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*  National Organization of Disorders of the Corpus Callosum National Organization of Disorders of the Corpus Callosum » National...
It would appear that beta-adrenergic agonism (adrenalin/noradrenalin like stimulation) may "warm up" the inclination to speak. ... This drug is also anxiolytic and has anti-panic activity, so it may also be that treatments aimed at social phobia / panic may ... I am a speech-language pathologist working with a first-grader with partial agenesis of the corpus callosum. He speaks in ... as in complete or partial agenesis, the brain has organized itself without those connections and there isn't anything to ...
  https://nodcc.org/resources/ask-a-professional/
*  First-in-class new drug for cachexia - Numedicus
... increase tissue anabolism via partial beta-1 adrenergic agonism, and antagonise fatigue via 5-HT1A receptors. No other existing ... First-in-class new drug for cachexia. Numedicus is please to note the report from PsiOxus, on the outcome of a Phase II trial ... In a trial of 87 patients over 16 weeks, involving 2 dose levels plus placebo, patients on the higher dose of active drug ... Pharmacologically, MT-102 does three things: oppose excess catabolic drive via beta-1 adrenergic antagonism, ...
  http://www.numedicus.co.uk/blog/first-in-class-new-drug-for-cachexia/
*  Penbutolol - Wikipedia
Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. It was ... two new beta-adrenergic blockers with partial agonism. Journal of Clinical Pharmacology, 30(5):412-21 PMID 2189902 FDA History ... Penbutolol is a sympathomimetic drug with properties allowing it to act as a partial agonist at β adrenergic receptors. ... Penbutolol is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making ...
  https://en.wikipedia.org/wiki/Penbutolol
*  Research Interests for Edward D. Levin
Drug Design, Drug Discovery, Drug Evaluation, Preclinical, Drug Implants, Drug Interactions, Drug Partial Agonism, Drug ... Adrenergic, Receptors, Adrenergic, alpha-2, Receptors, Adrenergic, beta, Receptors, Cholinergic, Receptors, Dopamine, Receptors ... Synergism, Drug Therapy, Combination, Drug Tolerance, Drug Toxicity, Drugs, Investigational, Dyskinesia, Drug-Induced, Eating, ... Drug Administration Schedule, Drug Antagonism, Drug Combinations, Drug Delivery Systems, ...
  http://fds.duke.edu/db/aas/pn/faculty/edlevin/research.html
*  ABSORPTION OF DRUGS FROM THE STOMACH. II. THE HUMAN | Journal of Pharmacology and Experimental Therapeutics
Binding, Partial Agonism, and Potentiation of α1-Adrenergic Receptor Function by Benzodiazepines: A Potential Site of ... Binding, Partial Agonism, and Potentiation of α1-Adrenergic Receptor Function by Benzodiazepines: A Potential Site of ... The human stomach is capable of absorbing most acidic drugs and the very weakly basic drugs. Salicylic acid, aspirin, ... ABSORPTION OF DRUGS FROM THE STOMACH. II. THE HUMAN. C. Adrian M. Hogben, Lewis S. Schanker, Dominick J. Tocco and Bernard B. ...
  http://jpet.aspetjournals.org/content/120/4/540?ijkey=13b06c12acff89e32d6589379ed8ebd2842512e1&keytype2=tf_ipsecsha
*  Iris View Profile
"Unknown Drug" Project practicals in the second half of this course, where teams of students identify an adrenergic drug by ... Indeed, to this day concepts that are central to pharmacology and receptor theory, such as partial agonism and efficacy, are ...
  http://iris.ucl.ac.uk/iris/browse/profile?upi=LGSIV31
*  Labetalol - Wikipedia
Labetalol was the first drug created that combined both alpha- and beta- adrenergic receptor blocking properties. It was ... Labetalol relaxes vascular smooth muscle by a combination of this partial beta2- agonism and through alpha1- blockade. Overall ... Labetalol is highly selective for postsynaptic alpha1- adrenergic, and non-selective for beta-adrenergic receptors. It is about ... and those with hypersensitivity to the drug. The minimum requirement for adrenergic agents is a primary or secondary amine ...
  https://en.wikipedia.org/wiki/Labetalol
*  Pejman Ghanouni, MD, PhD's Profile | Stanford Profiles
Drugs that activate G protein-coupled receptors are classified as either agonists or partial agonists. To study the mechanism ... These results provide new insight into the structural consequence of antagonist binding and the basis of agonism and partial ... Agonist-induced conformational changes in the G-protein-coupling domain of the beta(2) adrenergic receptor PROCEEDINGS OF THE ... Drugs acting at G protein coupled receptors can be classified in biological assays as either agonists, partial agonists, ...
  https://profiles.stanford.edu/pejman-ghanouni
*  Conformation guides molecular efficacy in docking screens of activated β-2 adrenergic G protein coupled receptor. - PubMed -...
... consistent with partial agonism. QUI is the known agonist quinpirole (black circle). (B) The GloSensor assay was run in inverse ... This functional fidelity has important implications in drug design, as the ability to predict ligands with predefined signaling ... Two partial β2AR agonists with new activating chemotypes in their docked poses. (A) The docked pose of isoproterenol, with a ... Conformation guides molecular efficacy in docking screens of activated β-2 adrenergic G protein coupled receptor.. Weiss DR1, ...
  https://www.ncbi.nlm.nih.gov/pubmed/23485065
*  Meta-Chlorophenylpiperazine - Wikipedia
It also has some affinity for α1-adrenergic, α2-adrenergic, H1, I1, and NET. It behaves as an agonist at most serotonin ... EMCDDA ANVISA resolution - Portaria SVS/MS 344/98 "关于印发《非药用类麻醉药品和精神药品列管办法》的通知" (in Chinese). China Food and Drug Administration ... 32.1 and 28.8 nM). It acts as a partial agonist of the human 5-HT2C receptor but as an antagonist of the human 5-HT2A and 5- ... In accordance with its lack of agonism towards the human 5-HT2A receptor, there are no reports that
  https://en.wikipedia.org/wiki/Meta-Chlorophenylpiperazine
*  Plus it
This phenomenon is termed protean agonism. Protean agonism indicates that a given drug may produce different physiological ... Prior stimulation at the β2-adrenergic receptor, for example, has been shown to enhance the inverse agonist activity of certain ... Both partial desensitization by receptor phosphorylation and release from calmodulin-induced constraints on basal MOR activity ... Data are expressed as percentage of adenylyl cyclase activity in the absence of drug. ★, ★★, compared with no drug, p , 0.05, p ...
  http://jpet.aspetjournals.org/content/308/2/512
*  Receptor antagonist - Wikipedia
Partial agonists are defined as drugs that, at a given receptor, might differ in the amplitude of the functional response that ... In addition, it has been suggested that partial agonism prevents the adaptive regulatory mechanisms that frequently develop ... Phenoxybenzamine is an example of an irreversible alpha blocker-it permanently binds to α adrenergic receptors, preventing ... Competitive antagonists are used to prevent the activity of drugs, and to reverse the effects of drugs that have already been ...
  https://en.wikipedia.org/wiki/Receptor_antagonist
*  Dopamine agonist - Wikipedia
... the psychoactivity of which is mainly due to Kappa-opioid receptor agonism; partial agonist at the D2 with an Intrinsic ... Some medical drugs act as dopamine agonists and can treat hypodopaminergic (low dopamine) conditions; they are typically used ... antagonist Dopamine reuptake inhibitor Receptor agonist GABA receptor agonist Dopaminergic Serotonin agonist Adrenergic agonist ... partial agonist. Psychoactivity mainly due to NMDA antagonism) Quinpirole (Partial agonist of the D2 and D3 family of receptors ...
  https://en.wikipedia.org/wiki/Dopamine_agonist
*  Beta blocker - Wikipedia
Ahrens RC (1990). "Skeletal muscle tremor and the influence of adrenergic drugs". The Journal of Asthma. 27 (1): 11-20. doi: ... See partial agonist for a more general description. Some beta blockers (e.g. oxprenolol, pindolol, penbutolol, labetalol and ... this term is used particularly with beta blockers that can show both agonism and antagonism at a given beta receptor, depending ... β1-adrenergic receptors are located mainly in the heart and in the kidneys. β2-adrenergic receptors are located mainly in the ...
  https://en.wikipedia.org/wiki/Beta_blocker
*  Azapirone - Wikipedia
... as antagonists or partial agonists) α1-adrenergic receptor (as antagonists) α2-adrenergic receptor (as antagonists) Actions at ... Stahl, SM; Lee-Zimmerman, C (May 1, 2013). "Serotonergic drugs for depression and beyond". Curr Drug Targets. 14 (5): 578-85. ... all of them except 5-HT1A agonism are generally undesirable in anxiolytics and only contribute to side effects. As a result, ... 1-PP possesses 5-HT1A partial agonist and α2-adrenergic antagonist actions and likely contributes overall mostly to side ...
  https://en.wikipedia.org/wiki/Azapirone
*  US8101619B2 - Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake...
... serotonin reuptake inhibition and partial agonism on dopamine-D 2 receptors. The invention also relates to the use of a ... "Antiparkinsonian Antidepressant Anxiolytic Dopamine D2 Partial Agonist 5-HT 1a Agonist," Drugs of the Future, vol. 26, No. 2, ... Selective β3 adrenergic agonist US20050124627A1 (en) 2005-06-09. Cyclic amides US6284759B1 (en) 2001-09-04. 2- ... US11294603 2004-12-08 2005-12-06 Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and ...
  https://patents.google.com/patent/US8101619B2/en
*  Plus it
5-HT1A partial agonism, and antagonism at 5-HT2A, α1B- and α2C-adrenergic receptors (Maeda et al., 2014), supporting a ... The importance of 5-HT1A receptor agonism in antipsychotic drug action: rationale and perspectives. Curr Opin Investig Drugs 11 ... combining moderate-intrinsic activity 5-HT1A receptor partial agonism and low-intrinsic activity D2 receptor partial agonism ... A key issue for D2 partial agonism is to determine an optimal level of intrinsic activity (or relative efficacy at the D2 ...
  http://jpet.aspetjournals.org/content/350/3/605
*  Molecules | Free Full-Text | Current Concepts and Treatments of Schizophrenia | HTML
... research on GPCRs resulted in the exploration of novel important signaling mechanisms of GPCRs which are crucial for drug ... drugs which display a balance between dopamine D2 antagonism or partial agonism and 5-HT1A receptor agonism/partial agonism ... Moreover, this drug also causes α1 adrenergic and histamine receptor blockade. Its anticholinergic effects are negligible. In ... Tuplin, E.W.; Holahan, M.R. Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity. Curr. Neuropharmacol ...
  https://www.mdpi.com/1420-3049/23/8/2087/htm
*  Elucidation of G-protein and β-arrestin functional selectivity at the dopamine D2 receptor | PNAS
2010) Third generation antipsychotic drugs: Partial agonism or receptor functional selectivity? Curr Pharm Des 16(5):488-501. ... G protein-coupled receptor kinases (GRKs) orchestrate biased agonism at the {beta}2-adrenergic receptor ... 2006) beta-arrestin-dependent, G protein-independent ERK1/2 activation by the beta2 adrenergic receptor. J Biol Chem 281(2): ... D2R is a prominent target for drug treatments in disorders where dopamine function is aberrant, such as schizophrenia. D2R ...
  https://www.pnas.org/content/112/22/7097
*  Section 6. Alcoholism and Drug Dependency | Harrison's Principles of Internal Medicine, 18e | AccessMedicine | McGraw-Hill...
... but primary buprenorphine overdose is nearly impossible because this agent is a partial opiate agonist. Partial agonism means ... partial agonist medications are commonly utilized for both maintenance and detoxification purposes. Alpha-2-adrenergic agonists ... Although some drug abusers may prefer a particular drug, the concurrent use of multiple drugs is often reported. Polydrug abuse ... It is a club drug commonly referred to as a "date-rape drug" or "roofies." The drug enhances GABAA receptor activity, and ...
  http://accessmedicine.mhmedical.com/content.aspx?bookid=331§ionid=40727212
*  Buspirone - Wikipedia
The drug has also been found to be effective in the treatment of depression as a standalone drug. There is evidence that ... The metabolite is a high-affinity partial agonist of the 5-HT1A receptor (Ki = 25 nM) similarly to buspirone, and has ... Some of its effects may be mediated via oxytocin release secondary to 5-HT1A receptor agonism.[non-primary source needed] ... However, buspirone has been reported to have shown "significant and selective intrinsic efficacy" at the α1-adrenergic receptor ...
  https://en.wikipedia.org/wiki/Buspirone
*  Lumateperone - Wikipedia
... a property which is likely due to its partial agonism of presynaptic D2 receptors. In accordance, similarly to aripiprazole, ... Nancy A. Melville (2015). "Novel Drug Promising for Schizophrenia". Medscape Medical News. Li P, Zhang Q, Robichaud AJ, Lee T, ... and α1B-adrenergic receptors (Ki = 73 nM at α1), 5-HT2C receptor (Ki = 173 nM), and D4 receptor. Lumateperone does not ... It acts as a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of ...
  https://en.wikipedia.org/wiki/Lumateperone
*  Method of Treating Airway Diseases With Beta-Adrenergic Inverse Agonists - Patent application
The drugs used were salbutamol (a β1/β2-adrenergic agonist), alprenolol (a β1/β2-adrenergic antagonist with partial agonist ... agonists that display inverse agonism to both the β1- and β2-adrenergic receptors or as a selective β2-inverse agonist. [0106] ... partial agonist activity. Carvedilol is a β1/β2 non-selective adrenergic antagonist with α1-adrenergic antagonist activity. In ... β-adrenergic inverse agonist drugs, either alone or in combination with other drugs, such as β2-agonists, steroids, leukotriene ...
  http://www.patentsencyclopedia.com/app/20080254022
*  Dopamine receptor D2 - Wikipedia
Agonism of D2sh receptors inhibits dopamine release; antagonism increases dopaminergic release. A third D2(Longer) form differs ... The dopamine D2 receptor is the main receptor for most antipsychotic drugs. This gene encodes the D2 subtype of the dopamine ... Giacomelli S, Palmery M, Romanelli L, Cheng CY, Silvestrini B (1998). "Lysergic acid diethylamide (LSD) is a partial agonist of ... Piribedil - also D3 receptor agonist and α2-adrenergic antagonist Pramipexole - also D3, D4 receptor agonist Quinelorane - ...
  https://en.wikipedia.org/wiki/Dopamine_receptor_D2
*  Mirtazapine - Wikipedia
The drug acts as an antagonist of certain adrenergic and serotonin receptors, and is also a strong antihistamine. It is ... Antagonism of the 5-HT2 subfamily of receptors and inverse agonism of the 5-HT2C receptor appears to be in part responsible for ... Although not clinically relevant, mirtazapine has been found to act as a partial agonist of the κ-opioid receptor at high ... Mirtazapine is the English and French generic name of the drug and its INN, USAN, USP, BAN, DCF, and JAN. Its generic name in ...
  https://en.wikipedia.org/wiki/Mirtazapine