keyword
MENU ▼
Read by QxMD icon Read
search

Phenibut

keyword
https://www.readbyqxmd.com/read/28726197/effect-of-phenibut-and-glufimet-a-novel-glutamic-acid-derivative-on-respiration-of-heart-and-brain-mitochondria-from-animals-exposed-to-stress-against-the-background-of-inducible-no-synthase-blockade
#1
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...
July 18, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28723730/phenibut-%C3%AE-phenyl-%C3%AE-aminobutyric-acid-psychosis
#2
William Li, Bhaskara Madhira
No abstract text is available yet for this article.
May 24, 2017: American Journal of Therapeutics
https://www.readbyqxmd.com/read/28651175/challenges-in-gc-ms-analysis-case-studies-on-phenibut-and-ethylphenidate
#3
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...
June 9, 2017: Forensic Science International
https://www.readbyqxmd.com/read/28614159/dissociative-intoxication-and-prolonged-withdrawal-associated-with-phenibut-a-case-report
#4
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
https://www.readbyqxmd.com/read/28441273/case-report-of-physiologic-phenibut-dependence-treated-with-a-phenobarbital-taper-in-a-patient-being-treated-with-buprenorphine
#5
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
https://www.readbyqxmd.com/read/27666756/phenibut-overdose
#6
Seth Sankary, Peter Canino, Jennifer Jackson
No abstract text is available yet for this article.
March 2017: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/27116874/-the-role-of-opioidergic-and-gabaergic-systems-in-the-mechanosensitivity-regulation-of-the-respiratory-system-in-rats
#7
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
https://www.readbyqxmd.com/read/26989804/l-proline-derived-bifunctional-organocatalysts-enantioselective-michael-addition-of-dithiomalonates-to-trans-%C3%AE-nitroolefins
#8
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
https://www.readbyqxmd.com/read/26906198/comparison-of-nootropic-and-neuroprotective-features-of-aryl-substituted-analogs-of-gamma-aminobutyric-acid
#9
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
https://www.readbyqxmd.com/read/26894962/optical-isomers-of-phenibut-inhibit-h-3-gabapentin-binding-in-vitro-and-show-activity-in-animal-models-of-chronic-pain
#10
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
https://www.readbyqxmd.com/read/26621244/the-neuroprotective-effects-of-r-phenibut-after-focal-cerebral-ischemia
#11
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
https://www.readbyqxmd.com/read/26234470/r-phenibut-binds-to-the-%C3%AE-2-%C3%AE-subunit-of-voltage-dependent-calcium-channels-and-exerts-gabapentin-like-anti-nociceptive-effects
#12
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
https://www.readbyqxmd.com/read/26205724/effects-of-a-new-glutamic-acid-derivative-on-myocardial-contractility-of-stressed-animals-under-conditions-of-nitric-oxide-synthesis-blockade
#13
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
https://www.readbyqxmd.com/read/26114346/acute-behavioural-disturbance-associated-with-phenibut-purchased-via-an-internet-supplier
#14
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
https://www.readbyqxmd.com/read/26107626/analytically-confirmed-recreational-use-of-phenibut-%C3%AE-phenyl-%C3%AE-aminobutyric-acid-bought-over-the-internet
#15
LETTER
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
https://www.readbyqxmd.com/read/26033589/effects-of-phenibut-and-citrocard-on-non-competitive-and-competitive-behavior-during-provoked-aggression-in-animals
#16
COMPARATIVE STUDY
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
https://www.readbyqxmd.com/read/25877201/multistep-continuous-flow-synthesis-of-r-and-s-rolipram-using-heterogeneous-catalysts
#17
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
https://www.readbyqxmd.com/read/25763683/palladium-catalyzed-cs2co3-promoted-arylation-of-unactivated-c-sp-3-h-bonds-by-diacetoxyiodo-arenes-shifting-the-reactivity-of-diacetoxyiodo-arenes-from-acetoxylation-to-arylation
#18
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
https://www.readbyqxmd.com/read/25432276/effect-of-gaba-derivatives-on-the-rate-of-thrombus-formation-platelet-aggregation-and-plasma-coagulation-capacity-in-rats-with-experimental-gestosis
#19
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
https://www.readbyqxmd.com/read/25365864/-cardioprotective-properties-of-new-glutamic-acid-derivative-under-stress-conditions
#20
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
keyword
keyword
30807
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"