Slide 1
... MCS (Maximal Common Substructure): find the largest set of 3D features that common to all of the input ligands MCS drawbacks: assume that there is a single common pharmacophore Relaxed MCS: relaxing the requirement that all ligands must possess all features ...
... MCS (Maximal Common Substructure): find the largest set of 3D features that common to all of the input ligands MCS drawbacks: assume that there is a single common pharmacophore Relaxed MCS: relaxing the requirement that all ligands must possess all features ...
John Salamone: Dopamine, Motivation and Schizophrenia
... antipsychotics based upon their mesolimbic actions; perhaps antipsychotic effects are due to actions on other systems (e.g. mesocortical DA). • They are related; the core antipsychotic effect could be directly dependent upon the fundamental motivational effects of D2 antagonists, which can be studie ...
... antipsychotics based upon their mesolimbic actions; perhaps antipsychotic effects are due to actions on other systems (e.g. mesocortical DA). • They are related; the core antipsychotic effect could be directly dependent upon the fundamental motivational effects of D2 antagonists, which can be studie ...
... As in previous studies, there was no effect of BAY u 3405 on baseline FEV1 at 90 min after ingestion and prior to agonist challenge, suggesting that TP receptormediated bronchoconstriction resulting from increased basal secretion of contractile prostanoids contributes little to baseline airway calib ...
OpioidAnalgesics_2
... • Like other opioids, e.g. Diamorphine (heroin), morphine acts directly on the central nervous system (CNS) to relieve pain, and at synapses of the nucleus accumbens in particular. • Morphine is highly addictive when compared to other substances, and tolerance and physical and ...
... • Like other opioids, e.g. Diamorphine (heroin), morphine acts directly on the central nervous system (CNS) to relieve pain, and at synapses of the nucleus accumbens in particular. • Morphine is highly addictive when compared to other substances, and tolerance and physical and ...
The so-called „designer steroids“ Nor
... The anabolic androgenic steroids belong to the list of prohibited substances given by the WADA´s List Committee. In fact, not all the biological and toxicological risks especially when administered for doping purposes are unknown. Thus, we completely characterized the substances Norbolethone, Desoxy ...
... The anabolic androgenic steroids belong to the list of prohibited substances given by the WADA´s List Committee. In fact, not all the biological and toxicological risks especially when administered for doping purposes are unknown. Thus, we completely characterized the substances Norbolethone, Desoxy ...
What is the prognosis for new centrally-acting anti
... diabetes. At Week-52, the placebo-subtracted weight-loss produced by locaserin was 3.6 kg (Smith et al., 2010) and 2.9 kg in healthy obese subjects (Lorcaserin NDA, 2010) and 3.1 kg in obese diabetics (Arena Pharmaceuticals Press Release, 2010) (Table 2). The corresponding responder analyses reveale ...
... diabetes. At Week-52, the placebo-subtracted weight-loss produced by locaserin was 3.6 kg (Smith et al., 2010) and 2.9 kg in healthy obese subjects (Lorcaserin NDA, 2010) and 3.1 kg in obese diabetics (Arena Pharmaceuticals Press Release, 2010) (Table 2). The corresponding responder analyses reveale ...
SECONDARY METABOLITES ISOLATED FROM PEROVSKIA
... atom types, number of chiral centers, and number of rings and chains (Gao, 2010). Based on the results of this investigation, it was determined that natural products are significantly more diverse than combinatorial compounds (Gao, 2010). Furthermore, natural products have superior drug-like propert ...
... atom types, number of chiral centers, and number of rings and chains (Gao, 2010). Based on the results of this investigation, it was determined that natural products are significantly more diverse than combinatorial compounds (Gao, 2010). Furthermore, natural products have superior drug-like propert ...
Pharmacodynamics of Selective Androgen Receptor
... androgens, our laboratories designed and synthesized multiple series of nonsteroidal compounds, and explored the structure-activity relationships for androgenic and anabolic activities, both in vitro and in vivo (He et al., 2002; Yin et al., 2003a,b). According to results from these structure-activi ...
... androgens, our laboratories designed and synthesized multiple series of nonsteroidal compounds, and explored the structure-activity relationships for androgenic and anabolic activities, both in vitro and in vivo (He et al., 2002; Yin et al., 2003a,b). According to results from these structure-activi ...
... prontosil had antibacterial properties in vivo (i.e. when given to laboratory animals). Strangely enough, no antibacterial effect was observed in vitro. In other words, prontosil could not kill bacteria grown in the test tube. This remained a mystery until it was discovered that prontosil was not in ...
Delta-Opioid Ligands Reverse Alfentanil
... colleagues also found stimulatory effects of opioids on respiration; the fetal breathing movement of lamb was stimulated by lower doses of DPDPE and deltrophin I (Cheng et al., 1992, 1993a, b). The involvement of the kappa receptor in respiratory control seems to be minimal (Pfeiffer et al., 1983; B ...
... colleagues also found stimulatory effects of opioids on respiration; the fetal breathing movement of lamb was stimulated by lower doses of DPDPE and deltrophin I (Cheng et al., 1992, 1993a, b). The involvement of the kappa receptor in respiratory control seems to be minimal (Pfeiffer et al., 1983; B ...
Naloxone fails to produce conditioned place aversion in
... AbstractöThere is growing evidence that tonic activity of the opioid system may be important in the modulation of a¡ective state. Naloxone produces a conditioned place aversion in rodents, an e¡ect that is centrally mediated. Previous pharmacological data using antagonists with preferential actions ...
... AbstractöThere is growing evidence that tonic activity of the opioid system may be important in the modulation of a¡ective state. Naloxone produces a conditioned place aversion in rodents, an e¡ect that is centrally mediated. Previous pharmacological data using antagonists with preferential actions ...
Anxiolytic-Like Effects of κ-Opioid Receptor Antagonists in Models of
... the exception of rats treated with fluoxetine and chlordiazepoxide, which were not tested in the FPS paradigm. Rats received i.p. injections of norBNI or JDTic 48 h before the first behavioral test (EPM test) and did not receive additional treatments. The time point of KOR antagonist administration ...
... the exception of rats treated with fluoxetine and chlordiazepoxide, which were not tested in the FPS paradigm. Rats received i.p. injections of norBNI or JDTic 48 h before the first behavioral test (EPM test) and did not receive additional treatments. The time point of KOR antagonist administration ...
Characterization of the Analgesic and Anti
... brain barrier in either rats or humans (Mroszczak et al., 1987), evidence that (R,S)-ketorolac acts at sites in the central as well as the peripheral nervous system to produce analgesia has accumulated. For example, after intrathecal (i.t.) administration, (R,S)-ketorolac blocks pain states associat ...
... brain barrier in either rats or humans (Mroszczak et al., 1987), evidence that (R,S)-ketorolac acts at sites in the central as well as the peripheral nervous system to produce analgesia has accumulated. For example, after intrathecal (i.t.) administration, (R,S)-ketorolac blocks pain states associat ...
Naltrexone potentiates anti-HIV-1 activity of antiretroviral drugs in
... The phenomenon of synergistic interactions of antimicrobial drugs has long been recognized in the field of antibacterial therapy. For example, at clinically achievable concentrations, aminoglycosides have no inhibitory activity against Enterococcus spp., a major cause of infective endocarditis, but ...
... The phenomenon of synergistic interactions of antimicrobial drugs has long been recognized in the field of antibacterial therapy. For example, at clinically achievable concentrations, aminoglycosides have no inhibitory activity against Enterococcus spp., a major cause of infective endocarditis, but ...
Reciprocal Regulation of Agonist and Inverse Agonist Signaling
... Results from cAMP accumulation assays appear in Fig. 2 and show that pretreatment with ICI174864 did not modify the dose-response curve for SNC-80 but increased bremazocine potency by 6.6-fold, an effect that was associated with an increase in the Hill coefficient (Hill slope values in controls, ⫺0. ...
... Results from cAMP accumulation assays appear in Fig. 2 and show that pretreatment with ICI174864 did not modify the dose-response curve for SNC-80 but increased bremazocine potency by 6.6-fold, an effect that was associated with an increase in the Hill coefficient (Hill slope values in controls, ⫺0. ...
Anti-platelet agents
... • Fab fragment of Chimeric monoclonal antibody against GP-IIb/IIIa. • Used to prevent platelet aggregation in patients having PCI, administered along with aspirin & heparin or LMW heparin • Most common A/E is bleeding • May cause thrombocytopenia, hypotension, bradycardia • Non antigenic • Dose: 0.2 ...
... • Fab fragment of Chimeric monoclonal antibody against GP-IIb/IIIa. • Used to prevent platelet aggregation in patients having PCI, administered along with aspirin & heparin or LMW heparin • Most common A/E is bleeding • May cause thrombocytopenia, hypotension, bradycardia • Non antigenic • Dose: 0.2 ...
The serotonin RECEPTOR antagonists NAN
... indicate that methamphetamine increased central serotonin (5-HT) levels more markedly than other psychomotor stimulants such as amphetamine or cocaine. However, several studies indicate that 5-HT agonists and uptake inhibitors did not produce any methamphetamine-like stimulus effects when administra ...
... indicate that methamphetamine increased central serotonin (5-HT) levels more markedly than other psychomotor stimulants such as amphetamine or cocaine. However, several studies indicate that 5-HT agonists and uptake inhibitors did not produce any methamphetamine-like stimulus effects when administra ...
CP47,497-C8 and JWH073, commonly found in `Spice` herbal
... ‘Spice’ is an herbal blend that has been reported to produce cannabis-like effects when smoked and is marketed as an alternative to marijuana. Synthetic additives have been identified in numerous ‘Spice’ preparations from different sources. Common among many of the preparations were the compounds JWH ...
... ‘Spice’ is an herbal blend that has been reported to produce cannabis-like effects when smoked and is marketed as an alternative to marijuana. Synthetic additives have been identified in numerous ‘Spice’ preparations from different sources. Common among many of the preparations were the compounds JWH ...
Effector Pathway-Dependent Relative Efficacy at Serotonin Type 2A
... Traditional receptor theory assumes that the degree of effector activity produced by an agonist is a function of the receptor stimulus produced by the agonist (Kenakin, 1997), that for a particular receptor the stimulus is independent of the effector pathway to which the receptor is linked, and that ...
... Traditional receptor theory assumes that the degree of effector activity produced by an agonist is a function of the receptor stimulus produced by the agonist (Kenakin, 1997), that for a particular receptor the stimulus is independent of the effector pathway to which the receptor is linked, and that ...
Pellow, S., File, S.E. (1986). Anxiolytic and anxiogenic drug effects
... injection of cannabinoid CB1 receptor antagonist (AM251) in the presence of alpha-1 adrenergic antagonist (Prazosin) on rat behavior in the EPM. Materials and Methods: In the present study, the data were obtained from male Wistar rat, which weighing 200-250 g. Animal behavior in EPM were videotaped ...
... injection of cannabinoid CB1 receptor antagonist (AM251) in the presence of alpha-1 adrenergic antagonist (Prazosin) on rat behavior in the EPM. Materials and Methods: In the present study, the data were obtained from male Wistar rat, which weighing 200-250 g. Animal behavior in EPM were videotaped ...
Structure-Based Identification of Binding Sites, Native Ligands and
... screening (VLS) algorithm that can screen millions of potential ligands by flexible docking them into a crystal structure or accurate model (experimentally and computationally validated) of a GPCR. In the past, we have successfully used an alliance between state-of-the-art computational techniques an ...
... screening (VLS) algorithm that can screen millions of potential ligands by flexible docking them into a crystal structure or accurate model (experimentally and computationally validated) of a GPCR. In the past, we have successfully used an alliance between state-of-the-art computational techniques an ...
I.2 New Prospects for Drug Discovery (IV)
... bind to the extracellular part of the receptor, and can interact with the TM domains, the three extracellular loops and/or the N-terminus. A significant number of GPCR binding sites for their corresponding ligands have been mapped from a combination of site-directed mutagenesis –and other biochemica ...
... bind to the extracellular part of the receptor, and can interact with the TM domains, the three extracellular loops and/or the N-terminus. A significant number of GPCR binding sites for their corresponding ligands have been mapped from a combination of site-directed mutagenesis –and other biochemica ...
Vapo-Cresolene - Society for Historical Archaeology
... Of the approximately 60,000 drug stores in the United States in the early 1900s, probably half devoted a large portion of their window–space and shelf–space to “antiseptics” and mouthwashes. Several million dollars were spent annually in magazine, newspaper and other advertising to convince a gullib ...
... Of the approximately 60,000 drug stores in the United States in the early 1900s, probably half devoted a large portion of their window–space and shelf–space to “antiseptics” and mouthwashes. Several million dollars were spent annually in magazine, newspaper and other advertising to convince a gullib ...
Discovery and development of TRPV1 antagonists
Relief from chronic pain remains a recognized unmet medical need. Consequently, the search for new analgesic agents is being intensively studied by the pharmaceutical industry. The TRPV1 receptor is an ion channel that has been implicated in mediation of many types of pain and therefore studied most extensively. The first competitive antagonist, capsazepine, was first described in 1990, since then development of novel TRPV1 antagonists has come a long way. This effort has led to the identification of several TRPV1 antagonists that have entered clinical trials as analgesic agents. Should these new chemical entities relieve symptoms of chronic pain then this class of compounds may offer one of the first novel mechanisms for the treatment of pain, in many years.