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Sympathetic Neurotransmission
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
The newer MAO inhibitors moclobemide (ManerixR) and toloxatone (DelalandeFR), which are selective for MAO-A and used as antidepressants do not produce the ‘cheese effect’. High levels of dietary tyramine are able to displace these inhibitors from the enzyme, making it available for the degradation of at least some of the tyramine (Tipton 1990).
Provocation of Anxiety States in Humans and its Possible Significance for the Pathogenesis of These Disorders
Published in Siegfried Kasper, Johan A. den Boer, J. M. Ad Sitsen, Handbook of Depression and Anxiety, 2003
Richard Balon, Robert Pohl, Vikram K Yeragani, Ravi K. Singareddy
Pretreatment with alprazolam, but not with clonidine, significantly reduced the rebreath-ing-induced increase in anxiety [156]. The anxiogenic effect of rebreathing 5% CO2 was significantly reduced in six patients after long-term imipramine treatment [157], a finding consistent with an increase of noradrenergic function in CO2-induced anxiety. Furthermore, alprazolam [158] and similarly clonazepam [159] blocked the 35% CO2-provoked panic in PD patients. Various antidepressants (mostly imipramine) or cognitive-behavioral therapy (CBT) reduced CO2 sensitivity in PD patients in a study by Gorman and colleagues [160]. Three other antidepressants, toloxatone (monoamine oxidase type A inhibitor) [161], fluoxetine [162], and citalopram [163] also significantly reduced 35% CO2 reactivity in PD patients. CBT was successful in reducing the sensitivity to 35% CO2 in PD patients in a study by Schmidt and colleagues [164]. Thus, treatments usually successful in the treatment of PD are also successful in blocking the effect of CO2 in PD patients.
Review on Chemistry of Oxazole derivatives: Current to Future Therapeutic Prospective
Published in Egyptian Journal of Basic and Applied Sciences, 2023
Sweta Joshi, Meenakshi Mehra, Ramandeep Singh, Satinder Kakar
Heterocyclic compounds are extensively used for therapeutic purpose, research areas and industries. Heterocycle containing nitrogen and oxygen atoms are a vital class of compounds in the medicinal chemistry. There has been interest in the biology and chemistry of heterocyclic molecules for researchers from decades, and oxazole moiety has become popular in the last few years considering its increasing relevance in the area of medicinal chemistry [1]. Oxazole contains two unsaturation in a five-membered ring including A carbon atom supports a nitrogen atom at position 3 and an oxygen atom at position 1, respectively [2]. The structure of oxazole derivatives exerts divergent weak interactions like hydrophobic effect, Vanderwaals force, hydrogen bonds, coordination bonds, ion-dipole and pi-pi bond; hence the derivatives exhibit potential application in agricultural, biotechnology, medicinal, chemical and material sciences [3]. From past, an immense number of oxazole derived medicinal agents have been used clinically shown on compounds (1–6) (Figure 1), such as Linezolid, Furazolidone, Toloxatone, Oxaprozin, Ditazole, and Aleglitazar [4].
Morpholine-based chalcones as dual-acting monoamine oxidase-B and acetylcholinesterase inhibitors: synthesis and biochemical investigations
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Rani Sasidharan, Bo Hyun Eom, Jeong Hyun Heo, Jong Eun Park, Mohamed A. Abdelgawad, Arafa Musa, Nicola Gambacorta, Orazio Nicolotti, Sreedharannair Leelabaiamma Manju, Bijo Mathew, Hoon Kim
MAO-A, MAO-B, AChE and BChE activities were measured after exposure to inhibitors at a concentration of 10 µM. Inhibitions of MAO-B at 10 µM of these compounds tested were too excessive, and thus, a concentration of 1.0 µM was used. IC50 values were determined by measuring the residual enzyme activities. Toloxatone, lazabemide and tacrine, were used as reference reversible inhibitors of MAO-A, MAO-B and AChE, respectively, and clorgyline and pargyline as reference irreversible inhibitors of MAO-A and MAO-B, respectively. Ki values and inhibitor types were determined by kinetic testing, as previously described50. Kinetic tests were conducted at 5 different substrate concentrations, and the inhibitor concentrations used were 0, ∼1/2 × IC50, IC50, and 2 × IC50 values. Lineweaver–Burk plots and their secondary plots were used to determine Ki values and inhibitor types.
The pharmacodynamic profile of “Blackadder” blackcurrant juice effects upon the monoamine axis in humans: A randomised controlled trial
Published in Nutritional Neuroscience, 2020
Anthony W. Watson, Arjan Scheepens, David O. Kennedy, Janine M. Cooney, Tania M. Trower, Crystal F. Haskell-Ramsay
Monoamine oxidase enzyme isoforms -A and -B are present in the periphery and the central nervous system and play a major role in the metabolism of both dietary and endogenous monoamines8. MAO-A preferentially catalyses the oxidation of serotonin; MAO-B is more active towards β-phenylethylamine and benzylamine; whereas dopamine, adrenaline, noradrenaline tryptamine and tyramine are oxidised by both isoforms9. Inhibition of MAO therefore results in an increased concentration of monoamine neurotransmitters and, in the case of MAO-B inhibition, is well documented as a therapeutic treatment for Parkinsonian symptoms10. Monoamine inhibition can be reversible or irreversible and can either act non-selectively, affecting both isoforms, or selectively, affecting only one isoform. For example, phenelzine is an irreversible, non-selective MAO inhibitor, which inhibits both MAO-A and B for up to three weeks11; in contrast, toloxatone, a reversible inhibitor of MAO-A (RIMA), inhibits MAO-A for only six hours before activity returns to baseline values12. This selective inhibition is preferable as the inhibition of both MAO isoforms can in some instances prevent the degradation of dietary amines in the digestive tract and if this continues for prolonged periods tyramine can accumulate to dangerous levels, potentiating a hypertensive crisis. It is therefore important to identify reversible and/or selective MAO inhibitors.