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https://www.readbyqxmd.com/read/27812593/a-new-synthesis-and-preliminary-evaluation-of-some-analogues-of-mecamylamine-a-compound-with-anti-addiction-properties
#1
David Mangan, Neasa McNabola, Emily H Clark, Isabel Bermudez, Susan Wonnacott, J Mike Southern
A new synthesis of mecamylamine - a known anti-hypertensive drug with anti-addictive properties is described. The new route allowed access to two novel analogues whose activity at two nicotinic acetylcholine receptor subtypes was assessed.
November 4, 2016: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/27734823/-ibogaine-structure-influence-on-human-body-clinical-relevance
#2
Zygmunt Zdrojewicz, Bartłomiej Kuszczak, Natalia Olszak
Ibogaine is a natural chemical compound, which belongs to the indole alkaloid family. It can be naturally found within the root bark of african plant Tabernanthe iboga. Ibogaine plays a significant role among tribal cultures. Ibogaine, in small amount, causes reduction of hunger, thirst and exhaustion. In bigger amount, however, it can cause intensive visions. Other effects include reduction or complete disappearance of absitnence symptoms visible in people addicted to the nicotine, alcohol, methamphetamine, cocaine or opioids, what has been scientifically proven after the tests on animals and small groups of people...
July 29, 2016: Polski Merkuriusz Lekarski: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/27678551/choice-between-delayed-food-and-immediate-oxycodone-in-rats
#3
Maria E Secci, Julie A Factor, Charles W Schindler, Leigh V Panlilio
RATIONALE: The choice to seek immediate drug effects instead of more meaningful but delayed rewards is a defining feature of addiction. OBJECTIVES: To develop a rodent model of this behavior, we allowed rats to choose between immediate intravenous delivery of the prescription opioid oxycodone (50 μg/kg) and delayed delivery of palatable food pellets. RESULTS: Rats preferred food at delays up to 30 s, but they chose oxycodone and food equally at 60-s delay and preferred oxycodone over food at 120-s delay...
December 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27617300/coupling-neurogenetics-gars%C3%A2-and-a-nutrigenomic-based-dopaminergic-agonist-to-treat-reward-deficiency-syndrome-rds-targeting-polymorphic-reward-genes-for-carbohydrate-addiction-algorithms
#4
Kenneth Blum, Thomas Simpatico, Rajendra D Badgaiyan, Zsolt Demetrovics, James Fratantonio, Gozde Agan, Marcelo Febo, Mark S Gold
Earlier work from our laboratory, showing anti-addiction activity of a nutraceutical consisting of amino-acid precursors and enkephalinase inhibition properties and our discovery of the first polymorphic gene (Dopamine D2 Receptor Gene [DRD2]) to associate with severe alcoholism serves as a blue-print for the development of "Personalized Medicine" in addiction. Prior to the later genetic finding, we developed the concept of Brain Reward Cascade, which continues to act as an important component for stratification of addiction risk through neurogenetics...
2015: Journal of Reward Deficiency Syndrome
https://www.readbyqxmd.com/read/27448833/quantification-of-anti-addictive-alkaloids-ibogaine-and-voacangine-in-in-vivo-and-in-vitro-grown-plants-of-two-mexican-tabernaemontana-species
#5
Felix Krengel, Josefina Herrera Santoyo, Teresa de Jesús Olivera Flores, Víctor M Chávez Ávila, Francisco J Pérez Flores, Ricardo Reyes Chilpa
Tabernaemontana alba and Tabernaemontana arborea are Apocynaceae species used in Mexican traditional medicine for which little phytochemical information exists. In this study, preliminary gas chromatography/mass spectrometry analyses of different organs obtained from wild plants of both species identified a total of 10 monoterpenoid indole alkaloids (MIAs) and one simple indole alkaloid, nine of which were reported for the first time in these species. Furthermore, callus cultures were established from T. alba leaf explants and regeneration of whole plants was accomplished via somatic embryogenesis...
July 23, 2016: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/27279696/effect-of-withinia-somnifera-and-shilajit-on-alcohol-addiction-in-mice
#6
Priya Bansal, Sugato Banerjee
BACKGROUND: Alcohol addiction is a social problem leading to both loss of health and economic prosperity among addicted individuals. Common properties of anti-addictive compounds include anti-anxiety, anticonvulsants, anti-depressant, and nootropic actions primarily through modulation of gamma-aminobutyric acid (GABA) and serotonergic systems. OBJECTIVE: Here, we screen ashwagandha and shilajit known ethnopharmacologically as nervine tonic and adaptogenic herbs for possible anti-addictive potential...
May 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27259232/characterization-and-use-of-hapt1-derived-homologous-tumors-as-a-preclinical-model-to-evaluate-therapeutic-efficacy-of-drugs-against-pancreatic-tumor-desmoplasia
#7
Sujit Suklabaidya, Biswajit Das, Syed Azmal Ali, Sumeet Jain, Sharada Swaminathan, Ashok K Mohanty, Susen K Panda, Pujarini Dash, Subhankar Chakraborty, Surinder K Batra, Shantibhusan Senapati
Desmoplasia in human pancreatic cancer (PC) promotes cancer progression and hinders effective drug delivery. The objectives of this study were to characterize a homologous orthotopic model of PC in Syrian golden hamster and investigate the effect of anti-fibrotic (pirfenidone), antioxidant (N-acetyl cysteine, NAC) and anti-addiction (disulfiram, DSF) drugs on desmoplasia and tumor growth in this model. The HapT1 PC cells when implanted orthotopically into hamsters formed tumors with morphological, cellular and molecular similarities to human PC...
July 5, 2016: Oncotarget
https://www.readbyqxmd.com/read/27230395/effects-of-ayahuasca-and-its-alkaloids-on-drug-dependence-a-systematic-literature-review-of-quantitative-studies-in-animals-and-humans
#8
Amanda A Nunes, Rafael G Dos Santos, Flávia L Osório, Rafael F Sanches, José Alexandre S Crippa, Jaime E C Hallak
Recently, the anti-addictive potential of ayahuasca, a dimethyltryptamine(DMT)- and β-carboline-rich hallucinogenic beverage traditionally used by indigenous groups of the Northwest Amazon and currently by syncretic churches worldwide, has received increased attention. To better evaluate this topic, we performed a systematic literature review using the PubMed database to find quantitative studies (using statistical analysis) that assessed the effects of ayahuasca or its components in drug-related symptoms or disorders...
July 2016: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/27223864/reactivity-to-addictive-drugs-in-the-methylazoxymethanol-mam-model-of-schizophrenia-in-male-and-female-rats
#9
Jana Ruda-Kucerova, Zuzana Babinska, Petra Amchova, Tibor Stark, Filippo Drago, Alexandra Sulcova, Vincenzo Micale
OBJECTIVES: Patients with schizophrenia suffer comorbid substance abuse regardless of gender. However, the vast majority of studies are only conducted in male subjects. Therefore, the aim of these experiments is to assess addictive behaviors of both sexes in a neurodevelopmental model of schizophrenia induced by prenatal methylazoxymethanol acetate (MAM) exposure. METHODS: MAM was administered intraperitoneally (22 mg/kg on gestational day 17). Two studies were performed in the offspring: (1) alcohol drinking procedure to assess daily intake of 20% alcohol and relapse-like behavior after a period of forced abstinence...
May 25, 2016: World Journal of Biological Psychiatry
https://www.readbyqxmd.com/read/27137199/the-effects-of-intranasal-oxytocin-in-opioid-dependent-individuals-and-healthy-control-subjects-a-pilot-study
#10
Josh D Woolley, Peter A Arcuni, Christopher S Stauffer, Daniel Fulford, Dean S Carson, Steve Batki, Sophia Vinogradov
RATIONALE: There has been an explosion of research on the potential benefits of the social neuropeptide oxytocin for a number of mental disorders including substance use disorders. Recent evidence suggests that intranasal oxytocin has both direct anti-addiction effects and pro-social effects that may facilitate engagement in psychosocial treatment for substance use disorders. OBJECTIVES: We aimed to assess the tolerability of intranasal oxytocin and its effects on heroin craving, implicit association with heroin and social perceptual ability in opioid-dependent patients receiving opioid replacement therapy (ORT) and healthy control participants...
July 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27020671/anti-addiction-drug-ibogaine-prolongs-the-action-potential-in-human-induced-pluripotent-stem-cell-derived-cardiomyocytes
#11
Lena Rubi, Daniel Eckert, Stefan Boehm, Karlheinz Hilber, Xaver Koenig
Ibogaine is a plant alkaloid used as anti-addiction drug in dozens of alternative medicine clinics worldwide. Recently, alarming reports of life-threatening cardiac arrhythmias and cases of sudden death associated with the ingestion of ibogaine have accumulated. Using whole-cell patch clamp recordings, we assessed the effects of ibogaine and its main metabolite noribogaine on action potentials in human ventricular-like cardiomyocytes derived from induced pluripotent stem cells. Therapeutic concentrations of ibogaine and its long-lived active metabolite noribogaine significantly retarded action potential repolarization in human cardiomyocytes...
March 28, 2016: Cardiovascular Toxicology
https://www.readbyqxmd.com/read/26807959/how-toxic-is-ibogaine
#12
REVIEW
Ruud P W Litjens, Tibor M Brunt
CONTEXT: Ibogaine is a psychoactive indole alkaloid found in the African rainforest shrub Tabernanthe Iboga. It is unlicensed but used in the treatment of drug and alcohol addiction. However, reports of ibogaine's toxicity are cause for concern. OBJECTIVES: To review ibogaine's pharmacokinetics and pharmacodynamics, mechanisms of action and reported toxicity. METHODS: A search of the literature available on PubMed was done, using the keywords "ibogaine" and "noribogaine"...
2016: Clinical Toxicology
https://www.readbyqxmd.com/read/26518330/differential-roles-of-gabab1-subunit-isoforms-on-locomotor-responses-to-acute-and-repeated-administration-of-cocaine
#13
Laura H Jacobson, Fabian F Sweeney, Klemens Kaupmann, Olivia F O'Leary, Martin Gassmann, Bernhard Bettler, John F Cryan
GABAB receptors are crucial modulators of the behavioural effects of drug abuse, and agonists and positive allosteric modulators show promise as pharmacological strategies for anti-addiction therapeutics. GABAB receptors are functional heterodimers of GABAB1 and GABAB2 subunits. The predominant neuronal GABAB1 subunit isoforms are GABAB1a and GABAB1b. Selective ablation of these isoforms in mice revealed differential behavioural responses in fear, cognition and stress sensitivity. However, the influence of the two GABAB1 isoforms on responses to drugs of abuse is unclear...
February 1, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/26337199/salvia-officinalis-l-attenuates-morphine-analgesic-tolerance-and-dependence-in-rats-possible-analgesic-and-sedative-mechanisms
#14
Parisa Hasanein, Masoud Teimuri Far, Abbasali Emamjomeh
BACKGROUND: Salvia officinalis L. (SO) has effects on the central nervous system, including anti-addiction properties that may involve an opioid mechanism. OBJECTIVE: Effects of a hydroalcoholic extract of SO on nociception and on morphine-induced tolerance and dependence were evaluated in rats. METHODS: Tolerance and dependence were induced by injection of morphine (10 mg/kg, s.c.) or escalating doses of morphine (2.5, 2.5, 5, 10, 20, 40 and 50 mg/kg, s...
2015: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/26334786/methamphetamine-blocks-exercise-effects-on-bdnf-and-drd2-gene-expression-in-frontal-cortex-and-striatum
#15
COMPARATIVE STUDY
Andrew B Thompson, Alexandra Stolyarova, Zhe Ying, Yumei Zhuang, Fernando Gómez-Pinilla, Alicia Izquierdo
Exposure to drugs of abuse can produce many neurobiological changes which may lead to increased valuation of rewards and decreased sensitivity to their costs. Many of these behavioral alterations are associated with activity of D2-expressing medium spiny neurons in the striatum. Additionally, Bdnf in the striatum has been shown to play a role in flexible reward-seeking behavior. Given that voluntary aerobic exercise can affect the expression of these proteins in healthy subjects, and that exercise has shown promise as an anti-addictive therapy, we set out to quantify changes in D2 and Bdnf expression in methamphetamine-exposed rats given access to running wheels...
December 2015: Neuropharmacology
https://www.readbyqxmd.com/read/26306328/enhancing-brain-pregnenolone-may-protect-cannabis-intoxication-but-should-not-be-considered-as-an-anti-addiction-therapeutic-hypothesizing-dopaminergic-blockade-and-promoting-anti-reward
#16
Kenneth Blum, Marlene Oscar-Berman, Eric R Braverman, Marcelo Febo, Mona Li, Mark S Gold
Many US states now embrace the medical and recreational use of Cannabis. Changes in the laws have heightened interest and encouraged research into both cannabinoid products and the potential harms of Cannabis use, addiction, and intoxication. Some research into those harms will be reviewed here and misgivings about the use of Pregnenolone, to treat cannabis addiction and intoxication explained. Pregnenolone considered the inactive precursor of all steroid hormones, has recently been shown to protect the brain from Cannabis intoxication...
2015: Journal of Reward Deficiency Syndrome
https://www.readbyqxmd.com/read/26302653/noribogaine-is-a-g-protein-biased-%C3%AE%C2%BA-opioid-receptor-agonist
#17
Emeline L Maillet, Nicolas Milon, Mari D Heghinian, James Fishback, Stephan C Schürer, Nandor Garamszegi, Deborah C Mash
Noribogaine is the long-lived human metabolite of the anti-addictive substance ibogaine. Noribogaine efficaciously reaches the brain with concentrations up to 20 μM after acute therapeutic dose of 40 mg/kg ibogaine in animals. Noribogaine displays atypical opioid-like components in vivo, anti-addictive effects and potent modulatory properties of the tolerance to opiates for which the mode of action remained uncharacterized thus far. Our binding experiments and computational simulations indicate that noribogaine may bind to the orthosteric morphinan binding site of the opioid receptors...
December 2015: Neuropharmacology
https://www.readbyqxmd.com/read/26244288/salvia-officinalis-l-attenuates-morphine-analgesic-tolerance-and-dependence-in-rats-possible-analgesic-and-sedative-mechanisms
#18
Parisa Hasanein, Masoud Teimuri Far, Abbasali Emamjomeh
BACKGROUND: Salvia officinalis L. (SO) has effects on the central nervous system, including anti-addiction properties that may involve an opioid mechanism. OBJECTIVE: Effects of a hydroalcoholic extract of SO on nociception and on morphine-induced tolerance and dependence were evaluated in rats. METHODS: Tolerance and dependence were induced by injection of morphine (10 mg/kg, s.c.) or escalating doses of morphine (2.5, 2.5, 5, 10, 20, 40 and 50 mg/kg, s...
August 5, 2015: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/26177654/dopamine-d3-receptor-antagonist-gsk598809-potentiates-the-hypertensive-effects-of-cocaine-in-conscious-freely-moving-dogs
#19
Nathan M Appel, Shou-Hua Li, Tyson H Holmes, Jane B Acri
The chronic and relapsing nature of addiction presents unique challenges for ensuring the safety of a potential medication. A patient may use cocaine, for example, while taking the medication or take more medication than prescribed. Thus, a potential medication must be safe and not exacerbate the effects of cocaine. Multiple published studies support antagonism of brain dopamine D3 receptor function as a potential mechanism of action for an anti-addiction medication. Dopamine D3 receptors are widely distributed outside the central nervous system, however; for example, dopamine D3 receptors in the kidneys are implicated in regulating blood pressure...
September 2015: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/26093587/-gabab-receptor-as-therapeutic-target-for-drug-addiction-from-baclofen-to-positive-allosteric-modulators
#20
REVIEW
Roberta Agabio, Giancarlo Colombo
The present paper summarizes experimental and clinical data indicating the therapeutic potential of the GABAB receptor agonist, baclofen, in the treatment of alcohol use disorder (AUD) and substance use disorder (SUD). Multiple preclinical studies have demonstrated the ability of baclofen to suppress alcohol drinking (including binge- and relapse-like drinking), oral alcohol self-administration, and intravenous self-administration of cocaine, nicotine, amphetamine, methamphetamine, morphine, and heroin in rodents...
March 2015: Psychiatria Polska
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