*  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/
*  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
*  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/
*  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
*  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
*  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
*  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
*  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
*  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
*  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
*  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
*  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
*  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
*  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
*  Plus it
... display of agonism and inverse agonism by H3 antagonists. J Pharmacol Exp Ther 299: 908-914. ... they reported that proxyfan could act as a partial inverse agonist (arachidonic acid release) as well as partial agonist (cAMP ... For the adrenergic receptors, it has been shown that the C-terminal portion of the i3 plays a crucial role in G-protein- ... Relative affinities are the MT6 Ki divided by the WT Ki for each drug. ...
  http://jpet.aspetjournals.org/content/307/1/213
*  The Discovery of Novel Selective D1 Dopaminergic Agonists: A-68930, A-77636, A-86929, and ABT-413
... journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug ... In support of this effort we developed 3D pharmacophore maps and 3D QSAR relationships for α1 and α2 adrenergic agonists and D2 ... Y. C. Martin, C. T. Lin, and J. Wu., "Application of CoMFA to D1 dopaminergic agonists: a case study," in 3D QSAR in Drug ... This early biological testing also revealed that the phenyl group of the partial D1 agonist SKF-38393, 2, increased the ...
  https://www.hindawi.com/journals/ijmc/2011/424535/
*  Plus it
2006) Molecular basis of partial agonism at the neurotransmitter alpha2A-adrenergic receptor and Gi-protein heterotrimer. J ... Functional selectivity is now well established as a drug phenomenon (Kenakin, 2007). Our results strengthen the case for ... It is noteworthy that the functional implications of partial agonism will differ in different CCR2-expressing cell types, as ... partial agonism, the stabilization of intrinsically different receptor conformations by different ligands emerges as a new ...
  http://molpharm.aspetjournals.org/content/79/3/488
*  Inverse Agonist Activity at the α2A-Adrenergic Receptor | Molecular Pharmacology
In contrast, the partial agonist clonidine exhibited only a 3.3-fold increase, whereas UK-14,304, discussed above, was more ... Drugs were assayed for their ability to stimulate cAMP production in forskolin-stimulated CAM cells over a range of ... To understand conformational changes in the CAM receptor and their relation to mechanisms of inverse agonism, we wanted to ... adrenergic receptor. 5-HT. 5-hydroxytrytamine. PTX. pertussis toxin. IBMX. isobutylmethylxanthine. HA. hemagglutinin. CHO. ...
  http://molpharm.aspetjournals.org/content/59/3/532
*  Plus it
In the β2-adrenergic receptor, ligands with proven inverse agonism on AC activity were used to see if they could also regulate ... Clark recognized that the ability of a drug to produce an intracellular signal depended upon the drug ("fixing") to a receptor ... Han M, Lou J, Nakanishi K, Sakmar TP, and Smith SO (1997) Partial agonist activity of 11-cis-retinal in rhodopsin mutants. J ... proxyfan displayed a spectrum of activity ranging from full agonism to full inverse agonism. Thus, protean agonism demonstrated ...
  http://pharmrev.aspetjournals.org/content/57/2/147
*  Comparative pharmacology of antipsychotics possessing combined dopamine D2and serotonin 5-HT1Areceptor properties | SpringerLink
Mailman RB, Murthy V (2010) Third generation antipsychotic drugs: partial agonism or receptor functional selectivity? Curr ... An alpha2C-adrenergic receptor polymorphism alters the norepinephrine-lowering effects and therapeutic response of the beta- ... Compounds possessing "balanced" 5-HT1A receptor agonism and D2 antagonism (or weak partial agonism) and, in some cases, ... Fermini B, Fossa AA (2003) The impact of drug-induced QT interval prolongation on drug discovery and development. Nat Rev Drug ...
  https://link.springer.com/article/10.1007%2Fs00213-011-2247-y
*  30+ New Antidepressants (2018): Drugs In Clinical Trials
The buprenorphine facilitates mood enhancement via partial agonism of the mu-opioid receptor (MOR) and full agonism of the ... The drug functions as an antagonist at several neurotransmitter receptor sites, including: Alpha-2A adrenergic receptors; D2 ... 20 New Antidepressants In The Pipeline (2015): Drugs In Clinical Trials. *The Most Dangerous Psychiatric Drugs: Highest Risk ... The drug functions as a selective partial agonist upon NMDA receptors, specifically at allosteric sites of the glycine binding ...
  https://mentalhealthdaily.com/2018/02/13/new-antidepressants-2018-drugs-in-clinical-trials/
*  Exploring the Mechanism of Agonist Efficacy: A Relationship between Efficacy and Agonist Dissociation Rate at the Muscarinic M3...
Hoeren M, Brawek B, Mantovani M, Löffler M, Steffens M, van Velthoven V, and Feuerstein TJ (2008) Partial agonism at the human ... Paton WD (1961) A theory of drug action based on rate of drug-receptor combination. Proc R Soc Lond B Biol Sci 154: 21-69. ... Krasel C, Bünemann M, Lorenz K, and Lohse MJ (2005) β-arrestin binding to the β2-adrenergic receptor requires both receptor ... Colquhoun D (1973) The relationship between classical and cooperative models for drug action, in A Symposium on Drug Receptors ...
  http://molpharm.aspetjournals.org/content/76/3/543.full