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https://www.readbyqxmd.com/read/29028556/buspirone-maintenance-does-not-alter-the-reinforcing-subjective-and-cardiovascular-effects-of-intranasal-methamphetamine
#1
Anna R Reynolds, Justin C Strickland, William W Stoops, Joshua A Lile, Craig R Rush
BACKGROUND: Medications development efforts for methamphetamine-use disorder have targeted central monoamines because these systems are directly involved in the effects of methamphetamine. Buspirone is a dopamine autoreceptor and D3 receptor antagonist and partial agonist at serotonin 1A receptors, making it a logical candidate medication for methamphetamine-use disorder. Buspirone effects on abuse-related behaviors of methamphetamine have been mixed in clinical and preclinical studies...
September 22, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29021837/the-bssg-rat-model-of-parkinson-s-disease-progressing-towards-a-valid-predictive-model-of-disease
#2
REVIEW
Jackalina M Van Kampen, Harold A Robertson
ABSTRACT: Parkinson's disease (PD) is a neurodegenerative disorder, classically considered a movement disorder. A great deal is known about the anatomical connections and neuropathology and pharmacological changes of PD, as they relate to the loss of dopaminergic function and the appearance of cardinal motor symptoms. Our understanding of the role of dopamine in PD has led to the development of effective pharmacological treatments of the motor symptoms in the form of dopamine replacement therapy using levodopa and dopaminergic agonists...
September 2017: EPMA Journal
https://www.readbyqxmd.com/read/29017334/brexpiprazole-a-new-leaf-on-the-partial-dopamine-agonist-branch
#3
Judy Hope, David Castle, Nicholas A Keks
OBJECTIVES: Brexpiprazole is a new dopamine partial agonist antipsychotic in the same class as aripiprazole. This paper will briefly review brexpiprazole and compare it with aripiprazole. CONCLUSIONS: Brexpiprazole and aripiprazole are both partial agonists at dopamine D2, and serotonin 5-HT1A and antagonists at serotonin 5-HT2A and noradrenergic α1B receptors. However, the two drugs are significantly different in potencies at various receptors; neurochemical profiles predict that brexpiprazole may be comparable with aripiprazole in its antipsychotic efficacy but may cause less akathisia, extrapyramidal side effects (EPS) and activation...
October 1, 2017: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
https://www.readbyqxmd.com/read/28993209/rotigotine-a-dopamine-receptor-agonist-increased-bdnf-protein-levels-in-the-rat-cortex-and-hippocampus
#4
Naoki Adachi, Aya Yoshimura, Shuichi Chiba, Shintaro Ogawa, Hiroshi Kunugi
Brain-derived neurotrophic factor (BDNF) critically controls the fate and function of the neuronal network and has received much attention as a target of many brain diseases. Dopaminergic system dysfunction has also been implicated in a variety of neuropsychiatric diseases. Rotigotine, a non-ergot dopamine receptor agonist, is used in the treatment of Parkinson's disease and restless legs syndrome. To investigate the effects of rotigotine on neuronal functions both in vivo and in vitro, rats and primary cortical neurons were administered rotigotine, and the mRNA and protein expression levels of BDNF, its receptor TrkB and downstream signaling molecules, and synaptic proteins were determined...
October 6, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28992711/-treatment-of-pituitary-adenomas
#5
Jana Ježková, Josef Marek, Manuela Vaněčková
Pituitary adenomas are the most common tumours of the sellar region. A combination of neurosurgery, radiation and pharmacological approaches are applied for the treatment of pituitary adenomas. In certain cases, patient observation is another option. Neurosurgery is the first-choice treatment for acromegaly, Cushing´s disease and TSH secreting adenomas. Leksell gamma knife irradiation is used in the treatment of tumour residues. Until the effect of the irradiation is evident, pharmacological treatment must be administered...
2017: Casopís Lékar̆ů C̆eských
https://www.readbyqxmd.com/read/28991505/modulation-of-sk-channels-regulates-locomotor-alternating-bursting-activity-in-the-functionally-mature-spinal-cord
#6
Amr A Mahrous, Sherif M Elbasiouny
The spinal cord contains specialized groups of cells called pattern generators, which are capable of orchestrating rhythmic firing activity in an isolated preparation. Different patterns of activity could be generated in vitro including right-left alternating bursting and bursting in which both sides are synchronized. The cellular and network mechanisms that enable these behaviors are not fully understood. We have recently shown that Ca(2+)-activated K(+) channels (SK channels) control the initiation and amplitude of synchronized bursting in the spinal cord...
October 9, 2017: Channels
https://www.readbyqxmd.com/read/28986565/activation-induced-conformational-changes-of-dopamine-d3-receptor-promote-the-formation-of-the-internal-water-channel
#7
Wei-Hsiang Weng, Ya-Tzu Li, Hao-Jen Hsu
The atomic-level dopamine activation mechanism for transmitting extracellular ligand binding events through transmembrane helices to the cytoplasmic G protein remains unclear. In the present study, the complete dopamine D3 receptor (D3R), with a homology-modeled N-terminus, was constructed to dock different ligands to simulate conformational alterations in the receptor's active and inactive forms during microsecond-timescale molecular dynamic simulations. In agonist-bound systems, the D3R N-terminus formed a "lid-like" structure and lay flat on the binding site opening, whereas in antagonist and inverse agonist-bound systems, the N-terminus exposed the binding cavity...
October 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28986235/alpha-synuclein-epigenetics-mitochondria-metabolism-calcium-traffic-circadian-dysfunction-in-parkinson-s-disease-an-integrated-strategy-for-management
#8
REVIEW
Oliver T Phillipson
The motor deficits which characterise the sporadic form of Parkinson's disease arise from age-related loss of a subset of dopamine neurons in the substantia nigra. Although motor symptoms respond to dopamine replacement therapies, the underlying disease process remains. This review details some features of the progressive molecular pathology and proposes deployment of a combination of nutrients: R-lipoic acid, acetyl-L-carnitine, ubiquinol, melatonin (or receptor agonists) and vitamin D3, with the collective potential to slow progression of these features...
October 3, 2017: Ageing Research Reviews
https://www.readbyqxmd.com/read/28984746/late-reduction-of-cocaine-cravings-in-a-randomized-double-blind-trial-of-aripiprazole-vs-perphenazine-in-schizophrenia-and-comorbid-cocaine-dependence
#9
Thomas Beresford, Jennifer Buchanan, Elizabeth Brie Thumm, Chad Emrick, David Weitzenkamp, Patrick J Ronan
PURPOSE: Co-occurring schizophrenia spectrum disorder and International Statistical Classification of Diseases, 10th Revision cocaine dependence present a particularly destructive constellation that is often difficult to treat. Both conditions raise dopamine transmission effects in the brain. Traditional neuroleptics block dopamine receptors, whereas aripiprazole modulates dopamine activity as an agonist/antagonist. We tested whether dopamine modulation is superior to dopamine blocking in dual-diagnosis patients...
October 3, 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28983964/dopamine-cross-reacts-with-adrenoreceptors-in-cortical-astrocytes-to-induce-bdnf-expression-creb-signaling-and-morphological-transformation
#10
Indrek Koppel, Kaur Jaanson, Airi Klasche, Jürgen Tuvikene, Tõnis Tiirik, Angela Pärn, Tõnis Timmusk
Expression of brain-derived neurotrophic factor (BDNF) is induced in cultured rat cortical astrocytes by catecholamines norepinephrine and dopamine as well as selective α1 and β adrenergic agonists. However, it has remained unknown which receptors mediate dopamine-induced BDNF upregulation in astrocytes. Here, we demonstrate that β adrenoreceptors are the main mediators of this effect in cultured cortical astrocytes, while α1 adrenoreceptors and D1 dopamine receptors contribute to a lesser extent. We show that in cortical astrocytes BDNF exon IV and exon VI containing mRNAs are induced by dopamine and norepinephrine via CREB-dependent signaling and that this regulation is mediated by a mechanism that is distinct from activity-dependent CREB-mediated activation of BDNF transcription in neurons...
October 6, 2017: Glia
https://www.readbyqxmd.com/read/28981227/-treatment-of-parkinson-s-disease
#11
S Dethy
Parkinson's disease in a neurodegenerative disorder that affects as many as 1-2 % of persons aged 60 years and older. Parkinson's disease occurs infrequently under 40 years of age, with major genetic implication. Alpha-synuclein plays significant pathogenic role in Parkinson's disease. Therapeutic advances based on a synucleinrelated mechanism are now developed : immunotherapy against alpha-synuclein for example. The diagnosis of Parkinson's disease remains mostly clinical. DatScan® may be helpful to distinguish parkinsonian syndrome and essential tremor...
2017: Revue Médicale de Bruxelles
https://www.readbyqxmd.com/read/28979633/-rare-localization-of-aneurysmal-bone-cyst-in-the-sphenoid-bone
#12
Farida Abdoulkader, Kaoutar Aammou, Abdellatif Siwane, Fatiha Essodegui
Aneurysmal bone cyst is a benign tumor that can affect all bones in the body. It rarely affects the base of the skull. It is usually located at the level of the long bones. We report the clinical case of a 44-year old man treated for a mass in the basisphenoid wrongly diagnosed as invasive prolactin-producing macroadenoma for which he was put under dopamine agonists over a period of 9 months. We adjusted the diagnosis by suggesting aneurysmal bone cyst in the sphenoid bone on the basis of its almost pathognomonic radiological aspect on MRI...
2017: Pan African Medical Journal
https://www.readbyqxmd.com/read/28978077/am1241-alleviates-mptp-induced-parkinson-s-disease-and-promotes-the-regeneration-of-da-neurons-in-pd-mice
#13
Jun Shi, Qiong Cai, Jingxing Zhang, Xiaolie He, Yigang Liu, Rongrong Zhu, Lingjing Jin
The main pathological feature of Parkinson's disease (PD) is the loss of dopaminergic neurons in the substantia nigra. In this study, we investigated the role of cannabinoid receptor 2 (CB2R) agonist AM1241 on 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced neurotoxicity in a mouse model of PD. Upon treatment with AM1241, the decreased CB2R level in the PD mouse brain was reversed and the behavior score markedly elevated, accompanied with a dose-dependent increase of dopamine and serotonin. In addition, western blot assay and immunostaining results suggested that AM1241 significantly activated PI3K/Akt/MEK phosphorylation and increased the expression of Parkin and PINK1, both in the substantia nigra and hippocampus...
September 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28975698/dopamine-d4-receptor-activation-restores-ca1-ltp-in-hippocampal-slices-from-aged-mice
#14
Fangli Guo, Jianhua Zhao, Dandan Zhao, Jiangang Wang, Xiaofang Wang, Zhiwei Feng, Martin Vreugdenhil, Chengbiao Lu
Normal aging is characterized with a decline in hippocampal memory functions that is associated with changes in long-term potentiation (LTP) of the CA3-to-CA1 synapse. Age-related deficit of the dopaminergic system may contribute to impairment of CA1 LTP. Here we assessed how the modulation of CA1 LTP by dopamine is affected by aging and how it is dependent on the Ca(2+) source. In slices from adult mice, the initial slope of the field potential showed strong LTP, but in slices from aged mice LTP was impaired...
October 3, 2017: Aging Cell
https://www.readbyqxmd.com/read/28973192/pituitary-tumor-suppression-by-combination-of-cabergoline-and-chloroquine
#15
Shao Jian Lin, Ze Rui Wu, Lei Cao, Yong Zhang, Zhi Gen Leng, Yu Hang Guo, Han Bing Shang, Wei Guo Zhao, Xun Zhang, Zhe Bao Wu
CONTEXT: The dopamine agonist cabergoline (CAB) has been used widely in treatment of prolactinomas and other types of pituitary adenomas, but its clinical use is hampered by intolerance in some prolactinoma patients and lack of effectiveness in other pituitary tumor types. Chloroquine (CQ) is an old drug widely used in treatment of malaria. Recent studies, including our own, have revealed that CAB and CQ are involved in induction of autophagy and activation of autophagic cell death. OBJECTIVE: We tested whether CAB and CQ can function cooperatively to suppress growth of pituitary adenomas as well as other cancers...
July 20, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28971230/effects-of-2-bromoterguride-a-dopamine-d2-receptor-partial-agonist-on-cognitive-dysfunction-and-social-aversion-in-rats
#16
Emilia Tarland, Robert T Franke, Heidrun Fink, Heinz H Pertz, Jan Brosda
RATIONALE: 2-Bromoterguride, a dopamine D2 receptor partial agonist with antagonist properties at serotonin 5-HT2A receptors and α2C-adrenoceptors, meets the prerequisites of a putative atypical antipsychotic drug (APD). We recently showed that 2-bromoterguride is effective in tests of positive symptoms of schizophrenia in rats without inducing extrapyramidal side effects or metabolic changes. OBJECTIVE: In continuation of our recent work, we now investigated the effect of 2-bromoterguride on apomorphine and phencyclidine (PCP)-induced disruptions of prepulse inhibition (PPI) of the acoustic startle response, a measure of sensory gating...
October 3, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28970253/characterization-of-soy-deprestatin-a-novel-orally-active-decapeptide-that-exerts-antidepressant-like-effects-via-gut-brain-communication
#17
Yukiha Mori, Saho Asakura, Akane Yamamoto, Saori Odagiri, Daisuke Yamada, Masayuki Sekiguchi, Keiji Wada, Masaru Sato, Atsushi Kurabayashi, Hideyuki Suzuki, Ryuhei Kanamoto, Kousaku Ohinata
We found that the orally administered thermolysin digest of β-conglycinin exhibits antidepressant-like effects in tail suspension and forced swim tests in mice. A comprehensive peptide analysis of the digest using liquid chromatography/mass spectrometry was performed, and LSSTQAQQSY emerged as a candidate antidepressant-like peptide. Orally administered synthetic LSSTQAQQSY exhibited antidepressant-like effects at a dose of 0.3 mg/kg; therefore, we named the decapeptide soy-deprestatin. In contrast, intraperitoneally administered soy-deprestatin was ineffective...
September 27, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28964731/time-and-dose-related-effects-of-a-gonadotropin-releasing-hormone-agonist-and-dopamine-antagonist-on-reproduction-in-the-northern-leopard-frog-lithobates-pipiens
#18
Maria Vu, Bradley Weiler, Vance L Trudeau
Gonadotropin-releasing hormone (GnRH) stimulates luteinizing hormone release to control ovulation and spermiation in vertebrates. Dopamine (DA) has a clear inhibitory role in the control of reproduction in numerous teleosts, and emerging evidence suggests that similar mechanisms may exist in amphibians. The interactions between GnRH and DA on spawning success and pituitary gene expression in the Northern leopard frog (Lithobates pipiens) were therefore investigated. Frogs were injected during the natural breeding season with a GnRH agonist [GnRH-A; (Des-Gly(10), D-Ala(6), Pro-NHEt(9))-LHRH; 0...
December 1, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28964519/inhibiting-prolactin-by-cabergoline-accelerates-mammary-gland-remodeling-during-the-early-dry-period-in-dairy-cows
#19
M Boutinaud, N Isaka, E Gandemer, P Lamberton, S Wiart, A I De Prado Taranilla, L M Sordillo, V Lollivier
The inhibition of prolactin release using cabergoline, a dopamine agonist, is an effective strategy to accelerate the changes in mammary secretion composition after drying-off. The objective of this study was to determine how cabergoline may affect mammary tissue remodeling during early involution. Holstein dairy cows were treated with either a single i.m. administration of 5.6 mg of cabergoline (Velactis, Ceva Santé Animale, Libourne, France, n = 7) or placebo (n = 7) at the time of drying-off. Mammary biopsy samples were collected 1 wk before drying-off (d -6), after 30 h of milk accumulation (d 1), and again 8 d following drying-off (d 8) to determine changes in gene expression, lactoferrin content, and cell turnover...
September 27, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28963856/dopamine-d2-receptor-signaling-controls-inflammation-in-acute-pancreatitis-via-pp2a-dependent-akt-nf%C3%AE%C2%BAb-signaling-pathway
#20
Xiao Han, Bin Li, Xin Ye, Tunike Mulatibieke, Jianghong Wu, Juanjuan Dai, Deqing Wu, Jianbo Ni, Ruling Zhang, Jing Xue, Rong Wan, Xingpeng Wang, Guoyong Hu
BACKGROUND AND PURPOSE: Dopamine (DA) has multiple anti-inflammatory effects, but its role and molecular mechanism in acute pancreatitis (AP) is unclear. We investigated the role of DA signaling on inflammatory response in AP. EXPERIMENTAL APPROACH: We analyzed the changes of pancreatic dopaminergic system and effects of DA, antagonists and agonists of DA receptor (DRD)1 and 2 in wild-type and pancreas-specific Drd2(-/-) mice with AP (induced by caerulein and lipopolysaccharide or L-Arginine) or in pancreatic acinar cells with or without CCK stimulation...
September 30, 2017: British Journal of Pharmacology
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