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Xiuxiu Li, Cai You, Yusheng Yang, Yuhong Yang, Pan Li, Guoxian Gu, Lung Wa Chung, Hui Lv, Xumu Zhang
With the assistance of hydrogen bonds, the first asymmetric hydrogenation of β-cyanocinnamic esters is developed, affording chiral β-cyano esters with excellent enantioselectivities (up to 99% ee). This novel methodology provides an efficient and concise synthetic route to chiral GABA-derivatives such as ( S )-Pregabalin, ( R )-Phenibut, ( R )-Baclofen. Interestingly, in this system, the catalyst with a single H-bond donor performs better than that with double H-bond donors, which is a novel discovery in the metalorganocatalysis area...
February 21, 2018: Chemical Science
A V Borisov, I I Prokofiev, I S Mokrousov, V N Perfilova, I N Tyurenkov
The effects of glufimet and phenibut (glutamic acid and GABA derivatives, respectively) on concentration of inducible NO synthase and cGMP in LPS-activated mouse peritoneal macrophages and on NO end products in their culture medium were examined in vitro and ex vivo. Addition of LPS into culture medium elevated concentration of NO metabolites in this medium and increased concentration of inducible NO synthase and cGMP in the lysates of peritoneal macrophages, whereas incubation of the cells with examined agents applied at concentration of 10-5 M diminished these indices...
December 2017: Bulletin of Experimental Biology and Medicine
V N Perfilova, T A Popova, I I Prokofiev, I S Mokrousov, O V Ostrovskii, I N Tyurenkov
Increased oxygen consumption by heart and brain mitochondria in the absence of ADP and reduced mitochondrial respiration in the presence of ADP were observed in rats exposed to stress simulated by suspension by the dorsal neck skin fold for 24 h, which attests to uncoupling of substrate oxidation and ATP synthesis and can cause electron drain from the respiratory chain, formation of ROS, and oxidative damage to cell structures. Blockade of inducible NO synthase with aminoguanidine (single intraperitoneal dose of 50 mg/kg before stress exposure) increased coupling of respiration and oxidative phosphorylation in heart and brain mitochondria of rats exposed to immobilization-painful stress, which was especially pronounced in cardiomyocytes...
June 2017: Bulletin of Experimental Biology and Medicine
William Li, Bhaskara Madhira
No abstract text is available yet for this article.
September 2017: American Journal of Therapeutics
Hui Zhi Shirley Lee, Mei Ching Ong, Jong Lee Wendy Lim, Tiong Whei Angeline Yap
The challenges associated with drug analysis using GC-MS such as thermal degradation, cyclisation or unwanted side reactions causing potential erroneous identification have become evident in view of the high surge in new drugs available in the market. Two case studies illustrated how alternative methods or modifications to existing techniques can help to circumvent the limitations. In the first case study, phenibut which is a GABA analogue, cyclises to 4-phenyl-2-pyrrolidinone under thermal conditions. The identification of phenibut was achieved through derivatisation and identification of its TMS derivative...
August 2017: Forensic Science International
Yash B Joshi, Samantha F Friend, Berenice Jimenez, Louisa R Steiger
No abstract text is available yet for this article.
August 2017: Journal of Clinical Psychopharmacology
Emily Brunner, Robert Levy
: This case report describes the development of dependence to phenibut, a gamma-aminobutyric acid-receptor type B agonist, in a patient concurrently being treated with buprenorphine. The patient experienced withdrawal symptoms which were successfully treated with a phenobarbital taper based on a protocol to treat sedative use disorder. This case report provided an example of the development of a phenibut use disorder and also brought up a public health question of whether phenibut should therefore be officially classified and monitored...
May 2017: Journal of Addiction Medicine
Seth Sankary, Peter Canino, Jennifer Jackson
No abstract text is available yet for this article.
March 2017: American Journal of Emergency Medicine
L N Tikhomirova, N F Safina, I A Tarakanov
In anaesthetized white outbred male rats we investigated the change of respiratory mechanoreceptors sensitivity to morphine and phenibut. Bilateral transection of the vagus nerves causes a severely slowdown of respiratory rate in 30 minutes after the systemic administration of morphine, however after administration of phenibut the respiratory rate and other respiration parameters have not changed significantly. It means that the activation of opioid receptors by morphine does not significantly affect the function of the respiratory mechanoreceptor control loop, and transection of the vagus nerves on this background increases the probability of respiratory rhythm disorders...
October 2015: Patologicheskaia Fiziologiia i èksperimental'naia Terapiia
Hui Jin, Seung Tae Kim, Geum-Sook Hwang, Do Hyun Ryu
A series of novel L-proline derived tertiary amine bifunctional organocatalysts 9 are reported, which were applied to the asymmetric Michael addition of dithiomalonates 2 to trans-β-nitroolefins 1. The reaction proceeded in high yields (up to 99%) with high enantioselectivities (up to 97% ee). The synthetic utility of this methodology was demonstrated in the short synthesis of (R)-phenibut in high yield.
April 15, 2016: Journal of Organic Chemistry
I N Tyurenkov, L E Borodkina, V V Bagmetova, V M Berestovitskaya, O S Vasil'eva
GABA analogs containing phenyl (phenibut) or para-chlorophenyl (baclofen) substituents demonstrated nootropic activity in a dose of 20 mg/kg: they improved passive avoidance conditioning, decelerated its natural extinction, and exerted antiamnestic effect on the models of amnesia provoked by scopolamine or electroshock. Tolyl-containing GABA analog (tolibut, 20 mg/kg) exhibited antiamnestic activity only on the model of electroshock-induced amnesia. Baclofen and, to a lesser extent, tolibut alleviated seizures provoked by electroshock, i...
February 2016: Bulletin of Experimental Biology and Medicine
Irina Belozertseva, Jens Nagel, Barbara Valastro, Lutz Franke, Wojciech Danysz
BACKGROUND: We report that R- and S-phenibut (β-phenyl-γ-aminobutyric acid) - derivatives of GABA - bind with an affinity of c.a. 90μM to the gabapentin binding site in a competitive assay, a value comparable to that for previously claimed targets for this enantioermic molecule. This finding implied potential activity in neuropathic pain, this being one of the clinically validated indications for gabapentin. METHODS: The effect of phenibut on tactile allodynia was tested in a chronic constriction nerve injury (CCI) neuropathic pain model and against hypersensitivity following inflammation induced by inoculation using complete Freund's adjuvant (CFA) model...
June 2016: Pharmacological Reports: PR
Edijs Vavers, Liga Zvejniece, Baiba Svalbe, Kristine Volska, Elina Makarova, Edgars Liepinsh, Kristina Rizhanova, Vilnis Liepins, Maija Dambrova
R-phenibut is a γ-aminobutyric acid (GABA)-B receptor and α2 -δ subunit of the voltage-dependent calcium channel (VDCC) ligand. The aim of the present study was to test the effects of R-phenibut on the motor, sensory and tactile functions and histological outcomes in rats following transient middle cerebral artery occlusion (MCAO). In this study, MCAO was induced by filament insertion (f-MCAO) or endothelin-1 (ET1) microinjection (ET1-MCAO) in male Wistar or CD rats, respectively. R-phenibut was administrated at doses of 10 and 50mg/kg for 14 days in the f-MCAO or 7 days in the ET1-MCAO...
November 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Liga Zvejniece, Edijs Vavers, Baiba Svalbe, Grigory Veinberg, Kristina Rizhanova, Vilnis Liepins, Ivars Kalvinsh, Maija Dambrova
Phenibut is clinically used anxiolytic, mood elevator and nootropic drug. R-phenibut is responsible for the pharmacological activity of racemic phenibut, and this activity correlates with its binding affinity for GABAB receptors. In contrast, S-phenibut does not bind to GABAB receptors. In this study, we assessed the binding affinities of R-phenibut, S-phenibut, baclofen and gabapentin (GBP) for the α2-δ subunit of the voltage-dependent calcium channel (VDCC) using a subunit-selective ligand, radiolabelled GBP...
October 2015: Pharmacology, Biochemistry, and Behavior
I N Tyurenkov, V N Perfilova, N V Sadikova, V M Berestovitskaya, O S Vasil'eva
Glufimet (glutamic acid derivative) in a dose of 28.7 mg/kg limited the reduction of the cardiac functional reserve in animals subjected to 24-h stress under conditions of nonselective NO synthase blockade with L-NAME (10 mg/kg). Adrenoreactivity and increased afterload tests showed that the increment of myocardial contraction/relaxation rates, left-ventricular pressure, and HR were significantly higher in glufimet-treated stressed animals with NO synthesis blockade than in animals which received no glufimet...
July 2015: Bulletin of Experimental Biology and Medicine
Michael A Downes, Ingrid L Berling, Ahmed Mostafa, Jeffrey Grice, Michael S Roberts, Geoffrey K Isbister
CONTEXT: Toxicity from recreational substances marketed for other purposes is a well-documented clinical entity. We present two cases of phenibut toxicity procured via the internet. CASE DETAILS: A 20-year-old female presented to the emergency department (ED) having used phenibut the prior day. The main finding was a decreased level of consciousness, however when roused she became delirious. Supportive care only was required with no specific intervention. The patient made a full recovery over a 24-hour period and admitted to use of phenibut purchased online...
2015: Clinical Toxicology
Anselm Wong, Mark Little, David Caldicott, Chris Easton, Daniel Andres, Shaun L Greene
No abstract text is available yet for this article.
2015: Clinical Toxicology
V V Bagmetova, A N Krivitskaya, I N Tyurenkov
Anti-aggressive effects of phenibut (25 mg/kg) and its structural analogue citrocard (50 mg/kg) were revealed in rats under condition of provoked intraspecific aggression. These substances significantly decreased manifestations of aggression in animals: they increased the latency of attacks and reduced their number. Anti-aggressive effects of citrocard were more pronounced than effects of phenibut under conditions of non-competitive aggression induced by fear of inescapable painful exposure or under conditions of competitive aggression reflecting the ability of animals to reveal adaptive social communicative skills in aversive situation...
May 2015: Bulletin of Experimental Biology and Medicine
Tetsu Tsubogo, Hidekazu Oyamada, Shū Kobayashi
Chemical manufacturing is conducted using either batch systems or continuous-flow systems. Flow systems have several advantages over batch systems, particularly in terms of productivity, heat and mixing efficiency, safety, and reproducibility. However, for over half a century, pharmaceutical manufacturing has used batch systems because the synthesis of complex molecules such as drugs has been difficult to achieve with continuous-flow systems. Here we describe the continuous-flow synthesis of drugs using only columns packed with heterogeneous catalysts...
April 16, 2015: Nature
Quan Gou, Zhao-Fu Zhang, Zhi-Cheng Liu, Jun Qin
PdCl2(CH3CN)2-catalyzed arylation of unactivated C(sp(3))-H bonds using (diacetoxyiodo)arenes as arylation reagents is reported. The reactivity of (diacetoxyiodo)arenes as arylation reagents is enabled in the presence of Cs2CO3 under the reaction conditions. This arylation method is highly efficient and occurs without the use of silver salt. The reaction tolerates a broad substrate scope that was not demonstrated by other silver salt-free C(sp(3))-H bond arylation conditions. The synthetic utility of the method is further illustrated in the synthesis of the psychotropic drug phenibut...
March 20, 2015: Journal of Organic Chemistry
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