Synaptic-Type a1b2g2L GABA A Receptors Produce Large
... fast-rising large inward currents that desensitized to 14 6 1% (mean 6 S.E.M.; 14 cells) of the peak response by the end of a 2-minute drug application. Exposure of same set of cells to 0.5 mM GABA elicited a peak response that was 3 6 1% and a steady-state current that was 1 6 1% of the peak respon ...
... fast-rising large inward currents that desensitized to 14 6 1% (mean 6 S.E.M.; 14 cells) of the peak response by the end of a 2-minute drug application. Exposure of same set of cells to 0.5 mM GABA elicited a peak response that was 3 6 1% and a steady-state current that was 1 6 1% of the peak respon ...
CURRICULUM VITAE
... Recent discovery of an allosteric binding site on the cannabinoid CB1 receptor invites new approaches to potential drugs that modulate cannabinoid signaling for therapeutic benefit. Several GPCRs have been shown to contain allosteric binding sites for endogenous/synthetic ligands which are discrete ...
... Recent discovery of an allosteric binding site on the cannabinoid CB1 receptor invites new approaches to potential drugs that modulate cannabinoid signaling for therapeutic benefit. Several GPCRs have been shown to contain allosteric binding sites for endogenous/synthetic ligands which are discrete ...
Protein Kinase C Mediates the Synergistic Interaction Between
... between intrathecally administered ␣2AR and opioid agonists is well documented, but the mechanism underlying this synergy remains unclear. The delta-opioid receptor (DOP) and the ␣2AARs are coexpressed on the terminals of primary afferent fibers in the spinal cord where they may mediate this phenome ...
... between intrathecally administered ␣2AR and opioid agonists is well documented, but the mechanism underlying this synergy remains unclear. The delta-opioid receptor (DOP) and the ␣2AARs are coexpressed on the terminals of primary afferent fibers in the spinal cord where they may mediate this phenome ...
Treatment of opioid-induced gut dysfunction
... peptides and opioid receptors in the gastrointestinal tract The adverse influence of opioid analgesics on GI function remained an enigma to scientists until it was realised that both opioid peptides and opioid receptors are expressed in the digestive tract; therefore, it is important to briefly cons ...
... peptides and opioid receptors in the gastrointestinal tract The adverse influence of opioid analgesics on GI function remained an enigma to scientists until it was realised that both opioid peptides and opioid receptors are expressed in the digestive tract; therefore, it is important to briefly cons ...
Discriminative Stimulus Properties of Cocaine
... and Cunningham, 1997). These initial studies demonstrated clearly that monoamine reuptake inhibitors such as fluoxetine and desipramine enhance the DS effects of cocaine, but the relative importance of NE and 5-HT to the DS effects of cocaine has not been firmly established in the rat. Inasmuch as c ...
... and Cunningham, 1997). These initial studies demonstrated clearly that monoamine reuptake inhibitors such as fluoxetine and desipramine enhance the DS effects of cocaine, but the relative importance of NE and 5-HT to the DS effects of cocaine has not been firmly established in the rat. Inasmuch as c ...
6 points each
... “Olanzapine’s antagonism of muscarinic M1-5 receptors may explain its anticholinergic effects.” Anticholinergic effects cause dry mouth among other symptoms. Thus, relatively decreased affinity for M1-5 receptors may decrease dry mouth. The dry mouth is probably caused by blockade of peripheral M3 r ...
... “Olanzapine’s antagonism of muscarinic M1-5 receptors may explain its anticholinergic effects.” Anticholinergic effects cause dry mouth among other symptoms. Thus, relatively decreased affinity for M1-5 receptors may decrease dry mouth. The dry mouth is probably caused by blockade of peripheral M3 r ...
Cannabidiol as a Potential Treatment for Anxiety Disorders
... agents for enhancing CB1R activation include THC, which is a potent and direct agonist; synthetic CB1R agonists; FAAH inhibitors and other agents that increase eCB availability, as well as nonpsychoactive cannabis phytocannabinoids, including CBD. While CBD has low affinity for the CB1R, it function ...
... agents for enhancing CB1R activation include THC, which is a potent and direct agonist; synthetic CB1R agonists; FAAH inhibitors and other agents that increase eCB availability, as well as nonpsychoactive cannabis phytocannabinoids, including CBD. While CBD has low affinity for the CB1R, it function ...
Histamine in Atopic Disorders: Atopic Dermatitis and
... in decreased quality of life. At present, the responsible mechanisms that are involved in inflammation and pruritus in these disorders and how they lead to pathogenesis are not completely understood. A major mediator of inflammation and allergic reactions is histamine, which plays an important role ...
... in decreased quality of life. At present, the responsible mechanisms that are involved in inflammation and pruritus in these disorders and how they lead to pathogenesis are not completely understood. A major mediator of inflammation and allergic reactions is histamine, which plays an important role ...
Opioid Tolerance and Dependence in Infants and Children
... of opioids for analgesia or sedation does not result in psychological dependence or addiction. Epidemiology: There are several clinical reports that indicate that the incidence of iatrogenic induced opioid withdrawal approaches 60% (1-3) Cellular and Molecular Mechanisms: Opioids act by binding to o ...
... of opioids for analgesia or sedation does not result in psychological dependence or addiction. Epidemiology: There are several clinical reports that indicate that the incidence of iatrogenic induced opioid withdrawal approaches 60% (1-3) Cellular and Molecular Mechanisms: Opioids act by binding to o ...
The hallucinogenic world of tryptamines: an updated review
... they are intentionally marketed as replacements for illegal drugs, being sold legally in certain countries under names such as ‘research chemicals’, ‘legal highs’ or ‘designer drugs’ (Arunotayanun and Gibbons 2012; Kjellgren and Soussan 2011; Musselman and Hampton 2014). These new psychoactive subst ...
... they are intentionally marketed as replacements for illegal drugs, being sold legally in certain countries under names such as ‘research chemicals’, ‘legal highs’ or ‘designer drugs’ (Arunotayanun and Gibbons 2012; Kjellgren and Soussan 2011; Musselman and Hampton 2014). These new psychoactive subst ...
Update on Serotonin - Mayo Medical Laboratories
... doses to achieve optimal response while avoiding toxicity. Patients who are ultrarapid metabolizers may benefit from increased doses or conversion to other drugs that are not primarily metabolized by CYP2D6. A complicating factor in correlating CYP2D6 genotype with phenotype is that many drugs (or t ...
... doses to achieve optimal response while avoiding toxicity. Patients who are ultrarapid metabolizers may benefit from increased doses or conversion to other drugs that are not primarily metabolized by CYP2D6. A complicating factor in correlating CYP2D6 genotype with phenotype is that many drugs (or t ...
Dopaminergic Pathways and their
... Dopamine was originally considered a precursor but by the 1950s was recognized to be pharmacologically active in its own right (for review: Blaschko, 1973). Dopamine is now accepted as a neurotransmitter in several pathways in the central nervous system and may have functional roles outside the nerv ...
... Dopamine was originally considered a precursor but by the 1950s was recognized to be pharmacologically active in its own right (for review: Blaschko, 1973). Dopamine is now accepted as a neurotransmitter in several pathways in the central nervous system and may have functional roles outside the nerv ...
Determination and Characterization of a Cannabinoid Receptor in
... by a G protein. The binding was also sensitive to MgCI2 and CaCI2. Binding of [3H]CP-55,940 was displaced by cannabinoid drugs in the following order of potency: CP-55,940 ...
... by a G protein. The binding was also sensitive to MgCI2 and CaCI2. Binding of [3H]CP-55,940 was displaced by cannabinoid drugs in the following order of potency: CP-55,940 ...
Dose-Response Study of N,N-Dimethyltryptamine in Humans
... Above threshold doses, they reliably elicit a unique constellation of perceptual, emotional, cognitive, interoceptive, and volitional effects, in a usually clear sensorium [1]. Although other drugs might cause similar symptoms (eg, subanesthetic doses of the dissociative anesthetics ketamine hydroch ...
... Above threshold doses, they reliably elicit a unique constellation of perceptual, emotional, cognitive, interoceptive, and volitional effects, in a usually clear sensorium [1]. Although other drugs might cause similar symptoms (eg, subanesthetic doses of the dissociative anesthetics ketamine hydroch ...
Assessment of the Influence of Histaminergic Actions on Cocaine
... the locomotor stimulant effects of cocaine. In addition, a second generation of compounds was synthesized that had reduced muscarinic affinity (Agoston et al., 1997). These compounds also possessed a reduced cocaine-like spectrum of behavioral effects (Katz et al., 2004), suggesting that the antimus ...
... the locomotor stimulant effects of cocaine. In addition, a second generation of compounds was synthesized that had reduced muscarinic affinity (Agoston et al., 1997). These compounds also possessed a reduced cocaine-like spectrum of behavioral effects (Katz et al., 2004), suggesting that the antimus ...
IDrugs The Investigational Drugs Journal
... chemists. There were more than 200 attendees at the symposium. ...
... chemists. There were more than 200 attendees at the symposium. ...
mechanism of action of antidepressants and mood stabilizers
... preceded the improvement in mood symptoms, indicating a temporal dissociation between changes in myo-inositol and clinical improvement. Consequently, these and other studies suggest that although inhibition of IMPase may represent an initial effect of lithium, reducing myo-inositol levels per se may ...
... preceded the improvement in mood symptoms, indicating a temporal dissociation between changes in myo-inositol and clinical improvement. Consequently, these and other studies suggest that although inhibition of IMPase may represent an initial effect of lithium, reducing myo-inositol levels per se may ...
Dopamine Hypothesis of Mania
... precursor in synthesis of the cat-echolamine neurotransmitters noradrenaline (norepinephrine) and adrenaline (epinephrine). In 1957 it was shown to be present in the brain with other catecholamines (1). In 1958, Carlsson discovered the function of dopamine a neurotransmitter (2), while studying the ...
... precursor in synthesis of the cat-echolamine neurotransmitters noradrenaline (norepinephrine) and adrenaline (epinephrine). In 1957 it was shown to be present in the brain with other catecholamines (1). In 1958, Carlsson discovered the function of dopamine a neurotransmitter (2), while studying the ...
PDF - National Alliance for Medication Assisted Recovery
... substance from binding to it. For example, narcotic antagonists such as naloxone or its' predecessor Naline are administered to reverse a heroin or opioid overdose. This is achieved because opioid antagonists have a greater affinity for the opiate receptor than agonists and in fact the affinity is s ...
... substance from binding to it. For example, narcotic antagonists such as naloxone or its' predecessor Naline are administered to reverse a heroin or opioid overdose. This is achieved because opioid antagonists have a greater affinity for the opiate receptor than agonists and in fact the affinity is s ...
... This study demonstrates that the TP receptor antagonist, BAY u 3405, produces only partial protection against PGD2-induced airway narrowing at 90 min after ingestion. The magnitude of protection was similar when 20, 50 or 100 mg doses were used, despite increasing plasma concentrations of BAY u 3405 ...
The Magic Mint - Stephanie Nichole Halbleib
... • Three opioid receptors, mu, delta and kappa • Activated endogenous by peptides (like endorphins), or exogenously by alkaloid opiates (such as morphine) • Signal transduction is theorized as follows: – Activation is coupled to the G protein which increases phosphodiesterase activity – Breaks down c ...
... • Three opioid receptors, mu, delta and kappa • Activated endogenous by peptides (like endorphins), or exogenously by alkaloid opiates (such as morphine) • Signal transduction is theorized as follows: – Activation is coupled to the G protein which increases phosphodiesterase activity – Breaks down c ...