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Journal: NLX-101, a cortical 5-HT receptor biased agonist, reverses scopolamine-induced deficit in the delayed non-matching to position model of cognition. (Pubmed Central) - Jan 26, 2022 Moreover, NLX-101 (0.04 and 0.16 mg/kg) dose-dependently and significantly opposed scopolamine-induced impairment for 5 and 10 s delays, with near-total reversal at 10 s. The acetylcholinesterase inhibitor, tacrine, also opposed scopolamine-induced impairment but was less potent and efficacious, with a single significant effect at 2.5 mg/kg and 5 s delay only. The present data suggest that biased agonism at post-synaptic, cortical 5-HT receptors could prove useful in neurological or neuropsychiatric pathologies characterized by cognitive deficits consecutive to a reduced central cholinergic tone.
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Preclinical, Journal: Odour Retrieval Processing in Mice: Cholinergic Modulation of Oscillatory Coupling in Olfactory Bulb-Piriform Networks. (Pubmed Central) - Jan 18, 2022 In conclusion, FYDWPK alleviated cognitive and memory impairments by regulating oxidative imbalance, reducing cholinergic dysfunction, and relieving pathological alterations. The results suggest that the acquisition and formation of odour reference memory rely primarily on FC at the OB-PC network and confirm the role of muscarinic receptors in olfactory retrieval processing.
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Preclinical, Journal: Sea Cucumber Peptides Attenuated the Scopolamine-Induced Memory Impairment in Mice and Rats and the Underlying Mechanism. (Pubmed Central) - Jan 14, 2022 SCP repaired damaged neuronal cells, enhanced the Nissl body number, increased the unsaturated lipid level, and activated the long-term potentiation (LTP) pathway (p-CaMKII, p-CREB, and BDNF), both in the mouse and rat hippocampus. The results indicated that SCP upregulated the LTP pathway and unsaturated lipid level to combat scopolamine-induced memory impairment, suggesting that SCP was a potential candidate for neurological recovery.
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PK/PD data, Journal: Skin Pharmacokinetics of Transdermal Scopolamine: Measurements and Modeling. (Pubmed Central) - Jan 11, 2022 The scopolamine concentration versus time profiles in SC and VT skin compartments, in vitro and in vivo, taken together with IVRT release and IVPT penetration kinetics, reflect the input rate and drug delivery specifications of the Scopoderm transdermal patch and reveal the importance of skin binding with respect to local drug disposition. Further data analysis and skin PK modeling are indicated to further refine and develop the approach outlined.
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Preclinical, Journal: Inhalation Administration of Agarwood Incense Rescues Scopolamine-Induced Learning and Memory Impairment in Mice. (Pubmed Central) - Jan 11, 2022 The other four treatment groups all showed improvements in these indicators, and the overall therapeutic effect of agarwood was superior. The inhalation administration of agarwood can significantly improve the learning and memory impairment caused by scopolamine in mice, and the therapeutic effect varied between doses.
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Preclinical, Journal: Therapeutic Effect of Novel Cyanopyrrolidine-Based Prolyl Oligopeptidase Inhibitors in Rat Models of Amnesia. (Pubmed Central) - Jan 11, 2022 We evaluated protective effects of the cyanopyrrolidine-based POP inhibitors using scopolamine- and maximal electroshock-induced models of amnesia in rats and showed that BocTrpPrdN, BocGlyPrdN, CbzMetPrdN, and CbzGlnPrdN significantly prolonged conditioned passive avoidance reflex (CPAR) retention time when administered intraperitoneally (1 and 2 mg/kg) before evaluation in both models of amnesia, although CbzAlaPrdN was not effective in scopolamine-induced amnesia. Our data support previous reports on the antiamnesic effects of prolinal-based POP inhibitors and indicate an important role of POP in the regulation of learning and memory processes in the CNS.
- |||||||||| hyoscine butylbromide oral / Generic mfg., galantamine hydrobromide / Generic mfg.
Preclinical, Journal: Effects of New Galantamine Derivatives in a Scopolamine Model of Dementia in Mice. (Pubmed Central) - Jan 7, 2022 Results show that Gal 43, Gal 44, and, in particular, Gal 46 are especially effective in improving both short- and long-term memory and in the case of Gal 46 having a significant effect on exploratory activity as well. Although Gal 34 did not show behavioral effects as convincing as those of the other three galantamine derivatives, it demonstrated persuasive antioxidant and restorative capacities, making all four galantamine derivatives promising AD treatment agents and prompting further research, especially that in many of our studies they performed better than galantamine.
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Journal: Sex differences shape zebrafish performance in a battery of anxiety tests and in response to acute scopolamine treatment. (Pubmed Central) - Jan 4, 2022 Overall, we report high baseline anxiety-like behavior and more individual variability in locomotion in female zebrafish, as well as distinct, sex-specific (anxiolytic-like in females and anxiogenic-like in males) effects of scopolamine. Collectively, these findings reinforce the growing importance of zebrafish models for studying both individual and sex differences in behavioral and pharmacological responses.
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Preclinical, Journal: Ficus erecta Thunb Leaves Alleviate Memory Loss Induced by Scopolamine in Mice via Regulation of Oxidative Stress and Cholinergic System. (Pubmed Central) - Dec 30, 2021 Our findings indicate that the mechanisms of neuroprotection and antioxidation of EEFE are regulated by the cholinergic system, promotion of cAMP response element-binding protein (CREB) phosphorylation, and the nuclear factor erythroid-2-related factor 2 (Nrf2)/heme oxygenase (HO)-1 signaling activation. The current study proposes that EEFE could be an encouraging plant resource and serve as a potent neuropharmacological drug candidate against neurodegenerative diseases.
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Preclinical, Journal: Tilapia Head Protein Hydrolysate Attenuates Scopolamine-Induced Cognitive Impairment through the Gut-Brain Axis in Mice. (Pubmed Central) - Dec 27, 2021 In addition, THPH administration maintained the stability of cholinergic system, alleviated oxidative stress and further improved the cognitive impairment by reshaping the gut microbiota structure of scopolamine-induced mice and alleviating the disorder of lipid metabolism and amino acid metabolism in serum. In conclusion, our research shows that THPH supplementation is a nutritional strategy to alleviate cognitive impairment through the gut-brain axis.
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Journal: Novel Antimuscarinic Antidepressant-like Compounds with Reduced Effects on Cognition. (Pubmed Central) - Dec 25, 2021 Significance Statement Some clinical studies with the muscarinic antagonist scopolamine document its ability to produce antidepressant effects in patients with mood disorders; however, scopolamine also has well-known adverse effects on both autonomic and centrally-mediated physiological functions that limit its therapeutic use. Here, we characterize the cardiovascular and discriminative stimulus effects of two novel muscarinic antagonists, L-687,306 and CJ2100, that produce antidepressant-like effects in a rodent model (forced swim test), without affecting touchscreen-based cognitive performance (titrating vigilance and delayed matching-to-position).
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Preclinical, Journal: Antidepressant-like effect of low dose of scopolamine in the H/Rouen genetic mouse model of depression. (Pubmed Central) - Dec 22, 2021 In addition, we showed this antidepressant-like effect was partly inhibited by an injection of 10 mg/kg of the AMPA receptor antagonist NBQX in both males and females, suggesting the antidepressant-like effect of scopolamine was mainly driven by AMPA receptors in the H/Rouen mouse line. Altogether, our results showed the high sensitivity of the H/Rouen mouse model of depression to study the antidepressant-like effects of pharmacological compounds.
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A POSITIVE MODULATOR OF NEUROTROPHIN RECEPTORS IMPROVES COGNITION AND MITOCHONDRIAL FUNCTION (Onsite - Hall E) - Dec 17, 2021 - Abstract #ADPD2022ADPD_432; Effects of AC-0027136 were investigated in vivo using scopolamine-induced or age-related memory impairment in a fear conditioning test...Conclusions We identified AC-0027136 as a positive modulator of neurotrophin receptors with beneficial effects on cognition and with promising properties as a mitochondrial enhancer in neurons. Our findings demonstrate that AC-0027136 act as a cognitive enhancer and improves mitochondrial function, which could be of importance for the treatment of neurodegenerative diseases characterized by reduced cognition and mitochondrial function.
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Preclinical, Journal: Effects of mirabegron on depression, anxiety, learning and memory in mice. (Pubmed Central) - Dec 17, 2021 Diazepam and mirabegron (3, 6 and 9 mg/kg) significantly increased the time spent in open arms and the number of entries to the open arms in elevated plus maze test...While scopolamine significantly increased the swimming speed, mirabegron (9 mg/kg) significantly decreased the swimming speed in scopolamine-treated mice. Mirabegron might be clinically useful for the treatment of OAB in elderly patients that should use drugs against depression and anxiety, without disrupt learning and memory.
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Journal: Neuroprotective effects of Sophora secundiflora, Sophora tomentosa leaves and formononetin on scopolamine-induced dementia. (Pubmed Central) - Dec 16, 2021 Formononetin, S. tomentosa and S. secundiflora leaves methanolic extract were evaluated in vivo for their neuroprotective activity where formononetin and S. tomentosa showed promising neuroprotective activity with reduction in acetylcholine esterase (AchE) enzyme activity and elevation of acetylcholine (Ach) and glutathione(GSH) brain levels and attenuation of dopamine (DA), nor-adrenaline (NA) and malonedialdehyde (MDA) brain level significantly, However S. secundiflora leaves methanolic extract didn't attenuate the AchE enzyme activity, DA and NA brain levels. [Formula: see text].
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Journal: Engineered Microbes for Anticholinergics Production. (Pubmed Central) - Dec 16, 2021 Many adverse factors such as climate fluctuations and pandemics can thus influence annual world production. Based on the landmark microbial production of the antimalarial semi-synthetic artemisinin, the Smolke group recently developed a yeast cell factory capable of de novo synthesizing hyoscyamine and scopolamine, thus paving the way for an alternative production of these compounds.
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Preclinical, Journal: Neurochemical and Behavioral Effects of a New Hallucinogenic Compound 25B-NBOMe in Rats. (Pubmed Central) - Dec 16, 2021 The effect of 25B-NBOMe in the NOR test was inhibited by scopolamine...The changes in neurotransmitter levels may be related to 25B-NBOMe affinity for 5-HT receptor. Alterations in the NOR, OF, and LDB indicate that 25B-NBOMe impacts short-term memory, locomotion, and may be anxiogenic.
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Preclinical, Journal: Tadalafil Reversed H-89 - and Scopolamine - Induced Spatial Learning Impairments in Male Rats. (Pubmed Central) - Dec 16, 2021 But, combination of tadalafil/H-89 or tadalafil/scopolamine reversed H-89 or scopolamine- induced spatial learning deficits in MWM. Taken together, these results showed the probable regulatory effects of cGMP on cholinergic and cAMP/PKA signaling pathways in co-administrations of these mentioned drugs on spatial learning in MWM.
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