A Brief History of Great Discoveries in Pharmacology: In Celebration
... Although pharmacology is a discipline with a rich and enduring heritage, present-day pharmacology is quite a different discipline than the more traditional subject I studied as a graduate student in the early 1960s. The discipline is now deeply rooted in molecular biology and molecular genetics, bot ...
... Although pharmacology is a discipline with a rich and enduring heritage, present-day pharmacology is quite a different discipline than the more traditional subject I studied as a graduate student in the early 1960s. The discipline is now deeply rooted in molecular biology and molecular genetics, bot ...
Supplement
... gene locus. This is distinct from the production of ectopic signals via non-mammalian actuators such as ChR2 (23). Actuators constructed from engineered mammalian proteins (71) (including OptoXR (72), LOV-Rac (30), DREADD (25, 26), PSAM (24) and the SPARK/LiGluR family of actuators (27-29, 31, 73)) ...
... gene locus. This is distinct from the production of ectopic signals via non-mammalian actuators such as ChR2 (23). Actuators constructed from engineered mammalian proteins (71) (including OptoXR (72), LOV-Rac (30), DREADD (25, 26), PSAM (24) and the SPARK/LiGluR family of actuators (27-29, 31, 73)) ...
Discovery of PF-04457845: A Highly Potent
... hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. Genetic or pharmacological inactivation of FAAH leads to analgesic and anti-inflammatory phenotypes in rodents without showing the undesirable side effects observed with direct cannabin ...
... hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. Genetic or pharmacological inactivation of FAAH leads to analgesic and anti-inflammatory phenotypes in rodents without showing the undesirable side effects observed with direct cannabin ...
Spinal NMDA Receptors Contribute to Neuronal Processing of Acute
... stimulation in the rat. J Neurophysiol 86: 1783–1791, 2001. The present study investigated the role of NMDA receptors in the spinal processing of acute noxious and nonnoxious colorectal stimulation using extracellular single-unit recording in the rat. Fifty-three neurons in the L6–S2 dorsal horn of ...
... stimulation in the rat. J Neurophysiol 86: 1783–1791, 2001. The present study investigated the role of NMDA receptors in the spinal processing of acute noxious and nonnoxious colorectal stimulation using extracellular single-unit recording in the rat. Fifty-three neurons in the L6–S2 dorsal horn of ...
The a7 Nicotinic Receptor Agonist ABT-107 Decreases L
... Iravani et al., 2012; Huot et al., 2013). Currently, the only drug approved for LIDs is amantadine, and it is of only limited effectiveness. There is, therefore, an ongoing search for new therapies. Drugs targeting numerous classes of neurotransmitter receptors, including glutamatergic, serotonergic ...
... Iravani et al., 2012; Huot et al., 2013). Currently, the only drug approved for LIDs is amantadine, and it is of only limited effectiveness. There is, therefore, an ongoing search for new therapies. Drugs targeting numerous classes of neurotransmitter receptors, including glutamatergic, serotonergic ...
Docking and Ligand Binding Affinity: Uses and Pitfalls
... between two or more constituent molecules, trying to predict the position and orientation of a ligand (a small molecule) when it is bound to a protein in order to know the predominant binding mode(s) of a ligand with a protein of known three-dimensional structure. Successful docking methods search h ...
... between two or more constituent molecules, trying to predict the position and orientation of a ligand (a small molecule) when it is bound to a protein in order to know the predominant binding mode(s) of a ligand with a protein of known three-dimensional structure. Successful docking methods search h ...
READ MORE - Seropeutics
... Serotonin (5-HT) 5-HT2C receptor agonists have shown promise as novel alcoholism pharmacotherapies, but developing selective agonists has been problematic. Female Sprague Dawley rats were given ethanol in a palatable gel vehicle during operant sessions. 5-HT2C receptor modulators (Ro60-0175, SB242,0 ...
... Serotonin (5-HT) 5-HT2C receptor agonists have shown promise as novel alcoholism pharmacotherapies, but developing selective agonists has been problematic. Female Sprague Dawley rats were given ethanol in a palatable gel vehicle during operant sessions. 5-HT2C receptor modulators (Ro60-0175, SB242,0 ...
Newer Immunosuppressive Drugs: A Review
... autoimmune diseases such as rheumatoid arthritis. A large preclinical program has been started to evaluate the potential use of the leflunomide analogues HMR 715 and HMR 279. These analogues, malononitriloamides, are very similar in structure to the active metabolite of leflunomide, A77 1726, and ma ...
... autoimmune diseases such as rheumatoid arthritis. A large preclinical program has been started to evaluate the potential use of the leflunomide analogues HMR 715 and HMR 279. These analogues, malononitriloamides, are very similar in structure to the active metabolite of leflunomide, A77 1726, and ma ...
Macrocycles in new drug discovery
... pic contribution to affinity has been lost from 4 that must be compensated for, presumably by an entropic gain attributed to macrocyclization. An alternative rationale could be that the protein is less ordered (thus the entropy is increased) when 4 is bound, due to the loss of the ionic interac ti ...
... pic contribution to affinity has been lost from 4 that must be compensated for, presumably by an entropic gain attributed to macrocyclization. An alternative rationale could be that the protein is less ordered (thus the entropy is increased) when 4 is bound, due to the loss of the ionic interac ti ...
The use of cannabis for medical purposes
... treatment option for various medical conditions, mainly where traditional first line drugs have proven ineffective for particular subclasses of patients. The most common conditions include pain and nausea associated with cancer and its treatment, HIV and other wasting diseases, rheumatoid arthritis ...
... treatment option for various medical conditions, mainly where traditional first line drugs have proven ineffective for particular subclasses of patients. The most common conditions include pain and nausea associated with cancer and its treatment, HIV and other wasting diseases, rheumatoid arthritis ...
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... adolescence are highly aggressive in early adulthood (see Melloni & Ricci, 2010). This increase in aggressive responding occurs in the absence of social learning, and as a function of various neuroanatomical changes. For example, adolescent AAS exposure in hamsters increases the density of arginine ...
... adolescence are highly aggressive in early adulthood (see Melloni & Ricci, 2010). This increase in aggressive responding occurs in the absence of social learning, and as a function of various neuroanatomical changes. For example, adolescent AAS exposure in hamsters increases the density of arginine ...
Drug-induced hypo- and hyperprolactinemia: mechanisms, clinical
... control with its own secretion/concentration in the biophase. The inhibition of secretion is triggered by activation of hypothalamic dopamine neurons or directly, by acting on the lactotroph cells [5]. The cholinergic system in the hypophysis, by activation of the muscarinic receptors, exerts a toni ...
... control with its own secretion/concentration in the biophase. The inhibition of secretion is triggered by activation of hypothalamic dopamine neurons or directly, by acting on the lactotroph cells [5]. The cholinergic system in the hypophysis, by activation of the muscarinic receptors, exerts a toni ...
A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine
... 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 and drug-seeking behaviors. However, both MPEP and MTEP have no translational potential for use in humans because of thei ...
... 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 and drug-seeking behaviors. However, both MPEP and MTEP have no translational potential for use in humans because of thei ...
Has an Angel Shown the Way? Etiological and
... has targeted the redox/GSH site.52 Most compounds studied to date have been compounds-of-convenience, which were able to be studied either because they are natural compounds or fortuitously cross-react with NMDAR as a secondary effect. These compounds have been used almost exclusively as add-on trea ...
... has targeted the redox/GSH site.52 Most compounds studied to date have been compounds-of-convenience, which were able to be studied either because they are natural compounds or fortuitously cross-react with NMDAR as a secondary effect. These compounds have been used almost exclusively as add-on trea ...
Functional analyses and molecular modeling of two c-Kit mutations
... modulus of AMBER 7.0 (Case et al., 2000) and the Cornell et al. (1995) force field. The 1.60-Å-resolution coordinates of the kinase domain of KIT in complex with imatinib were obtained from the Brookhaven Protein Data Bank (PDB code 1T46) (Mol et al., 2004), and used as the starting structure. All c ...
... modulus of AMBER 7.0 (Case et al., 2000) and the Cornell et al. (1995) force field. The 1.60-Å-resolution coordinates of the kinase domain of KIT in complex with imatinib were obtained from the Brookhaven Protein Data Bank (PDB code 1T46) (Mol et al., 2004), and used as the starting structure. All c ...
Psilocybin - TU Darmstadt Chemie
... On the other hand, the substance could be directly used as anxiolytic or antidepressant in disorders with very low levels of serotonin in the brain. A number of clinical studies with psilocybin exist, but were performed in the 1960s. Scientific papers found positive effects with low side effects, a ...
... On the other hand, the substance could be directly used as anxiolytic or antidepressant in disorders with very low levels of serotonin in the brain. A number of clinical studies with psilocybin exist, but were performed in the 1960s. Scientific papers found positive effects with low side effects, a ...
Inhibitors of Factor VIIa/Tissue Factor
... contributes significantly to potency in a number of inhibitors.8,16 In contrast, a series of compounds was shown to form a unique network of hydrogen bonds to Ser195 via a hydroxyl group on a non-P1 central ring.17,18 Another P1 substitution reported is the addition of an o-OH on -aminobenzamidine ...
... contributes significantly to potency in a number of inhibitors.8,16 In contrast, a series of compounds was shown to form a unique network of hydrogen bonds to Ser195 via a hydroxyl group on a non-P1 central ring.17,18 Another P1 substitution reported is the addition of an o-OH on -aminobenzamidine ...
3. Results
... neurons (Deutch et al., 1993; Herz, 1997), and the increase of extracellular DA concentrations in the NAcc, are known to be the key function for mediating alcoholinduced reinforcement (Koob, 1992). The first reports that systemic ethanol administration stimulates DA release in the NAcc, appeared in ...
... neurons (Deutch et al., 1993; Herz, 1997), and the increase of extracellular DA concentrations in the NAcc, are known to be the key function for mediating alcoholinduced reinforcement (Koob, 1992). The first reports that systemic ethanol administration stimulates DA release in the NAcc, appeared in ...
Cannabinoid Abuse and Addiction
... Among potential medications that have been tested, the most promising results have been obtained with replacement therapy using CB1 agonist medications. Dronabinol (Marinol) is a synthetic form of THC approved for treatment of nausea associated with chemotherapy and for use as an appetite stimulant ...
... Among potential medications that have been tested, the most promising results have been obtained with replacement therapy using CB1 agonist medications. Dronabinol (Marinol) is a synthetic form of THC approved for treatment of nausea associated with chemotherapy and for use as an appetite stimulant ...
Drug effects on acetic acid-depressed locomotor
... software. Each of the eight chambers consisted of an arena (25.91 × 25.91 × 40.6 cm) surrounded by Plexiglas walls. The floor consisted of a removable plastic drop pan that was cleaned between sessions. A sensor ring surrounded the arena on the bottom outside edges of the four sides of the chamber an ...
... software. Each of the eight chambers consisted of an arena (25.91 × 25.91 × 40.6 cm) surrounded by Plexiglas walls. The floor consisted of a removable plastic drop pan that was cleaned between sessions. A sensor ring surrounded the arena on the bottom outside edges of the four sides of the chamber an ...
Serotonin Syndrome - Available Courses
... function, temperature regulation, mood, sexual function, pain perception and personality. Serotonin also acts peripherally to stimulate smooth muscle. ! Serotonin activity is terminated mainly by reuptake into the presynaptic nerve terminal. Once inside it is either stored or metabolized by MAO and ...
... function, temperature regulation, mood, sexual function, pain perception and personality. Serotonin also acts peripherally to stimulate smooth muscle. ! Serotonin activity is terminated mainly by reuptake into the presynaptic nerve terminal. Once inside it is either stored or metabolized by MAO and ...
ACRIDINE: A VERSATILE HETEROCYCLIC NUCLEUS
... derivatives. The introduction of methyl group at C4 resulted in compounds which showed higher therapeutic efficacy and being developed as anticancer agent for solid tumors (44). ...
... derivatives. The introduction of methyl group at C4 resulted in compounds which showed higher therapeutic efficacy and being developed as anticancer agent for solid tumors (44). ...
