GPCR ontology: development and application of a G protein
... Motivation: Novel tools need to be developed to help scientists analyze large amounts of available screening data with the goal to identify entry points for the development of novel chemical probes and drugs. As the largest class of drug targets, G protein-coupled receptors (GPCRs) remain of particu ...
... Motivation: Novel tools need to be developed to help scientists analyze large amounts of available screening data with the goal to identify entry points for the development of novel chemical probes and drugs. As the largest class of drug targets, G protein-coupled receptors (GPCRs) remain of particu ...
Serotonergic Modulation of Rat Pineal Gland Activity: In Vivo
... receptor now available, but not by pretreatment with ketanserin, an antagonist with higher affinity for 5-HT2A than for 5-HT2C receptor. These results suggest that 5-HT2C receptors are likely involved in the mediation of the serotonergic modulation of pineal biosynthetic activity in rats. ...
... receptor now available, but not by pretreatment with ketanserin, an antagonist with higher affinity for 5-HT2A than for 5-HT2C receptor. These results suggest that 5-HT2C receptors are likely involved in the mediation of the serotonergic modulation of pineal biosynthetic activity in rats. ...
New pharmacological technologies in the clinical management of
... A compound that has an affinity for & stimulates physiological activity at the same cell receptors as opioid agonists but that produces only a partial (i.e., submaximal) bodily response. ...
... A compound that has an affinity for & stimulates physiological activity at the same cell receptors as opioid agonists but that produces only a partial (i.e., submaximal) bodily response. ...
2002
... the absence and presence of 10M naloxone. The potency of the drugs in displacing the specific binding of the 3Hligand is determined from data using Graphpad Prism (GraphPAD, San Diego, CA) and converted to Ki values by the method of Cheng and Prussoff (1973). Opioid binding is performed in membrane ...
... the absence and presence of 10M naloxone. The potency of the drugs in displacing the specific binding of the 3Hligand is determined from data using Graphpad Prism (GraphPAD, San Diego, CA) and converted to Ki values by the method of Cheng and Prussoff (1973). Opioid binding is performed in membrane ...
G protein-coupled receptor dimers: Functional
... Several groups demonstrated that the GABABR1 subtype was poorly expressed at the cell surface in heterologous systems with little signalling activity, but coexpression with a second subtype (GABABR2) resulted in a fully functional heterodimer that was expressed at the ...
... Several groups demonstrated that the GABABR1 subtype was poorly expressed at the cell surface in heterologous systems with little signalling activity, but coexpression with a second subtype (GABABR2) resulted in a fully functional heterodimer that was expressed at the ...
Cannabidiol as a Potential Treatment for Anxiety Disorders
... γ-aminobutryic acid-ergic and glutamatergic neurons. eCBs are fatty acid derivatives that are synthesized on demand in response to neuronal depolarization and Ca2+ influx, via cleavage of membrane phospholipids. The primary mechanism by which eCBs regulate synaptic function is retrograde signaling, ...
... γ-aminobutryic acid-ergic and glutamatergic neurons. eCBs are fatty acid derivatives that are synthesized on demand in response to neuronal depolarization and Ca2+ influx, via cleavage of membrane phospholipids. The primary mechanism by which eCBs regulate synaptic function is retrograde signaling, ...
The use of cannabinoids in animals and therapeutic implications for
... their psychoactive effects and addictive potential. Attempts by pharmaceutical companies in the sixth decade of the twentieth century to produce cannabinoids with pharmacological effects and without psychotropic activity were not successful (Fisar 2009; Pertwee 2009), although cannabinoids with very ...
... their psychoactive effects and addictive potential. Attempts by pharmaceutical companies in the sixth decade of the twentieth century to produce cannabinoids with pharmacological effects and without psychotropic activity were not successful (Fisar 2009; Pertwee 2009), although cannabinoids with very ...
Block of Delayed-Rectifier Potassium Channels by Reduced
... NaOH). In certain experiments, equimolar KCl or RbCl was used to replace NaCl, and pH was adjusted by adding KOH or RbOH, respectively. The intracellular solution contained 150 mM KCl, 10 mM HEPES, 1 mM MgCl2, 5 mM Na2ATP, and 5 mM EGTA, with pH adjusted to 7.2 (by KOH). Na2ATP (5 mM) and EGTA (5 mM ...
... NaOH). In certain experiments, equimolar KCl or RbCl was used to replace NaCl, and pH was adjusted by adding KOH or RbOH, respectively. The intracellular solution contained 150 mM KCl, 10 mM HEPES, 1 mM MgCl2, 5 mM Na2ATP, and 5 mM EGTA, with pH adjusted to 7.2 (by KOH). Na2ATP (5 mM) and EGTA (5 mM ...
Ignatowska-Jankowska et al, 2014
... pain. Through their stimulation of CB1 receptors, they inhibit pain transmission at central, spinal and peripheral synapses and may serve an auto protective role (Walker et al, 1999). While preclinical data indicate that Δ9-tetrahydrocannabinol (THC), the primary psychoactive constituent of Cannabis ...
... pain. Through their stimulation of CB1 receptors, they inhibit pain transmission at central, spinal and peripheral synapses and may serve an auto protective role (Walker et al, 1999). While preclinical data indicate that Δ9-tetrahydrocannabinol (THC), the primary psychoactive constituent of Cannabis ...
Allosteric Binding Sites on Muscarinic Acetylcholine Receptors
... existence of a second allosteric site on the M2 mAChR and provide data suggesting that two molecules of an allosteric agent and one orthosteric ligand may be able to bind to the M2 mAChR simultaneously (Fig. 1). The authors based their conclusions on analysis of the interactions of tacrine and Duo3 ...
... existence of a second allosteric site on the M2 mAChR and provide data suggesting that two molecules of an allosteric agent and one orthosteric ligand may be able to bind to the M2 mAChR simultaneously (Fig. 1). The authors based their conclusions on analysis of the interactions of tacrine and Duo3 ...
Morphine HO- Group is needed for activity HO
... Dihydromorphine is slightly stronger than morphine as an analgesic with a nearly identical sideeffect profile, and is a somewhat more active euphoriant -- therefore making it theoretically a bit superior in alleviating suffering -- and perhaps in a way subjectively closer to that of morphine than hy ...
... Dihydromorphine is slightly stronger than morphine as an analgesic with a nearly identical sideeffect profile, and is a somewhat more active euphoriant -- therefore making it theoretically a bit superior in alleviating suffering -- and perhaps in a way subjectively closer to that of morphine than hy ...
An Introduction to Medicinal Chemistry
... The answers we would get would almost certainly depend on who we were to ask. As far as the law is concerned, the dividing line is defined in black and white. As far as the party-going teenager is concerned, the law is an ass. As far as we are concerned, the questions are irrelevant. To try and divi ...
... The answers we would get would almost certainly depend on who we were to ask. As far as the law is concerned, the dividing line is defined in black and white. As far as the party-going teenager is concerned, the law is an ass. As far as we are concerned, the questions are irrelevant. To try and divi ...
Bioisosterism: A Rational Approach in Drug Design
... The ability of a group of bioisosteres to elicit similar biological activity has been attributed to common physicochemical properties. In this review an attempt has been made to quantitate, in specific instances, physicochemical effects such as electronegativity, steric size, and lipophilicity and t ...
... The ability of a group of bioisosteres to elicit similar biological activity has been attributed to common physicochemical properties. In this review an attempt has been made to quantitate, in specific instances, physicochemical effects such as electronegativity, steric size, and lipophilicity and t ...
DESIGNING OF POTENTIAL NEW ESTROGEN ANTAGONISTS FOR TREATMENT OF
... It has become a chronic disease nowadays and it can be controlled by estrogen antagonist as estrogen antagonist inhibits the action of estrogen and proliferation of endometrial cell is stopped [6, 13, 18]. The discovery of the first design of Estrogen antagonist drug has inspired a number of continu ...
... It has become a chronic disease nowadays and it can be controlled by estrogen antagonist as estrogen antagonist inhibits the action of estrogen and proliferation of endometrial cell is stopped [6, 13, 18]. The discovery of the first design of Estrogen antagonist drug has inspired a number of continu ...
Invited Review - International Journal of Pharmaceutical Science
... compounds tested [11] showed the most favorable antimicrobial activity. Shiradkar et al [21] reported a series of N-{4-[(4-amino-5sulphanyl-4H-1, 2, 4-triazol-3-yl) methyl]-1, 3-thiazol-2-yl}2-substituted amide derivatives. The compounds were tested for their preliminary in vitro antibacterial activ ...
... compounds tested [11] showed the most favorable antimicrobial activity. Shiradkar et al [21] reported a series of N-{4-[(4-amino-5sulphanyl-4H-1, 2, 4-triazol-3-yl) methyl]-1, 3-thiazol-2-yl}2-substituted amide derivatives. The compounds were tested for their preliminary in vitro antibacterial activ ...
Toxicant – Receptor Interactions: Fundamental - UNC
... more than a century ago, receptor theory remains a critical concept in toxicology and in many other branches of biology. In one sense, receptors may be considered as macromolecules that bind small molecules (commonly termed ligands) with high affinity and thereby initiate a characteristic biochemica ...
... more than a century ago, receptor theory remains a critical concept in toxicology and in many other branches of biology. In one sense, receptors may be considered as macromolecules that bind small molecules (commonly termed ligands) with high affinity and thereby initiate a characteristic biochemica ...
Scotopic vision in the monkey is modulated by the G protein
... (Bouskila et al., 2013b). A variety of anatomical and functional visual effects of cannabinoids have also been reported for every retinal cell type in both rodents and fish (Yazulla, 2008; Cécyre et al., 2013). However, these studies did not investigate GPR55 because of its recent and controversial ...
... (Bouskila et al., 2013b). A variety of anatomical and functional visual effects of cannabinoids have also been reported for every retinal cell type in both rodents and fish (Yazulla, 2008; Cécyre et al., 2013). However, these studies did not investigate GPR55 because of its recent and controversial ...
the PDF
... administration of doses up to 600 mg resulted in local plasma levels of 5–20 ng/g. In comparison, oral racemic baclofen at the very high dose of 100 mg gave concentrations of <3 ng/g in CSF. An additional benefit was a major reduction in the unwanted side effects with high doses required for systemi ...
... administration of doses up to 600 mg resulted in local plasma levels of 5–20 ng/g. In comparison, oral racemic baclofen at the very high dose of 100 mg gave concentrations of <3 ng/g in CSF. An additional benefit was a major reduction in the unwanted side effects with high doses required for systemi ...
Gaba - American College of Neuropsychopharmacology
... grouped in the superfamily of ligand-gated ion channel receptors, which includes the well-characterized nicotinic acetylcholine receptor, present at the skeletal neuromuscular junction (13,14). Chloride channel gating is generally inhibitory on a neuron by virtue of stabilizing the membrane potentia ...
... grouped in the superfamily of ligand-gated ion channel receptors, which includes the well-characterized nicotinic acetylcholine receptor, present at the skeletal neuromuscular junction (13,14). Chloride channel gating is generally inhibitory on a neuron by virtue of stabilizing the membrane potentia ...
Adverse Reactions to Fluoroquinolones. An Overview on
... toxicity of fluoroquinolones, including the newer derivatives such levofloxacin, sparfloxacin, graepafloxacin and the 7-azabicyclo derivatives, trovafloxacin and moxifloxacin. A special attention is given to new data on mechanistic aspects, particularly those regarding CNS effects. In recent years e ...
... toxicity of fluoroquinolones, including the newer derivatives such levofloxacin, sparfloxacin, graepafloxacin and the 7-azabicyclo derivatives, trovafloxacin and moxifloxacin. A special attention is given to new data on mechanistic aspects, particularly those regarding CNS effects. In recent years e ...
nausea and vomiting - KSU Faculty Member websites
... as well as afferent from the higher cortical center (including the visual center and the vestibular portion of the eight cranial nerve) and the chemoreceptor trigger zone (CTZ) in the area postrema. (Watcha and White, 1992). The gastrointestinal tract is directly connected to the emetic center via n ...
... as well as afferent from the higher cortical center (including the visual center and the vestibular portion of the eight cranial nerve) and the chemoreceptor trigger zone (CTZ) in the area postrema. (Watcha and White, 1992). The gastrointestinal tract is directly connected to the emetic center via n ...
Kinetics of metoclopramide effects on human 5
... expression vector pCDNA3 (Invitrogen) under control of human cytomegalovirus promoter. Cell culture was performed according b [1,5]. The condition for patch clamp experiments on excised outside out patches was identical to those performed in [1,5]. Two solution application systems were employed: (a) ...
... expression vector pCDNA3 (Invitrogen) under control of human cytomegalovirus promoter. Cell culture was performed according b [1,5]. The condition for patch clamp experiments on excised outside out patches was identical to those performed in [1,5]. Two solution application systems were employed: (a) ...
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.