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https://www.readbyqxmd.com/read/28889212/cocaine-like-discriminative-stimulus-effects-of-norepinephrine-preferring-monoamine-releasers-time-course-and-interaction-studies-in-rhesus-monkeys
#1
Stephen J Kohut, David S Jacobs, Richard B Rothman, John S Partilla, Jack Bergman, Bruce E Blough
RATIONALE: The therapeutic potential of monoamine releasers with prominent dopaminergic effects is hindered by their high abuse liability. OBJECTIVES: The present study examined the effects of several novel "norepinephrine (NE)-preferring" monoamine releasers relative to non-selective monoamine releasers, d-amphetamine and d-methamphetamine, in rhesus monkeys trained to discriminate cocaine. NE-preferring releasers were approximately 13-fold more potent for NE compared to dopamine release and ranged in potency for serotonin release (PAL-329 < l-methamphetamine < PAL-169)...
September 9, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28878639/differential-associations-between-cortical-thickness-and-striatal-dopamine-in-treatment-na%C3%A3-ve-adults-with-adhd-vs-healthy-controls
#2
Mariya V Cherkasova, Nazlie Faridi, Kevin F Casey, Kevin Larcher, Gillian A O'Driscoll, Lily Hechtman, Ridha Joober, Glen B Baker, Jennifer Palmer, Alan C Evans, Alain Dagher, Chawki Benkelfat, Marco Leyton
Alterations in catecholamine signaling and cortical morphology have both been implicated in the pathophysiology of attention deficit/hyperactivity disorder (ADHD). However, possible links between the two remain unstudied. Here, we report exploratory analyses of cortical thickness and its relation to striatal dopamine transmission in treatment-naïve adults with ADHD and matched healthy controls. All participants had one magnetic resonance imaging (MRI) and two [(11)C]raclopride positron emission tomography scans...
2017: Frontiers in Human Neuroscience
https://www.readbyqxmd.com/read/28860974/striatal-distribution-and-cytoarchitecture-of-dopamine-receptor-subtype-1-and-2-evidence-from-double-labeling-transgenic-mice
#3
Keke Ren, Baolin Guo, Chunqiu Dai, Han Yao, Tangna Sun, Xia Liu, Zhantao Bai, Wenting Wang, Shengxi Wu
As the main input nucleus of the basal ganglion, the striatum executes different functions, including motivation, reward and attention. The functions of the striatum highly rely on its subregions that receive projections from various cortical areas and the distribution of striatonigral neurons that express D1 dopamine (DA) receptors (or D1 medium-sized spiny neurons, D1 MSNs) and striatopallidal neurons that express D2 DA receptors (or D2 MSNs). Using bacterial artificial chromosome (BAC) transgenic mice, several studies have recently been performed on the spatial distribution of D1 and D2 MSNs...
2017: Frontiers in Neural Circuits
https://www.readbyqxmd.com/read/28855799/review-of-lisdexamfetamine-dimesylate-in-adults-with-attention-deficit-hyperactivity-disorder
#4
REVIEW
Jadwiga Najib, Dexter Wimer, Julie Zeng, Kristina W Lam, Natalya Romanyak, Eva Paige Morgan, Anu Thadavila
Lisdexamfetamine dimesylate (LDX) is the first prodrug stimulant used for the treatment of attention-deficit/hyperactivity disorder (ADHD) dosed once daily. Due to its long-acting properties, LDX remains pharmacologically inactive until an enzymatic process predominantly associated with red blood cells converts it to the active ingredient, d-amphetamine and the amino acid lysine. The efficacy of LDX over placebo has been demonstrated in several studies in adults with moderate to severe ADHD with significant improvements noted in ADHD rating scales, Clinical Global Improvement scores, and assessments of executive function, for all doses of LDX (30-70 mg daily)...
2017: Journal of Central Nervous System Disease
https://www.readbyqxmd.com/read/28828549/postnatal-hypoxia-evokes-persistent-changes-within-the-male-rat-s-dopaminergic-system
#5
Michael J Decker, Karra A Jones, Glenda L Keating, David B Rye
PURPOSE: Hypoxic insults occurring during the perinatal period remain the leading cause of permanent brain impairment. Severe cognitive and motor dysfunction, as seen in cerebral palsy, will occur in 4-10% of post-hypoxic newborns. Subtle cognitive impairment, apparent in disorders of minimal brain dysfunction will occur in > 3 million post-hypoxic newborns. Analyses of post-hypoxic rodent brains reveal reduced extracellular levels of dopamine, a key neurotransmitter of vigilance, execute function, and behavior...
August 22, 2017: Sleep & Breathing, Schlaf & Atmung
https://www.readbyqxmd.com/read/28815279/evaluation-of-training-dose-in-male-sprague-dawley-rats-trained-to-discriminate-4-methylmethcathinone
#6
Michael D Berquist, Nathyn A Thompson, Lisa E Baker
RATIONALE: Although the synthetic cathinone 4-methylmethcathinone (4-MMC, mephedrone) has been a subject of intensive research investigation, the pharmacological mechanisms involved in its interoceptive stimulus effects have yet to be fully characterized. OBJECTIVE: The present study employed drug discrimination methods in rats to compare the interoceptive stimulus properties of two different training doses of 4-MMC to other substances with similar pharmacological actions...
August 16, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28772011/brain-molecular-changes-and-behavioral-alterations-induced-by-propofol-anesthesia-exposure-in-peripubertal-rats
#7
Željko Pavković, Kosara Smiljanić, Selma Kanazir, Desanka Milanović, Vesna Pešić, Sabera Ruždijić
BACKGROUND: Propofol is commonly used in modern anesthesiology. Some findings suggest that it is highly addictive. AIM: In this study it was examined whether propofol anesthesia exposure was able to induce behavioral alterations and brain molecular changes already described in addictive drug usage in peripubertal rats, during the onset of mid/periadolescence as a developmental period with increasing vulnerability to drug addiction. METHODS: The expression of D1 dopamine receptor, a dopamine, and cAMP-regulated phosphoprotein with a Mr 32 000; Ca(2+) /calmodulin-dependent protein kinase IIα; and Finkel-Biskis-Jinkins murine osteosarcoma viral oncogene homolog-B was examined in peripubertal rats 4, 24, and 48 hour after propofol anesthesia exposure by Western blot and immunohistochemistry...
September 2017: Paediatric Anaesthesia
https://www.readbyqxmd.com/read/28762072/sweet-taste-liking-is-associated-with-subjective-response-to-amphetamine-in-women-but-not-men
#8
Jessica Weafer, Nicholas Lyon, Donald Hedeker, Harriet de Wit
RATIONALE AND OBJECTIVE: Preference for sweet taste rewards has been linked to the propensity for drug use in both animals and humans. Here, we tested the association between sweet taste liking and sensitivity to amphetamine reward in healthy adults. We hypothesized that sweet likers would report greater euphoria and stimulation following D-amphetamine (20 mg) compared to sweet dislikers. METHODS: Men (n = 36) and women (n = 34) completed a sweet taste test in which they rated their liking of various concentrations of sucrose and filtered water (0...
July 31, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28728424/annals-express-false-negative-results-in-the-immunoassay-analysis-of-drugs-of-abuse-can-adulterants-be-detected-by-sample-check-test
#9
Barbara Matriciani, Bernd Huppertz, Ruprecht Keller, Ralf Weiskirchen
BACKGROUND: The dilution or adulteration of urine is a serious problem in drugs of abuse (DOA) testing. Tests to identify adulteration are currently available. This study investigated the ability of the CEDIA® sample check to detect adulteration. METHODS: Eight different DOAs were added to a urine sample obtained from a healthy, drug free subject: 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine, 3,4-methylenedioxyamphetamine, benzoylecgonine, D-amphetaminesulfate, ethyl-D-glucuronide, morphine sulfate, oxazepam, (-)-11-nor-9-carboxy-∆(9)-tetrahydrocannabinol...
January 1, 2017: Annals of Clinical Biochemistry
https://www.readbyqxmd.com/read/28716726/early-life-risperidone-enhances-locomotor-responses-to-amphetamine-during-adulthood
#10
Bobbie Lee Stubbeman, Clifford J Brown, Justin R Yates, Mark E Bardgett
Antipsychotic drug prescriptions for pediatric populations have increased over the past 20 years, particularly the use of atypical antipsychotic drugs such as risperidone. Most antipsychotic drugs target forebrain dopamine systems, and early-life antipsychotic drug exposure could conceivably reset forebrain neurotransmitter function in a permanent manner that persists into adulthood. This study determined whether chronic risperidone administration during development modified locomotor responses to the dopamine/norepinephrine agonist, D-amphetamine, in adult rats...
October 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28704276/effects-of-d1-and-d2-receptor-antagonists-on-the-discriminative-stimulus-effects-of-methylendioxypyrovalerone-and-mephedrone-in-male-sprague-dawley-rats-trained-to-discriminate-d-amphetamine
#11
Eric L Harvey, Rachel L Burroughs, Lisa E Baker
Psychopharmacology research has amassed substantial evidence for similarities between synthetic cathinones and other commonly abused psychostimulants. Few studies have utilized drug discrimination methods to investigate synthetic cathinones, and the precise neurochemical substrates underlying their interoceptive effects have not been examined. The present study assessed the involvement of D1 and D2 dopaminergic receptors in the stimulus effects of 3,4-methylenedioxypyrovalerone (MDPV) and mephedrone (MEPH) in rats trained to discriminate D-amphetamine...
October 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28633996/effects-of-monoaminergic-drugs-on-training-induced-motor-cortex-plasticity-in-older-adults
#12
Trisha M Kesar, Samir R Belagaje, Paola Pergami, Marc W Haut, Gerald Hobbs, Cathrin M Buetefisch
Primary motor cortex (M1) plasticity is involved in motor learning and stroke motor recovery, and enhanced by increasing monoaminergic transmission. Age impacts these processes but there is a paucity of systematic studies on the effects of monoaminergic drugs in older adults. Here, in ten older adults (age 61+4years, 4 males), we determine the effects of a single oral dose of carbidopa/levodopa (DOPA), d-amphetamine (AMPH), methylphenidate (MEPH) and placebo (PLAC) on M1 excitability and motor training-induced M1 plasticity...
September 1, 2017: Brain Research
https://www.readbyqxmd.com/read/28623171/broad-analgesic-activity-of-a-novel-selective-m1-agonist
#13
Michael W Wood, Giovanni Martino, Martin Coupal, Mattias Lindberg, Patricia Schroeder, Vijayaratnam Santhakumar, Manon Valiquette, Johan Sandin, Daniel Widzowski, Jennifer Laird
Although the muscarinic receptor family has long been a source of potentially compelling targets for small molecule drug discovery, it was difficult to achieve agonist selectivity within the family. A new class of M1 muscarinic agonists has emerged, and these compounds have been characterized as agonists that activate the receptor at an allosteric site. Members of this class of M1 agonists have been shown to be selective across the muscarinic receptors. However, upon introduction of a novel pharmacologic mechanism, it is prudent to ensure that no new off-target activities have arisen, particularly within the context of in vivo experiments...
June 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28598863/characterization-of-the-discriminative-stimulus-effects-of-3-4-methylenedioxypyrovalerone-in-male-sprague-dawley-rats
#14
Michael D Berquist, Lisa E Baker
Recreational use of 3,4-methylenedioxypyrovalerone (MDPV) in the early 2000s prompted numerous scientific investigations of its behavioral and neurochemical effects. The purpose of this study was to further characterize the interoceptive stimulus effects of MDPV using a validated in-vivo drug-detection assay. Male Sprague-Dawley rats were trained to discriminate 0.3 mg/kg MDPV from saline under a fixed ratio 20 (FR 20) schedule of food reinforcement. After stimulus control was established with MDPV (∼35 training sessions), substitution tests were commenced with drugs from several chemical classes, including drugs with predominantly dopaminergic actions [MDPV, D-amphetamine, (+)-methamphetamine, (-)-cocaine], drugs with predominantly serotonergic actions [(+)-lysergic acid diethylamide, (+)-fenfluramine], and drugs with both serotonergic and dopaminergic actions (3,4-methylenedioxymethamphetamine, 4-methylmethcathinone)...
August 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28588509/behavioral-effects-of-a-novel-benzofuranyl-piperazine-serotonin-2c-receptor-agonist-suggest-a-potential-therapeutic-application-in-the-treatment-of-obsessive-compulsive-disorder
#15
Michelle M Rodriguez, Carl Overshiner, J David Leander, Xia Li, Denise Morrow, Richard G Conway, David L Nelson, Karin Briner, Jeffrey M Witkin
Selective serotonin reuptake inhibitors (SSRIs) are the only effective pharmacological treatments for obsessive-compulsive disorder (OCD). Nonetheless, their generally limited efficacy, side-effects, and delayed onset of action require improved medications for this highly prevalent disorder. Preclinical and clinical findings have suggested serotonin2C (5-HT2C) receptors as a potential drug target. Data in rats and mice are presented here on the effects of a novel 5-HT2C receptor agonist ((3S)-3-Methyl-1-[4-(trifluoromethyl)-7-benzofuranyl]-piperazine) (CPD 1) with high potency and full efficacy at 5-HT2C receptors and less potency and partial agonism at 5-HT2A and 5-HT2B receptors...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28579351/preclinical-abuse-liability-assessment-of-abt-126-an-agonist-at-the-%C3%AE-7-nicotinic-acetylcholine-receptor-nachr
#16
Thomas J Hudzik, Ana M Basso, James J Lynch, William M Bracken, Eric G Mohler, Kathy L Kohlhaas, Hongyu Xu, George Haig, Laura Gault
ABT-126 is a nicotinic acetylcholine receptor (nAChR) agonist that is selective for the α7 subtype of the receptor. nAChRs are thought to play a role in a variety of neurocognitive processes and have been a pharmacologic target for disorders with cognitive impairment, including schizophrenia and Alzheimer's disease. As part of the preclinical safety package for ABT-126, its potential for abuse was assessed. While the involvement of the α4β2 subtype of the nicotinic receptor in the addictive properties of nicotine has been demonstrated, the role of the α7 receptor has been studied much less extensively...
July 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28527692/regional-differences-in-dopamine-receptor-blockade-affect-timing-impulsivity-that-is-altered-by-d-amphetamine-on-differential-reinforcement-of-low-rate-responding-drl-behavior-in-rats
#17
Ruey-Kuang Cheng, Ruey-Ming Liao
The ability to control when to start an action and when to stop is crucial in human and animal behavior. A failure to suppress premature behavior or to carry out an action in a timely manner is commonly seen in several neuropsychological disorders. Despite the phenomenon, the exact neural mechanisms underlying this timing impulsivity remain to be elucidated. Systemic injection of d-amphetamine (AMP) has been shown to disrupt rat's performance in the differential reinforcement of low-rate (DRL) task that requires both optimal timing and proper impulsive control as measured by peak time and non-reinforced responses, respectively...
July 28, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28487656/adolescent-female-cannabinoid-exposure-diminishes-the-reward-facilitating-effects-of-%C3%AE-9-tetrahydrocannabinol-and-d-amphetamine-in-the-adult-male-offspring
#18
George Pitsilis, Dimitrios Spyridakos, George G Nomikos, George Panagis
Marijuana is currently the most commonly abused illicit drug. According to recent studies, cannabinoid use occurring prior to pregnancy can impact brain plasticity and behavior in future generations. The purpose of the present study was to determine whether adolescent exposure of female rats to Δ(9)-tetrahydrocannabinol (Δ(9)-THC) induces transgenerational effects on the reward-facilitating effects of Δ(9)-THC and d-amphetamine in their adult male offspring. Female Sprague-Dawley rats received Δ(9)-THC (0...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28450187/nitrosoamphetamine-binding-to-myoglobin-and-hemoglobin-crystal-structure-of-the-h64a-myoglobin-nitrosoamphetamine-adduct
#19
Bing Wang, Samantha M Powell, Ye Guan, Nan Xu, Leonard M Thomas, George B Richter-Addo
N-hydroxyamphetamine (AmphNHOH) is an oxidative metabolite of amphetamine and methamphetamine. It is known to form inhibitory complexes upon binding to heme proteins. However, its interactions with myoglobin (Mb) and hemoglobin (Hb) have not been reported. We demonstrate that the reactions of AmphNHOH with ferric Mb and Hb generate the respective heme-nitrosoamphetamine derivatives characterized by UV-vis spectroscopy. We have determined the X-ray crystal structure of the H64A Mb-nitrosoamphetamine complex to 1...
July 1, 2017: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/28396142/atypical-binding-at-dopamine-and-serotonin-transporters-contribute-to-the-discriminative-stimulus-effects-of-mephedrone
#20
Alyssa F DeLarge, Laura L Erwin, Peter J Winsauer
Mephedrone (4-methylmethcathinone), a constituent of the recreational substances known as "bath salts", is a synthetic cathinone that can produce auditory and visual hallucinations, as well as problematic cardiovascular effects. This study compared the discriminative stimulus effects of mephedrone (0.32-10 mg/kg) with other prototypical drugs of abuse: cocaine (0.56-32 mg/kg), d-amphetamine (0.18-3.2 mg/kg), ketamine (1.8-18 mg/kg), phencyclidine (PCP, 1-5.6 mg/kg), heroin (1-10 mg/kg), 2,5-dimethoxy-4-iodoamphetamine (R-DOI, 0...
June 2017: Neuropharmacology
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