Semax, synthetic ACTH(4–10) analogue, attenuates behavioural and neurochemical alterations following early-life fluvoxamine exposure in white rats

Glazova, N. Yu.; Manchenko, D. M.; Володина, М. А.; Merchieva, S. A.; Andreeva, L. A.; Кудрин, В. С.; Myasoedov, N. F.; Levitskaya, N. G.

doi:10.1016/j.npep.2020.102114

Neuropeptides

2021

DOI: 10.1016/j.npep.2020.102114

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Semax, synthetic ACTH(4–10) analogue, attenuates behavioural and neurochemical alterations following early-life fluvoxamine exposure in white rats

N. Yu. Glazova

D. M. Manchenko

М. А. Володина

et al.

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Cited by 4 publications

(2 citation statements)

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“…Semax has no hormonal activity and retains a significant part of the spectrum of neurotropic effects of natural melanocortins. The heptapeptide Semax is a synthetic analogue of ACTH (4-10) which exerts marked nootropic and neuroprotective activities [15], protects effectively the brain against ischemic stroke [14]. Semax promotes the survival of neurons during glutamate excitotoxicity [16], protects against the optic nerve atrophy and optic neuritis of inflammatory or toxic-allergic etiology [17].…”

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confidence: 99%

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Correction of hypertensive retinal changes in rats with Semax

Lugovskoy¹,

Chernyaeva²,

Peresypkina³

et al. 2021

RRB

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Currently, there are no drugs for the specific treatment of hypertensive retinal changes. The main therapy is for the treatment of a systemic disease – hypertensive disease. Therefore, the search for ways of specific pharmacological correction of hypertensive retinal changes is of great interest. The aim of the study: To evaluate the correction possibility of retinal injuries with Semax in a rat model of hypertensive neuroretinopathy. Materials and methods: The model was performed by injection of N-nitro-L-arginine methyl ester (L-NAME) at a dose of 1.25 mg/100 g of rat mass within 28 days and a single increase in intraocular pressure (IOP) to 110 mmHg for 5 min. The retinoprotective effect of Semax at a dose of 7.2 μg/100 g of rat mass, in comparison with Picamilon at a dose of 3 mg/100 g of rat mass, was estimated by laser Doppler flowmetry (LDF) and electroretinography (ERG). Results: The use of Semax led to an increase in retinal perfusion by 62.7%, p < 0.05, in comparison with the group with the model, and by 9.9%, p < 0.05, in comparison with Picamilon; an increase in the b/a coefficient by 31.4% in comparison with the group with the model, p < 0.05, and by 14.6%, p < 0.05 in comparison with Picamilon. Conclusion: The neuroretinoprotective effect of Semax in correction of hypertensive retinal changes in rats may be due to the presence of neuroprotective, neurometabolic, antioxidant and endothelioprotective effects in Semax. Thus, Semax can be a promising agent in hypertensive neuroretinopathy treatment.

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confidence: 99%

“…The effect of Semax and PGP previously was shown on the expression of genes that encode neurotrophic factors and their receptors in a model of brain ischemia in rats [20]. However, despite the advances described above, the molecular mechanisms underlying the Semax neuroprotective action and the degree of PGP participation in them remain obscure [15].…”

mentioning

confidence: 99%

Correction of hypertensive retinal changes in rats with Semax

Lugovskoy¹,

Chernyaeva²,

Peresypkina³

et al. 2021

RRB

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P.0038 Adrenocorticotropic hormone (4-10) analogue semax attenuates the effects of neonatal antidepressant fluvoxamine exposure on the social behaviour in pre-adolescent rats

Monicheva

Glazova

Manchenko

et al. 2021

European Neuropsychopharmacology

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Propranolol as a Model Drug to Treat Smoking Cessation and its Formulation as a Transdermal Patch for Effective Management

Mohapatra¹,

Srivastava²,

Varshney³

et al. 2023

LDDD

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Background: Smoking causes cancer, breathing problems, heart attacks, and stroke and can lead to asthma and breathing problems. Nicotine replacement therapy (NRT) is considered one of the most widely accepted methods to quit smoking. However, it can lead to relapsed physical and psychological dependence. Aim: The present study aimed to explore propranolol, as a model drug to treat relapsed physical and psychological dependence due to NRT in smoking cessation. Furthermore, for its effective management, the transdermal drug delivery system has opted for effective and long-term release of propranolol. Material and Method: The molecular association of propranolol with eight different potential targets, namely, Acetylcholine Binding Protein (AChBP), Cannabinoid Receptor, CB1 and CB2, Monoamine oxidase (MAO), human dopamine D3 receptor, kainite, Leu- biogenic amine transporters (BAT) and α-type peroxisome proliferator-activated receptor were studied via molecular simulation models. Polymeric films containing propranolol HCI were prepared and evaluated to select a suitable formulation for developing transdermal drug delivery systems (TDDS). Films containing different ratios of HPMC K4M, HPMC 15M, and Sodium CMC were prepared by the solvent evaporation technique using PEG 4000 incorporated as a plasticizer, and SLS was used to act as a penetration enhancer. Manufactured transdermal films were physically evaluated for thickness, weight uniformity %, moisture content %, moisture uptake %, drug content %, and folding endurance. Result: Results indicated that propranolol can interact with all eight receptors at the active binding site. It was found to show considerable interaction with Acetylcholine Binding Protein (AChBP), MAO, human dopamine D3 receptor, kainite, and Leu- biogenic amine transporters (BAT) with the binding energy of -6.27, -6.74, -7.07, -6.84, and -6.63 kcal/mol respectively. The release rate of propranolol HCI decreased linearly with increasing polymer concentration in the film and depended on the film thickness. In contrast, the quantity of drug release was proportional to the square root of time. Kinetic data based on the release exponent, ‘n’ in the Peppas model showed that n values were between 0.95 and 1.08, indicating that drug release from polymer matrix was predominantly by diffusion with swelling. Conclusion: Transdermal drug delivery of propranolol could act as a potential regulator of all studied targets associated with physical and psychological dependence associated with NRT and smoking cessation. Furthermore, propranolol loaded transdermal patches with optimized release could be utilized to deliver the drug with optimum bioavailability for a considerable time.

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Semax, synthetic ACTH(4–10) analogue, attenuates behavioural and neurochemical alterations following early-life fluvoxamine exposure in white rats

Cited by 4 publications

References 78 publications

Correction of hypertensive retinal changes in rats with Semax

Correction of hypertensive retinal changes in rats with Semax

P.0038 Adrenocorticotropic hormone (4-10) analogue semax attenuates the effects of neonatal antidepressant fluvoxamine exposure on the social behaviour in pre-adolescent rats

Propranolol as a Model Drug to Treat Smoking Cessation and its Formulation as a Transdermal Patch for Effective Management

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