tofisopam / Generic mfg. - LARVOL DELTA

A simple route to 2,3-benzodiazepines from substituted indenes. (PubMed, Org Biomol Chem) - "The optimized conditions for a wide range of substituted 2,3-benzodiazepines, including the well-known anxiolytic tofisopam, were investigated. A detailed mechanism for the cyclization of 1,5-diketones with hydrazine hydrate was established using 1H NMR kinetic experiments."

Journal

Cardioprotective effect of Tofisopam against isoprenaline-induced myocardial infarction in rats via modulation of NLRP3IL-1βcaspase-1 pathway. (PubMed, Immunopharmacol Immunotoxicol) - "In contrast, the tofisopam-pretreated group showed a significant reversal of the cardiac damage induced by isoprenaline. Tofisopam protects against isoprenaline-induced MI through its antioxidant, anti-inflammatory, and anti-apoptotic properties."

Journal • Preclinical • Cardiovascular • CNS Disorders • Coronary Artery Disease • Depression • Heart Failure • Mood Disorders • Myocardial Infarction • Psychiatry • IL1B • NLRP3

Computational Studies on the Diastereospecific Lithium Variant of Oppenauer Oxidation of a Tofisopam Intermediate. (PubMed, J Org Chem) - "The computations revealed energetic differences caused by steric differences between the diastereomers that might provide an explanation for the experimentally formed products. In addition, the trend in the measured NMR shifts was also in line with the computed values, which allowed the assignment of the absolute configuration of the diastereomers."

Journal

A Comparison of the Anxiolytic Properties of Tofisopam and Diazepam: A Double-Blind, Randomized, Crossover, Placebo-Controlled Pilot Study. (PubMed, Pharmaceuticals (Basel)) - "Tofisopam did not impair cognitive abilities, and related withdrawal symptoms resembled those of the placebo. If larger future studies corroborate these findings, tofisopam should be classified as a homophtalazine."

Journal • CNS Disorders • General Anxiety Disorder • Mood Disorders • Psychiatry

Economic Separations of Organic Acidic or Basic Enantiomeric Mixtures-A Protocol Suggestion. (PubMed, Int J Mol Sci) - "The examples discussed are resolutions developed by our research team, through which we will try to illustrate the impact of all these considerations, presenting the methodological investigations interpreting recent discoveries and observations. Some special solid-state analytical and structural investigations assisting us in the elucidation and invention design of the resolution processes of some active pharmaceutical ingredients, such as Tetramisole, tofisopam, and Amlodipine, are also shown."

Journal • Review

Distribution of neuromedin U (NMU)-like immunoreactivity in the goldfish brain, and effect of intracerebroventricular administration of NMU on emotional behavior in goldfish. (PubMed, Peptides) - "ICV administration of NMU-21 at 10 pmol g body weight (BW) prolonged the time spent in the upper area of the tank, and this action mimicked that of ICV administration of the central-type benzodiazepine receptor (CBR) agonist tofisopam at 100 pmol g BW. These results suggest that NMU-21 potently induces anxiolytic-like action in the goldfish brain."

Journal • CNS Disorders • NMU

Antidepressant-like effect of tofisopam in mice: A behavioural, molecular docking and MD simulation study. (PubMed, J Psychopharmacol) - "Our in silico studies supported the behavioural findings that the antidepressant-like effect of tofisopam is mediated by μ- and δ-opioid receptors. This study is the first to show that tofisopam has antidepressant-like activity mediated by the serotonergic, catecholaminergic and opioidergic systems."

Journal • Preclinical • CNS Disorders • Depression • Psychiatry

Chronic fatigue syndrome against the background of the COVID-19 pandemic (PubMed, Zh Nevrol Psikhiatr Im S S Korsakova) - "One of the most frequent manifestations will be the development of chronic fatigue syndrome (CFS) after COVID-19. This article discusses the possible causes of the development of CFS, as well as possible ways of its treatment and prevention."

Journal • Fatigue • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Intracerebroventricular administration of α-melanocyte-stimulating hormone (α-MSH) enhances thigmotaxis and induces anxiety-like behavior in the goldfish Carassius auratus. (PubMed, Peptides) - "The action of α-MSH mimicked those of FG-7142 (a central-type benzodiazepine receptor (CBR) inverse agonist with an anxiogenic effect) at 10 pmol g BW and melanotan II (a melanocortin 4 receptor (MC4R) agonist) at 50 pmol g BW, whereas ICV administration of tofisopam (a CBR agonist with an anxiolytic effect) at 10 pmol g BW prolonged the time spent in the central area. The anxiogenic-like effect of α-MSH was abolished by treatment with the MC4R antagonist HS024 at 50 pmol g BW. These data indicate that α-MSH affects psychomotor activity in goldfish, and exerts an anxiogenic-like effect via the MC4R-signaling pathway."

Journal • Mood Disorders • Psychiatry

Cross reactivity of the CEDIA and HEIA benzodiazepine kits for 29 designer benzodiazepines and tofisopam. (PubMed, Drug Test Anal) - No abstract available

Journal

Vasorelaxant effects of benzodiazepines, non-benzodiazepine sedative-hypnotics, and tandospirone on isolated rat arteries. (PubMed, Eur J Pharmacol) - "Zolpidem and tandospirone caused over 80% relaxation at a concentration of 10 μM; diazepam, estazolam, etizolam, and tofisopam caused 60-70% relaxation; whereas 18 other BDZs (alprazolam, bromazepam, brotizolam, chlordiazepoxide, clobazam, clonazepam, clorazepate, ethyl loflazepate, flunitrazepam, flurazepam, lorazepam, lormetazepam, midazolam, nimetazepam, nitrazepam, oxazepam, temazepam, and triazolam) and zaleplon caused less than 50% relaxation. In conclusion, the direct vasodilatory effects of these drugs may be involved in the mechanisms underlying their adverse effects. Additionally, the decreased BP observed in persons who take BDZs or non-BDZs may be partly due to direct vasodilation."

Journal • CNS Disorders • Insomnia • Pain • Sleep Disorder

Benefits of androgen replacement therapy and audio-visual correction inclusion in the prevention of premature aging. (PubMed, Adv Gerontol) - "They were divided into 3 groups depending on the treatment: the 1st - standard therapy and escitalopram / tofisopam; the 2nd - standard therapy + audiovisual correction; the 3rd - standard therapy + audiovisual correction + testosterone undecanoate. In group of audiovisual correction we saw a more significant improvement in the lipid profile after treatment. Audiovisual correction and androgen therapy contributed to the improvement of erectile function indices and a decrease in the severity of the symptoms of ageing in men."

Journal • Cardiovascular • CNS Disorders • Depression • Diabetes • Dyslipidemia • Erectile Dysfunction • Genetic Disorders • Metabolic Disorders • Mood Disorders • Obesity

Antiamnesic effects of tofisopam against scopolamine-induced cognitive impairments in rats. (PubMed, Pharmacol Biochem Behav) - "Presented beneficial effects of tofisopam on cognitive dysfunctions may have a notable clinical value considering the fact that one of the most important side effects of 1,4-benzodiazepines, which are classical anxiolytic drugs, is amnesia. However, these preclinical results need to be confirmed with further clinical studies, first."

Journal • Preclinical • Glial Fibrillary Acidic Protein • Synaptophysin

Synthesis of Tofisopam by Way of Photoinduced CO2 Fixation. (PubMed, Chem Asian J) - "Herein reported is a unique synthetic route of Tofisopam, an anxiolytic drug containing a 2,3-benzodiazepine core structure.  3,4-Dimethoxypropylbenzene and 3,4-dimethoxybenzoic acid, which are both plant-origin, and CO2 constitute its carbon skeleton.  These three renewable substances are united by two C-C bond forming reactions, i.e., a Friedel-Crafts acylation reaction and a photoinduced carboxylation reaction to construct the major carbon framework.  Finally, a methyl group is introduced by a Kumada-type cross-coupling reaction to furnish Tofisopam.  Various analogs of Tofisopam are readily synthesized by introducing other substituents than a methyl group at the last C-C bond forming step."

Journal

Pharmacological Characteristics of Anxiolytics on Acetylcholine-Induced Contractions in Rat Detrusor Smooth Muscle. (PubMed, Pharmacology) - "ACh-induced contractions in rat DSM were inhibited by clotiazepam and diazepam (benzodiazepine anxiolytics) at concentrations that were clinically relevant. These contractions were also significantly inhibited by paroxetine, escitalopram (selective serotonin reuptake inhibitors -[SSRIs]), and hydroxyzine (a histamine H1 receptor antagonist), albeit at concentrations that substantially exceeded clinically achievable blood levels. At a concentration of 10-5 mol/L, paroxetine, escitalopram, and hydroxyzine inhibited 80 mmol/L high-KCl solution-induced rat DSM contractions but not clotiazepam and diazepam. Paroxetine, escitalopram, and hydroxyzine also inhibited specific binding of [3H]NMS in mouse cerebral cortex but clotiazepam and diazepam did not. In contrast to the effects of the abovementioned anxiolytics, ACh-induced contractions were not significantly affected by tofisopam, alprazolam, lorazepam, bromazepam, oxazolam, chlordiazepoxide, clonazepam, ethyl..."

Journal • Preclinical

Hallucinogen persisting perception disorder: A literature review and three case reports. (PubMed, J Addict Dis) - "The first case report describes a 23-year old patient with a previous history of cannabis consumption who reported HPDD type I after the use of psilocybin mushrooms with small amounts of alcohol and hash...Both patients sought medical help and received tofisopam, lamotrigine and sertraline...Scientific sources suggest that HPPD may affect more than 50% of hallucinogen users and this disorder is often underdiagnosed. Therefore, patients suffering from HPPD can present in various clinical settings, and clinicians should be aware of this condition."

Clinical • Journal