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Seth Sankary, Peter Canino, Jennifer Jackson
No abstract text is available yet for this article.
September 1, 2016: 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
I N Tyurenkov, V N Perfilova, V I Karamysheva, L B Reznikova, I S Mokrousov, L I Mikhailova, V M Berestovitskaya, O S Vasil'eva
Experimental gestosis induced by replacement of drinking water with 1.8% NaCl promoted hypercoagulation, increased the rate and degree of platelet aggregation, and reduced clotting time in pregnant females. GABA derivatives, compounds RGPU-151, RGPU-152, and phenibut normalized parameters of hemostasis and platelet aggregation and the rate of thrombus formation in the animals. The efficiency of the test substances did not significantly differ from that of the reference drug sulodexide.
December 2014: Bulletin of Experimental Biology and Medicine
V N Perfilova, N V Sadikova, V M Berestovitskaia, O S Vasil'eva
The effect of new glutamic acid derivative on the cardiac ino- and chronotropic functions has been studied in experiments on rats exposed to 24-hour immobilization-and-pain stress. It is established that glutamic acid derivative RGPU-238 (glufimet) at a dose of 28.7 mg/kg increases the increment of myocardial contractility and relaxation rates and left ventricular pressure in stress-tested animals by 13 1,1, 72.4, and 118.6%, respectively, as compared to the control group during the test for adrenoreactivity...
2014: Eksperimental'naia i Klinicheskaia Farmakologiia
Charles W O'Connell, Aaron B Schneir, James Q Hwang, F Lee Cantrell
No abstract text is available yet for this article.
August 2014: American Journal of Medicine
E V Volotova, D V Kurkin, N V Mazina, V M Berestovitskaia, O S Vasil'eva
A comparative analysis of the effect of phenyl derivatives of glutamic (RGPU-135) and gamma-aminobutyric acid (Phenibut) on cerebral blood flow, vasodilatory endothelial function and the number of circulating endothelial cells desquamated in animals after irreversible occlusion of the common carotid arteries. It was found that animals treated prophylactically by RGPU-135, after occlusion of the common carotid arteries have higher cerebral blood flow and lower the severity of endothelial dysfunction than in animals treated with Phenibut...
2013: Eksperimental'naia i Klinicheskaia Farmakologiia
Lovisa Högberg, István Szabó, Jaan Ruusa
No abstract text is available yet for this article.
April 17, 2013: Läkartidningen
Andriy V Samokhvalov, C Lindsay Paton-Gay, Kam Balchand, Jürgen Rehm
Phenibut is a γ-aminobutyric acid (GABA) agonist designed and used as an anxiolytic in Russia. In Western countries, phenibut is not a registered medication but is available through online stores as a supplement. We present a case of a patient who used phenibut to self-medicate anxiety, insomnia and cravings for alcohol. While phenibut was helpful initially, the patient developed dependence including tolerance, significant withdrawal symptoms within 3-4 h of last use and failure to fulfil his roles at work and at home...
February 6, 2013: BMJ Case Reports
I N Tiurenkov, E V Volotova, D V Kurkin, A A Litvinov, A S Tarasov
It is shown that, in rats with global cerebral ischemia modeled by a complete irreversible occlusion of the common carotid artery and forced hypotension, the hemostasis is characterized by a shift toward hypercoagulation. A single preventive introduction of phenibut and, to a greater degree, a composition of phenibut with nicotinic acid, in rats with acute cerebral ischemia reduced the extent of disturbances in the hemostasis system of experimental animals.
2012: Eksperimental'naia i Klinicheskaia Farmakologiia
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