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Current Neuropharmacology

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https://www.readbyqxmd.com/read/28521704/dopamine-d2-receptors-dimers-how-can-we-pharmacologically-target-them
#1
Marco Carlia, Shivakumar Kolachalam, Stefano Aringhieri, Mario Rossib, Luca Giovannini, Roberto Maggio, Marco Scarselli
Dopamine D2 and D3 receptors are important pharmacological targets in Schizophrenia and Parkinson's disease. Intriguingly, many studies have shown that they form homo- and heterodimers, and they can be targeted in specific tissues with new drugs. In this direction, many efforts have been made to develop new molecules that are able to interact with these receptor dimeric complexes. Among various strategies for targeting dopamine receptors dimers, two distinct classes of compounds, such as bivalent and bitopic ligands, have gained particular attention and their use in pharmacology looks promising...
May 18, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28521703/recent-advances-in-antiepileptic-herbal-medicine
#2
Stephen M Manchishi
Epilepsy is one of the most common neurological disorders worldwide, with about 80 percent of cases thought to be in developing nations where it is mostly linked to superstition. Most cases of epilepsy are idiopathic, though brain injury, brain tumor, severe systemic infection and genetic mutations have been implicated in some cases. Anti-epileptic drugs (AEDs) currently in existence are not sufficient to contain the disorder. This is not only because of their limited availability and cost, but also their adverse side effects...
May 18, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28521702/role-of-ectonucleotidases-in-the-synapse-formation-during-brain-development-physiological-and-pathological-implications
#3
Ivana Grković, Dunja Drakulić, Jelena Martinović, Nataša Mitrović
Extracellular adenine nucleotides and nucleosides, such as ATP and adenosine, are among the most recently identified and least investigated diffusible signaling factors that contribute to the structural and functional remodeling of the brain, both during embryonic and postnatal development. Their levels in the extracellular milieu are tightly controlled by various ectonucleotidases: ectonucleotide pyrophosphatase/phosphodiesterases (E-NPP), alkaline phosphatases (AP), ectonucleoside triphosphate diphosphohydrolases (E-NTPDases) and ecto-5'-nucleotidase (eN)...
May 18, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28521701/unexpected-effects-of-acetylcholine-precursors-on-pilocarpine-seizure-induced-neuronal-death
#4
Minwoo Lee, Bo Young Choi, Sang Won Suh
Choline alfoscerate (α-GPC) and Cytidine 5'-diphosphocholine (CDP-Choline) are both acetylcholine precursors and are considered to act as pro-cholinergic nootropic agents. Acetylcholine precursors have also recently found frequent use in the neurology clinic. Stroke and many types of dementia have been shown to respond favorably after treatment with these agents, not only in terms of cognitive dysfunction but also behavioral and psychological symptoms. The primary mechanisms of Acetylcholine precursors are the following: 1) Acetylcholine precursors themselves are used in the biosynthesis of acetylcholine and 2) byproducts like glycerophosphate have protective functions for neuronal phospholipids...
May 18, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28521671/the-anticonvulsant-effects-of-ketogenic-diet-on%C3%A2-epileptic-seizures-and-potential-mechanisms
#5
Yifan Zhang, Jingwei Xu, Yingchao Zhang, Wei Yang, Bingjin Li
Epilepsy is one of the most commonly diagnosed neurologic disorders with characteristics of epileptic seizures. Although the multitude of anticonvulsant drugs has been developed, recurrent epileptic seizures remain intractable and contribute to the serious morbidity worldwide. Recently, increasing studies have established the beneficial effects of ketogenic diet (KD) on epileptic seizure reduction. Both basic experiments and clinical trials demonstrated that KD significantly reduced seizure frequency with mild adverse effects...
May 17, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28494719/levodopa-in-parkinson-s-disease-current-status-and-future-developments
#6
N Tambasco, M Romoli, P Calabresi
Ever since the pioneering reports in the 60s, L-3,4-Dioxyphenylalanine (levodopa) has represented the gold standard for the treatment of Parkinson's Disease (PD). However, long-term levodopa (LD) treatment is frequently associated with fluctuations in motor response, often challenging to resolve, with serious impact on patients quality of life. The pharmacokinetic and pharmacodynamics properties of LD are pivotal to such motor fluctuations: discontinuous drug delivery, short half-life, poor bioavailability, and narrow therapeutic window are all crucial for such fluctuations...
May 10, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28486926/5-ht3-receptors-a-potential-therapeutic-target-for-epilepsy
#7
Hongyan Zhao, Pu Wang, Shurui Chen, Xin Li, Hongliang Huo
Epilepsy is a syndrome of brain dysfunction caused by spontaneous, abnormal discharge. Many anti-epileptic drugs have developed in past decades. 5-HT is an important neurotransmitter in the central and peripheral nervous system of the human body which is involved in a number of physiological activities, such as sensation, movement, and behavior. 5-HT subtype have been divided into seven sub-groups from 5-HT1 to 5HT7. An increasing number of studies have shown that the activation of the 5-HT3 receptor can inhibit epileptic seizures, while inhibition of the 5HT3 receptor can promote spike waves...
May 8, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28486925/the-mutual-interaction-between-sleep-and-epilepsy-on-the-neurobiological-basis-and-therapy
#8
Yi-Qun Wang, Meng-Qi Zhang, Rui Li, Wei-Min Qu, Zhi-Li Huang
Sleep and epilepsy are mutually related in a complex, bidirectional manner. However, our understanding of this relationship remains unclear. In this paper, we address the issues involved in these phenomena and also discuss the various therapies used to modify them. The literatures of the neurobiological basis of the interactions between sleep and epilepsy indicate that non-rapid eye movement sleep and idiopathic generalized epilepsy share the same thalamocortical networks. Neuromodulators-such as adenosine, melatonin, prostaglandin D2, serotonin, and histamine-promote wakefulness and are considered to have antiepilepsy effects; antiepileptic drugs, in turn, also have effects on sleep...
May 8, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28474565/drug-resistant-epilepsy-and-surgery
#9
Jiyao Sheng, Shui Liu, Hanjiao Qin, Bingjin Li, Xuewen Zhang
Epilepsy is a chronic brain disease that is caused by various factors and characterized by recurrent, episodic and temporary central nervous system dysfunction which results due to excessive discharge of brain neurons. In the past decades, despite the continuous development of antiepileptic drugs, there are still many patients with epilepsy progressing to drug-resistant epilepsy. Currently, surgical treatment is the only possible way to cure drug-resistant epilepsy. However, surgical treatment alone often results in postoperative recurrence of epilepsy...
May 4, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28474564/substance-p-regulation-in-epilepsy
#10
Guangfan Chi, Zhehao Huang, Xianglan Li, Guangquan Li
Substance P (SP), an undecapeptide, is a member of the tachykinin family, and is encoded by the preprotachykinin-a gene. SP is widely distributed in the regions of the central nervous system associated with epilepsy and it contributes to the initiation and maintenance phases of epilepsy. In vivo, SP binds to the neurokinin-1 (NK-1) receptor and modulates the biological activity of the receptor. Although NK-1 receptor antagonists have anti-epileptic properties in animal models, the clinical efficacy of these drugs has not yet been verified...
May 4, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28474563/opioids-and-the-blood-brain-barrier-a-dynamic-interaction-with-consequences-on-drug-disposition-in-brain
#11
Catarina Chaves, Fernando Remião, Salvatore Cisterninoa, Xavier Declèves
Opioids are widely used in pain management whose effects are due to binding to classical opioid receptors and/or Toll-like receptors (TLR) present at the central nervous system (CNS). At the blood-brain barrier (BBB), several influx and/or efflux transporters are expressed, such as the ATP-binding cassette (ABC) P-glycoprotein (P-gp, ABCB1), Breast Cancer Resistance Protein (BCRP, ABCG2) and multidrug resistance-associated proteins (MRP, ABCC) transporters, and solute carrier transporters (SLC), and are responsible for the transport of many xenobiotics from the brain into the bloodstream or vice versa...
May 3, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28440188/trp-channels-as-novel-targets-for-endogenous-ligands-focus-on-endocannabinoids-and-nociceptive-signalling
#12
Maksim V Storozhuk, Alexander V Zholos
The endocannabinoid system is gaining steadily increasing research interest as its important role in the regulation of many fundamental physiological processes becomes more and more evident. One area which received particularly significant attention concerns targeting the endocannabinoid system as a useful strategy in pain control, especially in refractory, difficult to treat cases of chronic pain. Apart from the classical targets of cannabinoids, the CB1 and CB2 receptors, several members of the large TRP family of Ca2+-permeable cation channels have been designated as "ionotropic cannabinoid receptors" to highlight their role in cannabinoid signalling...
April 24, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28412910/aripiprazole-a-drug-that-displays-partial-agonism-and-functional-selectivity
#13
Erin W Tuplin, Matthew R Holahan
The treatment of schizophrenia is challenging due to the wide range of symptoms (positive, negative, cognitive) associated with the disease. Typical antipsychotics that antagonize D2 receptors are effective in treating positive symptoms, but extrapyramidal side-effects (EPS) are a common occurrence. Atypical antipsychotics targeting 5-TH2A and D2 receptors are more effective at treating cognitive and negative symptoms compared to typical antipsychotics, but these drugs also result in side-effects such as metabolic syndromes...
April 13, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28382869/the-role-of-autophagy-in-subarachnoid-hemorrhage-an-update
#14
Yuanjian Fang, Sheng Chen, Cesar Reis, Jianmin Zhang
Autophagy is an extensive self-degradation process for the disposition of cytosolic aggregated or misfolded proteins and defective organelles. Due to different cytosolic components, autophagy pathway executes the functions of pro-survival and pro-death to maintain cellular homeostasis. The pathway plays essential roles in several neurological disorders. Subarachnoid Hemorrhage (SAH) is a devastating subtype of hemorrhagic stroke with high risk of neurological deficit and high mortality. Early brain injury (EBI) plays a role in the poor clinical course and outcome after SAH...
April 6, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28393704/epigenetic-regulation-of-memory-therapeutic-potential-for-disorders
#15
Padmanabh Singh, Sweta Srivas, M K Thakur
Memory is a vital function which declines in different physiological and pathological conditions such as aging and neurodegenerative diseases. Research in the past has reported that memory formation and consolidation require the precise expression of synaptic plasticity genes. However, little is known about the regulation of these genes. Epigenetic modification is now a well established mechanism that regulates synaptic plasticity genes and neuronal functions including memory. Such modification includes mainly DNA methylation and hydroxymethylation, histone acetylation and methylation which involve chromatin modifying enzymes...
April 4, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28356049/calcium-engaged-mechanisms-of-nongenomic-action-of-neurosteroids
#16
Elzbieta Rebas, Tomasz Radzik, Tomasz Boczek, Ludmila Zylinska
Among hundreds of molecules affecting variety of neuronal processes, neurosteroids form the unique group because of their dual mechanism of action. Classically, they bind to intracellular and/or nuclear receptors, and next modify gene transcription. Another mode of action is linked with the rapid effects induced at the plasma membrane level within seconds or milliseconds. The negative and positive modulations have been documented for GABAA receptor complex, glycine receptor, NMDA receptor, AMPA receptor, G protein-coupled receptors and sigma-1 receptor, as well as for several membrane ion channels and plasma membrane enzymes...
March 28, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28322166/glutamate-modulating-drugs-as-a-potential-therapeutic-strategy-in-obsessive-compulsive-disorder
#17
Zoya Marinova, De-Maw Chuang, Naomi Fineberg
OBJECTIVE: Obsessive-compulsive disorder (OCD) is a mental disease commonly associated with severe distress and impairment of social functioning. Serotonin reuptake inhibitors and/or cognitive behavioural therapy are the therapy of choice, however up to 40% of patients do not respond to treatment. Glutamatergic signalling has also been implicated in OCD. The aim of the current study was to review the clinical evidence for therapeutic utility of glutamate-modulating drugs as an augmentation or monotherapy in OCD patients...
March 20, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28294068/cognitive-impacts-of-estrogen-treatment-in-androgen-deprived-males-what-needs-to-be-resolved
#18
Erik Wibowo
BACKGROUND: Many prostate cancer (PCa) patients are on androgen deprivation therapy (ADT) as part of their cancer treatments but ADT may cause cognitive impairments. ADT depletes men of both androgen and estrogen. Whether estradiol supplementation can improve cognitive impairments in patients on ADT is understudied. OBJECTIVE: To summarize data on the effects of estradiol treatment on cognitive function of androgen-deprived genetic male populations (PCa patients and male-to-female transsexuals) and castrated male animals...
March 13, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28294067/the-infectious-etiology-of-alzheimer-s-disease
#19
Marta Sochocka, Katarzyna Zwolińska, Jerzy Leszek
Inflammation is a part of the first line of defense of the body against invasive pathogens, and plays a crucial role in tissue regeneration and repair. A proper inflammatory response ensures the suitable resolution of inflammation and elimination of harmful stimuli, but when the inflammatory reactions are inappropriate it can lead to damage of the surrounding normal cells. The relationship between infections and Alzheimer's Disease (AD) etiology, especially late-onset AD (LOAD) has been continuously debated over the past three decades...
March 13, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28294066/mechanisms-of-melatonin-in-alleviating-alzheimer-s-disease
#20
Mayuri Shukla, Parichart Boontem, Russel J Reiter, Jutamaad Satayavivad, Piyarat Govitrapong
Alzheimer's disease (AD) is a chronic, progressive and prevalent neurodegenerative disease characterized by the loss of higher cognitive functions and an associated loss of memory. The thus far "incurable" stigma for AD prevails because of variations in the success rates of different treatment protocols in animal and human studies. Among the classical hypotheses explaining AD pathogenesis, the amyloid hypothesis is currently being targeted for drug development. The underlying concept is to prevent the formation of these neurotoxic peptides which play a central role in AD pathology and trigger a multispectral cascade of neurodegenerative processes post-aggregation...
March 13, 2017: Current Neuropharmacology
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