A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine
... Pre-clinical studies suggest that negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGluR5), including 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and fenobam are highly effective in attenuating drug-taking an ...
... Pre-clinical studies suggest that negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGluR5), including 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and fenobam are highly effective in attenuating drug-taking an ...
Glucagon Receptor Agonists and Antagonists
... that suppress ocular elongation (plus-lens treatment, recovery from form-deprivation [FD] myopia), but not by conditions that permit or induce ocular elongation (form deprivation, minuslens treatment).7,11 The release of glucagon during plus defocus may be inferred from the supposition that inductio ...
... that suppress ocular elongation (plus-lens treatment, recovery from form-deprivation [FD] myopia), but not by conditions that permit or induce ocular elongation (form deprivation, minuslens treatment).7,11 The release of glucagon during plus defocus may be inferred from the supposition that inductio ...
Salvia divinorum and Salvinorin A: An Update on Pharmacology and
... olism of salvinorin A or of other compounds in the plant that exhibit an antidepressant activity. If salvinorin A is metabolized to an either active or inactive metabolite, then the binding affinity and the pharmacological profile studied in vitro are at jeopardy. A further study evaluated the effec ...
... olism of salvinorin A or of other compounds in the plant that exhibit an antidepressant activity. If salvinorin A is metabolized to an either active or inactive metabolite, then the binding affinity and the pharmacological profile studied in vitro are at jeopardy. A further study evaluated the effec ...
Structure-based design of hyaluronidase inhibitors
... growth and migration as well as tumour spread. Increased levels of hyaluronan are observed during morphogenesis, embryonic development, wound healing and inflammation.5,7 The function of HA may be partly regulated dependent on its chain length, e.g. angiogenesis is presumably induced by small HA oli ...
... growth and migration as well as tumour spread. Increased levels of hyaluronan are observed during morphogenesis, embryonic development, wound healing and inflammation.5,7 The function of HA may be partly regulated dependent on its chain length, e.g. angiogenesis is presumably induced by small HA oli ...
antihistamines in allergic disease
... onset of effect occurs within 1-3 hours; their duration of action varies from several hours to 24 hours, (second-generation drugs being generally around 24 hours) (Table II).7 First-generation antihistamines and some of the second-generation agents are oxidatively metabolised by the hepatic cytochro ...
... onset of effect occurs within 1-3 hours; their duration of action varies from several hours to 24 hours, (second-generation drugs being generally around 24 hours) (Table II).7 First-generation antihistamines and some of the second-generation agents are oxidatively metabolised by the hepatic cytochro ...
Seeing Through the MIST: Abundance Versus Percentage
... channel can have profound influence on cardiac function, therefore the intrinsic potency of the drug or metabolite for the IKr channel does not have to be as high as that for the primary pharmacology to exert an undesirable side effect. ...
... channel can have profound influence on cardiac function, therefore the intrinsic potency of the drug or metabolite for the IKr channel does not have to be as high as that for the primary pharmacology to exert an undesirable side effect. ...
The Sleep - American Osteopathic Association
... • Commonly used medications include trazodone, mirtazapine, amitriptyline, and doxepin • Doses used for insomnia are much lower than those used for depression • Doxepin was approved in 2010 for maintenance insomnia (3 and 6 mg), because it has histamine selective properties at low doses ...
... • Commonly used medications include trazodone, mirtazapine, amitriptyline, and doxepin • Doses used for insomnia are much lower than those used for depression • Doxepin was approved in 2010 for maintenance insomnia (3 and 6 mg), because it has histamine selective properties at low doses ...
Serum albumin, the most abundant protein in the
... Serum albumin, the most abundant protein in the circulatory system, has been one of the most extensively studied of all proteins 1. Serum albumins are prone to bind effectively many small organic molecules. Bovine serum albumin (BSA), a large globular protein (65,000 Daltons), consists of a single c ...
... Serum albumin, the most abundant protein in the circulatory system, has been one of the most extensively studied of all proteins 1. Serum albumins are prone to bind effectively many small organic molecules. Bovine serum albumin (BSA), a large globular protein (65,000 Daltons), consists of a single c ...
Lesson 24: Cannabis student notes cannabislessonStudent
... cannabis plant are huge numbers of similarly-shaped molecules called cannabinoids. Many reputable sources will claim that one cannabinoid, 9-THC or delta-9 tetra-hydro-cannabinol is THE psychoactive cannabinoid. Since more than 60 cannabinoids have been identified, and since some are present in Can ...
... cannabis plant are huge numbers of similarly-shaped molecules called cannabinoids. Many reputable sources will claim that one cannabinoid, 9-THC or delta-9 tetra-hydro-cannabinol is THE psychoactive cannabinoid. Since more than 60 cannabinoids have been identified, and since some are present in Can ...
Actions of bufalin and cinobufotalin, two bufadienolides respectively
... The results of the ouabain-sensitive binding assays with the addition of non-labelled ouabain, bufalin and cinobufotalin are shown in Fig. 1.All nine blood samples were tested separately over the range 10-9-10-6 mol/l for ouabain and cinobufotalin and 10- l o - l O - h mol/l for bufalin. The curve w ...
... The results of the ouabain-sensitive binding assays with the addition of non-labelled ouabain, bufalin and cinobufotalin are shown in Fig. 1.All nine blood samples were tested separately over the range 10-9-10-6 mol/l for ouabain and cinobufotalin and 10- l o - l O - h mol/l for bufalin. The curve w ...
Addictiveness and Attractiveness of Tobacco Additives
... potential whereas in humans, tobacco is used differently (e.g. inhalation, oral consumption) and is highly addictive. No method currently used to define addictive potency of a compound can therefore be considered as adequate. 3. Dose-dependency of development of nicotine addictiveness In humans, the ...
... potential whereas in humans, tobacco is used differently (e.g. inhalation, oral consumption) and is highly addictive. No method currently used to define addictive potency of a compound can therefore be considered as adequate. 3. Dose-dependency of development of nicotine addictiveness In humans, the ...
Structural Basis for Interaction of Inhibitors with Cyclin
... interest in chemical CDKs inhibitors that could play an important role in the discovery of a new family of antitumor agents [12]. Since ATP is the authentic cofactor of CDK2 it can be considered as a "lead compound" for discovery of CDK2 inhibitors. However, there are two major concerns: adenine con ...
... interest in chemical CDKs inhibitors that could play an important role in the discovery of a new family of antitumor agents [12]. Since ATP is the authentic cofactor of CDK2 it can be considered as a "lead compound" for discovery of CDK2 inhibitors. However, there are two major concerns: adenine con ...
1. Clinical Pharmacology
... reported to be effective in reducing respiratory depression (Boyd et al 2003). Because of the uncertain response to naloxone, prolonged ventilatory support may be required in overdoses involving buprenorphine. Naltrexone can precipitate a withdrawal reaction in patients on buprenorphine, although th ...
... reported to be effective in reducing respiratory depression (Boyd et al 2003). Because of the uncertain response to naloxone, prolonged ventilatory support may be required in overdoses involving buprenorphine. Naltrexone can precipitate a withdrawal reaction in patients on buprenorphine, although th ...
as a PDF
... EtOH (Gallate et al., 1999). The EtOH deprivation effect is 2002). In addition, downregulation of CB1 receptors and CB1 also blocked by SR141716A treatment in EtOH-preferring receptor agonist stimulated [35S]GTPgS binding in SPM of mice chronically exposed to EtOH have been reported (sP) rats (Serra ...
... EtOH (Gallate et al., 1999). The EtOH deprivation effect is 2002). In addition, downregulation of CB1 receptors and CB1 also blocked by SR141716A treatment in EtOH-preferring receptor agonist stimulated [35S]GTPgS binding in SPM of mice chronically exposed to EtOH have been reported (sP) rats (Serra ...
pharmacological manipulation of cb1 receptor
... mice. However, chronic CP-55,940 administration alone resulted in tolerance to the sedative effect of a challenge dose of EtOH in control mice. Acute CP-55,940 administration after chronic alcoholization blocked the development of tolerance to EtOH-induced sedation compared to the EtOH alone exposed ...
... mice. However, chronic CP-55,940 administration alone resulted in tolerance to the sedative effect of a challenge dose of EtOH in control mice. Acute CP-55,940 administration after chronic alcoholization blocked the development of tolerance to EtOH-induced sedation compared to the EtOH alone exposed ...
Treatment of Bronchial Asthma
... They are 1000-fold more potent than histamine in stimulating airway smooth muscle constriction. They also promote microvascular leakage, mucus secretion and eosinophil chemotaxis. Pathway augmented by COX inhibitors (i.e. NSAIDs) ...
... They are 1000-fold more potent than histamine in stimulating airway smooth muscle constriction. They also promote microvascular leakage, mucus secretion and eosinophil chemotaxis. Pathway augmented by COX inhibitors (i.e. NSAIDs) ...
ABSTRACT Title of Dissertation: ENERGETICS OF DRUG INTERACTIONS
... enhances the binding enthalpies so that the β-cyclodextrin binding reactions are enthalpydriven. In the larger γ-cyclodextrin cavity, water is retained so that, not only are the interactions between the drug and the cavity reduced, there is an increase in the drug configurations resulting in increas ...
... enhances the binding enthalpies so that the β-cyclodextrin binding reactions are enthalpydriven. In the larger γ-cyclodextrin cavity, water is retained so that, not only are the interactions between the drug and the cavity reduced, there is an increase in the drug configurations resulting in increas ...
Ultra-Low Dose Antagonist Effects on Cannabinoids and Opioids in Models... Is Less More? By
... An ultra-low dose of a drug is approximately 1000-fold lower than the dose range traditionally used to induce a therapeutic effect. The purpose of the present thesis was to broaden the knowledge of the ultra-low dose effect, that was previously identified in the opioid receptor system, by looking at ...
... An ultra-low dose of a drug is approximately 1000-fold lower than the dose range traditionally used to induce a therapeutic effect. The purpose of the present thesis was to broaden the knowledge of the ultra-low dose effect, that was previously identified in the opioid receptor system, by looking at ...
article in press
... programmed. After that, it was investigated the effect of guanosine, flunarizine and cinnarizine on animal models of psychosis, as well as in other behavioral tasks. Guanosine was chosen because it has been shown to interact with the glutamatergic system – which is known to be involved in the pathop ...
... programmed. After that, it was investigated the effect of guanosine, flunarizine and cinnarizine on animal models of psychosis, as well as in other behavioral tasks. Guanosine was chosen because it has been shown to interact with the glutamatergic system – which is known to be involved in the pathop ...
Multiple mechanisms involved in the large-spectrum
... CBD was able to antagonize the effects of the CB1 agonist CP55940-induced stimulation of [35S]GTPgS binding to mouse brain membranes at a much lower concentration (KB ¼ 79 nM) than the Ki for displacement of the CB1 ligand. b CBD acts as an inverse agonist with a lower concentration (KB ¼ 65 nM) tha ...
... CBD was able to antagonize the effects of the CB1 agonist CP55940-induced stimulation of [35S]GTPgS binding to mouse brain membranes at a much lower concentration (KB ¼ 79 nM) than the Ki for displacement of the CB1 ligand. b CBD acts as an inverse agonist with a lower concentration (KB ¼ 65 nM) tha ...
Systemic administration of β2-adrenoceptor agonists, formoterol and
... (Löfdahl and Svedmyr, 1989; Ball et al., 1991; Guhan et al., 2000). To this end, two b2-agonists, formoterol fumarate and salmeterol xinafoate, have been recently approved in the U.S. for the treatment of asthma. These b2-agonists have an extended duration of action in relaxing smooth muscle compar ...
... (Löfdahl and Svedmyr, 1989; Ball et al., 1991; Guhan et al., 2000). To this end, two b2-agonists, formoterol fumarate and salmeterol xinafoate, have been recently approved in the U.S. for the treatment of asthma. These b2-agonists have an extended duration of action in relaxing smooth muscle compar ...
Nicotinic agonist
A nicotinic agonist is a drug that mimics the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs). The nAChR is named for its affinity for nicotine.Examples include nicotine (by definition), acetylcholine (the endogenous agonist of nAChRs), choline, epibatidine, lobeline, varenicline and cytisine.