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*  G protein-coupled receptor
"The Top Prescription Drugs of 2012 Globally: Biologics Dominate, But Small Molecule CNS Drugs Hold on to Top Spots" (PDF). ACS ... Three types of ligands exist: Agonists are ligands that shift the equilibrium in favour of active states; inverse agonists are ... or conformation-specific agonism). However, the binding of any single particular agonist may also initiate activation of ... Overington JP, Al-Lazikani B, Hopkins AL (December 2006). "How many drug targets are there?". Nature Reviews. Drug Discovery. 5 ...
*  Cannabinoid receptor antagonist
... or inverse agonism - as potential obesity treatment and other therapeutic use", Journal of Clinical Pharmacy and Therapeutics, ... The lack of efficient and well-tolerated drugs to cure obesity has led to an increased interest in research and development of ... A general CB1 inverse agonist pharmacophore model can be extracted from the common features of these analogs, diarylpyrazoles ( ... CB1 antagonists produce inverse cannabimimetic effects that are opposite in direction from those produced by agonists for these ...
*  GPR35
Both ML145 and ML144 unfurl their antagonistic activity through inverse agonism. They are, however, highly species-selective, ... This phenomenon is well established for other GPCRs and complicates the development of pharmaceutical drugs. Antagonists of ... "G-Protein-Coupled Receptor 35 Is a Target of the Asthma Drugs Cromolyn Disodium and Nedocromil Sodium". Pharmacology. S. Karger ...
*  Michel Bouvier
Bouvier's work in the regulation of receptors led to new paradigms (inverse agonism; pharmacological chaperones; receptor ... Their physiological significance makes them a prime target in drug development, and over a third of existing drugs use GPCRs as ... He is a world-known expert in cell signaling and drug discovery, notably in the field of G protein-coupled receptors (GPCRs). ... His work focuses on the study of cell signaling towards the discovery of new pharmaceutical drugs. Michel Bouvier earned a B.Sc ...
*  Mirtazapine
Antagonism of the 5-HT2 subfamily of receptors and inverse agonism of the 5-HT2C receptor appears to be in part responsible for ... The drug acts as an antagonist of certain adrenergic and serotonin receptors, and is also a strong antihistamine. It is ... Mirtazapine is the English and French generic name of the drug and its INN, USAN, USP, BAN, DCF, and JAN. Its generic name in ... Blockade of the 5-HT3 receptors has also shown to improve anxiety and to be effective in the treatment of drug addiction in ...
*  Drug interaction
On the other hand, in the case of antagonism the substances involved are known as inverse agonists. The different responses of ... For example, when the synergy occurs at a cellular receptor level this is termed agonism, and the substances involved are ... drug-drug interaction). However, interactions may also exist between drugs and foods (drug-food interactions), as well as drugs ... The drug digoxin is an example of this type of drug. Steep dose-response curve: Small changes in the dosage of a drug produce ...
*  List of cocaine analogues
Ger.) V.1-1951-Volume(issue)/page/year: 18,517,1968 Dopamine reuptake transporter (DAT) ``inverse agonism´´ - A novel ... The term may also be loosely used to refer to drugs manufactured from cocaine or having their basis as a total synthesis of ... Similar to several other kinds of aromatics in structure and being an inverse agonist at the 5-HT2C receptor as well as an ... "Drugbank website "drug card", "(DB00907)" for Cocaine: Giving ten targets of the molecule in vivo, including dopamine/serotonin ...
*  Pharmacodynamics
There are 7 main drug actions: stimulating action through direct receptor agonism and downstream effects depressing action ... inverse agonist). In principle, a pharmacologist would aim for a target plasma concentration of the drug for a desired level of ... Colchicine, a drug for gout, interferes with the function of the structural protein tubulin, while Digitalis, a drug still used ... The duration of action of a drug is the length of time that particular drug is effective. Duration of action is a function of ...
*  Ethylphenidate
... "inverse agonism"--a novel hypothesis to explain the enigmatic pharmacology of cocaine". Neuropharmacology. 87: 19-14. doi: ... Ethylphenidate is illegal in Poland by "the Act on Counteracting Drug Addiction" since 1 July 2015 It is illegal in Lithuania ... Australian state and federal legislation contains provisions that mean that analogues of controlled drugs are also covered by ... Ethylphenidate is illegal in Jersey under the Misuse of Drugs (Jersey) Law 1978. ...
*  Nuclear receptor
... receptor ligands may display dramatically diverse effects ranging in a spectrum from agonism to antagonism to inverse agonism. ... Overington JP, Al-Lazikani B, Hopkins AL (2006). "How many drug targets are there?". Nature Reviews. Drug Discovery. 5 (12): ... Food and Drug Administration (FDA) approved drugs target nuclear receptors. A number of nuclear receptors, referred to as ... A number of drugs that work through nuclear receptors display an agonist response in some tissues and an antagonistic response ...
*  Receptor (biochemistry)
The anti-obesity drugs rimonabant and taranabant are inverse agonists at the cannabinoid CB1 receptor and though they produced ... Note that the idea of receptor agonism and antagonism only refers to the interaction between receptors and ligands and not to ... Affinity: The ability of a drug to combine with a receptor to create a drug-receptor complex. Efficacy: The ability of a drug- ... Antagonist: A drug with a fast association & slow dissociation As a drug approaches a receptor, the receptor alters the ...
*  LY-320,135
Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sciences. 2005 Feb 4;76(12):1307-24. PMID 15670612. ... LY-320,135 is a drug used in scientific research which acts as a selective antagonist of the cannabinoid receptor CB1. It was ... particularly for elucidating the mechanisms by which many CB1 antagonists act as inverse agonists at higher doses. Felder CC, ...
*  H1 antagonist
... inverse agonism, anti-inflammatory actions and cardiac effects". Clinical & Experimental Allergy. 32 (4): 489-98. doi:10.1046/j ... CS1 maint: Uses editors parameter (link) "Drug Interaction Report". drugs.com. Retrieved 28 January 2017. Camelo-Nunes, Inês ... giving the drug a very high potency. Second-generation H1-antihistamines are newer drugs that are much more selective for ... derivatives of second-generation drugs are intended to have increased efficacy with fewer adverse drug reactions. Fexofenadine ...
*  Receptor antagonist
Many drugs previously classified as antagonists are now beginning to be reclassified as inverse agonists because of the ... Greasley PJ, Clapham JC (December 2006). "Inverse agonism or neutral antagonism at G-protein coupled receptors: a medicinal ... Kenakin T (January 2004). "Efficacy as a vector: the relative prevalence and paucity of inverse agonism". Molecular ... Leurs R, Church MK, Taglialatela M (April 2002). "H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac ...
*  Antihistamine
Leurs R, Church MK, Taglialatela M (April 2002). "H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac ... "Drug Interaction Report". drugs.com. Retrieved 28 January 2017. Yoneyama H, et al. (March 2008). "Efficient approaches to S- ... Research into these drugs led to the discovery that they were H1 antagonists and also to the development of H2 antagonists, ... The newer drugs are not necessarily safer or more effective. Because so many antihistamines are available, patients can have ...
*  Azapirone
Herrick-Davis K, Grinde E, Teitler M (October 2000). "Inverse agonist activity of atypical antipsychotic drugs at human 5- ... all of them except 5-HT1A agonism are generally undesirable in anxiolytics and only contribute to side effects. As a result, ... Stahl, SM; Lee-Zimmerman, C (May 1, 2013). "Serotonergic drugs for depression and beyond". Curr Drug Targets. 14 (5): 578-85. ... Drugs classed as azapirones can be identified by their -spirone or -pirone suffix. On a pharmacological level, azapirones ...
*  Diphenhydramine
Khilnani and Khilnani (October 2011). "Inverse agonism and its therapeutic significance". Indian J Pharmacol. 43 (5): 492-501. ... Because the drug is cheap and sold over-the-counter in most countries, adolescents without access to stronger, illicit drugs ... Food and Drug Administration, HHS (2002). "Labeling of Diphenhydramine-Containing Drug Products for Over-the-Counter Human Use ... ISBN 0-9626523-7-7. "List of prohibited and controlled drugs according to chapter 96 of the laws of Zambia" (DOC). The Drug ...
*  Agonist
Kenakin T (March 2001). "Inverse, protean, and ligand-selective agonism: matters of receptor conformation". FASEB J. 15 (3): ... However, a drug can act as a full agonist in some tissues and as a partial agonist in other tissues, depending upon the ... An inverse agonist is an agent that binds to the same receptor binding-site as an agonist for that receptor and inhibits the ... When a drug is used therapeutically, it is important to understand the margin of safety that exists between the dose needed for ...
*  JD5037
... is an antiobesity drug candidate which acts as a peripherally-restricted cannabinoid inverse agonist at CB1 receptors. ... "Peripheral Cannabinoid-1 Receptor Inverse Agonism Reduces Obesity by Reversing Leptin Resistance". Cell Metabolism. 16 (2): 167 ... In obese mice given the drug, the resulting resensitization to leptin levels produced decreased food intake, weight loss, and ...
*  Biological target
... or be the opposite of the endogenous substance which in the case of receptors is referred to as inverse agonism. The term " ... The most common drug targets of currently marketed drugs include: proteins G protein-coupled receptors (target of 50% of drugs ... Drug Discovery. 5 (12): 993-6. doi:10.1038/nrd2199. PMID 17139284. Landry Y, Gies JP (February 2008). "Drugs and their ... Lundstrom K (2009). "An overview on GPCRs and drug discovery: structure-based drug design and structural biology on GPCRs". ...
*  Atypical antipsychotic
Note: Unless otherwise specified, the drugs below serve as antagonists/inverse agonists at the receptors listed. Legend: ... To have partial agonism at the 5-HT1A receptor can yield absence of weight gain in an antipsychotic. This is very relevant for ... These drugs have relatively long half-lives. Each drug has a different half-life, but the occupancy of the D2 receptor falls ... It has been suggested that there is no validity to the term "second-generation antipsychotic drugs" and that the drugs that ...
*  Cannabidiol
In 2016, the Drug Enforcement Administration added "marihuana extracts" to the list of Schedule I drugs, which it defined as " ... Recently, cannabidiol has been identified as a novel inverse agonist of the GPR12. Cannabidiol is insoluble in water but ... Cannabidiol's pharmacological effects have additionally been attributed to PPARγ agonism and intracellular calcium release. ... Cannabidiol is currently a class B1 controlled drug in New Zealand under the Misuse of Drugs Act. It is also a prescription ...
*  VCHSR
... is crucial for its inverse agonism at the cannabinoid CB1 receptor". Molecular Pharmacology. 62 (6): 1274-87. doi:10.1124/mol. ... VCHSR is a drug used in scientific research which acts as a selective antagonist of the cannabinoid receptor CB1. It is derived ... 2006). "Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28( ... which removes the inverse agonist effect that rimonabant produces at high doses, so that VCHSR instead acts as a neutral ...
*  Opioid antagonist
... and so is the preferred antidote drug for treating opioid overdose. Naltrexone is also a partial inverse agonist, and this ... by virtue of the fact that both MOR and KOR agonism independently confer pain relief). However, these opioid analgesics have ... These drugs are used mainly as antidotes to reverse opioid overdose and in the treatment of alcohol dependence and opioid ... On the other hand, Naloxone has no partial agonist effects, and is in fact a partial inverse agonist at μ-opioid receptors, ...
*  Receptor theory
Mechanisms of drug action and the relationship between drug concentration and effect. In Goodman & Gilman's The Pharmacological ... In this model, agonists and inverse agonists are thought to have selective binding affinity for the pre-existing resting and ... 1983) Operational Models of Pharmacological Agonism. In: Proc. R. Soc. London Ser. B 220, pp. 141-162. Leff P (1995). "The two- ... Drug Discovery. 1 (8): 637-41. doi:10.1038/nrd875. PMID 12402503. Colquhoun D (2006). "The quantitative analysis of drug- ...
*  Functional selectivity
Drug Discovery. doi:10.1038/nrd.2017.229. ISSN 1474-1784. PMID 29302067. Urban JD, Clarke WP, von Zastrow M, Nichols DE, ... Costa-Neto CM, Parreiras-E-Silva LT, Bouvier M (2016). "A Pluridimensional View of Biased Agonism". Mol. Pharmacol. 90 (5): 587 ... antagonist or more recently an inverse agonist through a specific receptor subtype, and that this characteristic will be ... Drug Discovery. doi:10.1038/nrd.2017.229. ISSN 1474-1784. PMID 29302067. Simmons MA (June 2005). "Functional selectivity, ...
*  List of adverse effects of olanzapine
... or more specifically inverse agonism). Somnolence (dose-dependent). Tends to produce a moderate amount of sedation, less than ... 2010) Lexi-Comp Drug Information Handbook 19th North American Ed. Hudson, OH: Lexi-Comp Inc. ISBN 978-1-59195-278-7. Brunton, L ... Sep 2013). "Comparative efficacy and tolerability of 15 antipsychotic drugs in schizophrenia: a multiple-treatments meta- ... Neuroleptic malignant syndrome a potentially fatal complication of antipsychotic drug treatment. Presents with hyperthermia, ...