological and behavioral syndrome).
		Antagonists and agonist-antagonists in the patient who is physically dependent should be strictly avoided because their use will neutralize the analgesic effect and cause a withdrawal syndrome.
	www.whocancerpain.wisc.edu /eng/11_3/tpda.html (1203 words)

	1471-2202-3-18.rtf
		Since specific pharmacological antagonists of AGRP do not presently exist, we assessed if reduction of hypothalamic AGRP mRNA by RNA interference (RNAI) would influence metabolic function, an outcome suggesting that pharmacological antagonists might constitute useful reagents to treat obesity.
		The present study demonstrates that RNAI protocols can be used to assess physiological function of neuronal genes in vivo.
		Since both the AGRPi and the control GFPi mice were still recovering from the effects of the surgery and anesthesia at 48 hours, it is not surprising that the effects on body weight were not statistical at this time.
	www.indexingonline.com /BISTIC/NIH/1471-2202-3-18.rtf (1203 words)

	IPHY 3430 Human Physiology, University of Colorado at Boulder
		Agonists and antagonists to the alpha, beta1, and beta2 receptors in the sympathetic and muscarinic and nicotinic receptors in the parasympathetic system are often used in treatments.
		The ANS is further subdivided into the sympathetic and parasympathetic nervous systems, both of which are involved in integration of involuntary physiological processes, such as control of heart rate.
		What different pharmacological or physiological approaches (provide more than one possibility) might you employ to confirm your anatomical evidence?
	www.colorado.edu /epob/epob1220lynch/07pns2.html (906 words)

	IPHY 3430 Human Physiology, University of Colorado at Boulder
		Agonists and antagonists to the alpha1, alpha2, beta1, and beta2 receptors in the sympathetic and muscarinic and nicotinic receptors in the parasympathetic system are often used in treatments.
		The ANS is further subdivided into the sympathetic and parasympathetic nervous systems, both of which are involved in integration of involuntary physiological processes, such as control of heart rate.
		What different pharmacological or physiological approaches (provide more than one possibility) might you employ to confirm your anatomical evidence?
	www.colorado.edu /kines/Class/IPHY3430-200/07pns2.html (973 words)

	Molecular and Physiological Diversity of Nicotinic Acetylcholine Receptors in the Midbrain Dopaminergic Nuclei -- Klink et al. 21 (5): 1452 -- Journal of Neuroscience
		El-Bizri H, Clarke PB (1994) Blockade of nicotinic receptor-mediated release of dopamine from striatal synaptosomes by chlorisondamine and other nicotinic antagonists administered in vitro.
		Cauli B, Audinat E, Lambolez B, Angulo MC, Ropert N, Tsuzuki K, Hestrin S, Rossier J (1997) Molecular and physiological diversity of cortical nonpyramidal cells.
		Elliott KJ, Jones JM, Sacaan AI, Lloyd GK, Corey-Naeve J (1998) 6-hydroxydopamine lesion of rat nigrostriatal dopaminergic neurons differentially affects nicotinic acetylcholine receptor subunit mRNA expression.
	www.jneurosci.org /cgi/content/full/21/5/1452 (6195 words)

	Genetic Variations in Human G Protein-Coupled Receptors: Implications for Drug Therapy
		The presence of endogenous GPCR antagonists is a rare observation; yet, we have found that the opioid peptide dynorphin also serves as an endogenous antagonist, which may regulate melanocortin function under physiological conditions.
		GPCRs comprise a large class of membrane proteins that are encoded by approximately 600 human genes with broadly diverse functions.
		Whereas SMO is a member of the 7-TMD GPCR class, PTCH is an integral membrane protein with approximately 9 TMDs unrelated in sequence to the GPCRs.
	www.aapspharmsci.org /view.asp?art=ps030322 (6195 words)

	www.HandsForHealing.com - Sports Massage 2 - Maintenance/Clinical
		How to apply a variety of techniques appropriate to this phase of sports massage and understand the physiological effects of each technique.
		How to analyze various sports movements to determine the agonists and antagonists.
		How muscles interact to produce movement, including: reciprocal innervation/inhibition, synergists, types of muscular contractions, and classification according to the number of articulations they cross.
	www.handsforhealing.com /sports2.htm (6195 words)

	Estrogen Receptor Null Mice: What Have We Learned and Where Will They Lead Us? -- Couse and Korach 20 (3): 358 -- Endocrine Reviews
		of estrogen in some physiological systems, such as in male fertility.
		are then acutely treated with estrogen agonists or antagonists.
		in the genes encoding the receptors for androgen (37, 38), glucocorticoids
	edrv.endojournals.org /cgi/content/full/20/3/358 (9749 words)

	GIP
		Effects of the novel (Pro(3))GIP antagonist and exendin(9-39)amide on GIP- and GLP-1-induced cyclic AMP generation, insulin secretion and postprandial insulin release in obese diabetic (ob/ ob) mice: evidence that GIP is the major physiological incretin.
		Effect of GIP and GLP-1 antagonists on insulin release in the rat.
		GIP stimulation of pancreatic beta-cell survival is dependent upon phosphatidylinositol 3-kinase (PI3-K)/ protein kinase B (PKB) signaling, inactivation of the forkhead transcription factor Foxo1 and downregulation of bax expression.
	www.glucagon.com /gip.htm (1335 words)

	Mekk1
		The availability of this radioligand will be a valuable tool with which to investigate the physiological functions of OX1 recepto.
		Calcium mobilisation studies showed that SB-334867, SB-408124 and SB-410220 are all functional antagonists of the OX1 receptor, with potencies in line with their affinities, as measured in the radioligand binding assays, and with approximately 50-fold selectivity over the orexin-2 receptor.
		This study characterises the binding of a novel nonpeptide antagonist radioligand, [(3)H]SB-674042 (1-(5-(2-fluoro-phenyl)-2-methyl-thiazol-4-yl)-1-((S)-2-(5-phenyl-(1,3,4)oxadiazol-2-ylmethyl)-pyrrolidin-1-yl)- methanone), to the human orexin-1 (OX1) receptor stably expressed in Chinese hamster ovary (CHO) cells in both a whole cell assay and in a cell membrane-based scintillation proximity assay (SPA) format.
	www.gene2gene.com /Rb.htm (1335 words)

	Heterodimeric Opioid G-Protein Coupled Receptor
		Understanding possible differences in the affinity and efficacy of various agonists and antagonists for the various forms of these receptors and their differential ability to transmit signals will help explain the differences in the physiological responses induced and will be instrumental in identifying and developing novel therapeutic compounds and formulations.
		Their current research relates to the discovery that the opioid receptors are capable of forming functional heterodimers.
		Other types of opioid receptors have been postulated but are less well characterized and have not been cloned.
	www.med.nyu.edu /oil/tech/therapeutics/topioid.html (316 words)

	nerdshit.com: Psychointegration: The Physiological Effects of Entheogens
		Entheogens have these roles in the serotonergic system, substituting for neurotransmitters in some receptor locations, and, in others, functioning as antagonists (or blockers) that prevent the normal response.1 These actions2 upon neurotransmission mediate their profound effects upon human experience and consciousness.
		The cross-cultural social and therapeutic uses of entheogens are based in their neurophysiological effects upon the serotonergic neurotransmitter systems.
		Cross-cultural research indicates that their common effects include the induction of powerful emotional, cognitive and therapeutic reactions and interpretations, suggesting these are consequences of similar psychophysiological properties of the substances.
	www.nerdshit.com /archive/2004/11/05/psychointegrati (316 words)

	tab001hgs: Retinoid receptors and their ligands
		(1996) Identification and functional separation of retinoic acid receptor neutral antagonists and inverse agonists.
		No physiological ligand has been definitely defined, but candidates are: 9-cis retinoic acid, docosahexanoic acid and phytanic acid
		(2002) Co-regulator recruitment and the mechanism of retinoic acid receptor synergy.
	www-ermm.cbcu.cam.ac.uk /04008543h.htm (316 words)

	ROBERTO FRANCESCO ROMOLO BELLARMINE - LoveToKnow Article on ROBERTO FRANCESCO ROMOLO BELLARMINE
		Do not employ such physiological antagonists as pilocarpine or morphine, for the lethal actions of all these drugs exhibit not mutual antagonism but coincidence.
		Bellarmino), Italian cardinal and theologian, was born at Monte Pulciano, in Tuscany, on the 4th of October 1542.
		"ROBERTO FRANCESCO ROMOLO BELLARMINE." LoveToKnow 1911 Online Encyclopedia.
	www.1911encyclopedia.org /B/BE/BELLARMINE_ROBERTO_FRANCESCO_ROMOLO.htm (316 words)

	Motilin antagonists
		Soon after the discovery of motilin in 1971, functional antagonism of motilin-induced contractility was described (and forgotten), but the absence of specific antagonists has hampered the study of the physiological role of motilin until today.
		However as part of an attempt to delineate the bio-active part of motilin, so as to understand the relationship between the structure of motilin and erythromycin, a fragment of motilin was synthetized in which residue number 3 was substituted with phenylalanine.
		To avoid the problem, motilin was either neutralized with antibodies, or suppressed with somatostatin, but neither of these experiments was truly convincing.
	www.kuleuven.ac.be /gih/motchar.htm (316 words)

	Tetrazole binding to amidine bases
		The tetrazole pharmacophore has been used extensively during the past two decades in the development of angiotensin II receptor antagonists, a class of antihypertensive drugs.[1] Under physiological conditions, tetrazoles are deprotonated.
		Tetrazoles form non-covalent complexes with amidines, although there are certain pecularities.
		The downfield shift of the NH signal compared to the non-coordinating borate confirms that the tetrazolate is hydrogen-bonded to the amidine.
	www.mdpi.org /ecsoc/ecsoc-5/Papers/c0004/c0004.htm (316 words)

	International Union of Pharmacology. XXXVI. Current Status of the Nomenclature for Receptors for Corticotropin-Releasing Factor and Their Ligands -- Hauger et al. 55 (1): 21 -- Pharmacological Reviews
		Dunn AJ and Berridge CW (1990) Physiological and behavioral responses of corticotropin releasing factor administration: is CRF a mediator of anxiety or stress responses?
		Corticotropin releasing factor receptor antagonists: potential future therapy in gastroenterology?
		Perrin MH, Donaldson CJ, Chen R, Lewis KA and Vale WW (1993) Cloning and functional expression of a rat brain corticotropin releasing factor (CRF) receptor.
	pharmrev.aspetjournals.org /cgi/content/full/55/1/21 (316 words)

	Surround inhibition of mammalian AII amacrine cells is generated in the proximal retina -- Bloomfield and Xin 523 (3): 771 -- The Journal of Physiology Online
		Neurotransmitter agonists and antagonists were applied exogenously via the superfusate to dissect the synaptic pathways pharmacologically and thereby determine those pathways responsible for the generation of the on-centre/off-surround receptive fields of AII amacrine cells.
		Following physiological characterization of a cell, Neurobiotin was iontophoresed into the neuron using a combination of sinusoidal (3 Hz, 0·8 nA peak to peak) and direct (0·4 nA) currents applied simultaneously; this method allowed passage of tracer through the electrode without polarization.
		Light-evoked responses of AII amacrine cells in the dark-adapted retina
	jp.physoc.org /cgi/content/full/523/3/771 (316 words)

	German Journal of Psychiatry Moreyra Pathological Gambling
		Patients with spectrum-related disorders show an intense desire to perform a specific behavior preceded by unpleasant feelings and physiological activation, all of which are relieved when the behavior is performed (Hantouche and Merckaert, 1991; Hollander, Skodol and Oldham, 1996; Cartwright et al., 1998).
		In this context, the term obsessive-compulsive spectrum disorder is used to describe a group of disorders with pathophysiological similarities that also share genetic and biological mechanisms.
		Opioid antagonists in the treatment of impulse-control disorders.
	www.gjpsy.uni-goettingen.de /gjp-article-moreyra.htm (5313 words)

	Circuitry Underlying Antiopioid Actions of Cholecystokinin Within the Rostral Ventromedial Medulla -- Heinricher et al. 85 (1): 280 -- Journal of Neurophysiology
		Characterization of the effect of cholecystokinin (CCK) on neurons in the periaqueductal gray of the rat: immunocytochemical and in vivo and in vitro electrophysiological studies.
		Effects of spinal cholecystokinin receptor antagonists on morphine antinociception in a model of visceral pain in the rat.
		the role of cholecystokinin (CCK) as a physiological opioid antagonist
	jn.physiology.org /cgi/content/full/85/1/280 (4812 words)

	cardiac home
		The opiate nature of HIT is well established and induces profound physiological depression mimicking natural hibernation: an anesthetized state, profound hypothermia, bradycardia, decreased renal function and feeding inhibition, which can be reversed or retarded by the opiate antagonists naloxone and naltrexone.
		Recent studies have revealed that opiate-like hibernation triggering or induction factors may play a role in maintaining cellular energy status and membrane integrity during hibernation, which could provide for "natural" cellular protection and metabolic inhibition for cardiac surgery or during other times when organ and cellular damage may occur.
		Evidence indicates that the HIT molecule may initiate its potent metabolic inhibitory effects through specific membrane opioid receptors, and HIT may alter membrane geometry and potentially may be a membrane stabilizing agent.
	www.cardiac.um-surgery.org /research/10a_research.htm (4812 words)

	Heavy Metals
		Heavy metal antagonists (HMA) - chelating agents are designed specifically to compete with these groups for the metals, and thereby prevent or reverse toxic effects and enhance excretion of metals.
		Heavy metals (HM) exert their toxic effects by combining with one or more reactive groups (ligands) essential for normal physiological functions.
		By definition, Chelation is the formation of a metal ion complex in which the metal ion is associated with a charged or uncharged electron donor, referred to as a ligand.
	www.med.howard.edu /pharmacology/handouts/heavymetals2.htm (734 words)

	Roles of 5-HT receptors in the release and action of secretin on pancreatic secretion in rats -- Li et al. 280 (4): 595 -- AJP - Gastrointestinal and Liver Physiology
		The combination of the two antagonists produced a greater inhibition than their individual effect also at the physiological doses of Sec only.
		of ketanserin or ondansetron at 10 µg/kg (Fig.
		Ketanserin inhibited duodenal acidification-evoked pancreatic secretion and elevation of plasma Sec concentration.
	ajpgi.physiology.org /cgi/content/full/280/4/G595 (734 words)

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