scopolamine

Methscopolamine (Hyoscine methyl bromide) (Pamine), as a natural plant alkaloid, is a muscarinic acetylcholine receptor blocker.

Tropine is a secondary metabolite of the Solanaceae family of plants and is an anticholinergic reagent. It is a common intermediate used in the synthesis of various biologically active alkaloids (e.g. hyoscyamine, scopolamine).

TZ3O is an anticholinergic compound with neuroprotective activity.TZ3O ameliorates memory impairment and cognitive decay in Scopolamine-induced Alzheimer's type model in rats, and can be used in the study of Alzheimer's disease.

RU 47213 can be used to inhibit scopolamine-induced working memory impairment in rats.

SAK3 is a novel modulator of nAChR activity that enhances T-type voltage-gated Ca2+ channel (T-VGCC) activity, and has potentiating effects on both Cav3.1 and Cav3.3 T-type Ca2+ channel currents.SAK3 is neuroprotective against scopolamine-induced cholinergic dysfunction in human neuroblastoma SH-SY5Y cells.SAK3 is used for the study of memory deficits and Alzheimer's disease. SAK3 can be used to study memory deficits and Alzheimer's disease.

Anisodamine (6-beta-Hydroxyhyoscyamine) is an antagonist of muscarinic and nicotinic cholinoceptor with similar affinities at the muscarinic receptor as scopolamine and atropine. Anisodamine improve the microcirculation in states of shock and can be used in studies about organophosphate poisoning.

Norscopolamine is a natural product

Suffruticosol A, a neuroprotective compound isolated from the seeds of P. lactiflora [1], mitigates scopolamine-induced neurodegenerative cellular damage and improves hippocampal cholinergic function. Additionally, it partially boosts BDNF signaling and has neuromodulatory effects, leading to the restoration of memory and cognitive performance in a scopolamine-induced mouse model.

Tropine is a secondary metabolite of the Solanaceae family of plants and is an anticholinergic reagent. It is a common intermediate used in the synthesis of various biologically active alkaloids (e.g. hyoscyamine, scopolamine).

PZ-1922 (Compound 16), able to cross the blood-brain barrier, is a dual antagonist for 5-HT6R and 5-HT3R with K i values of 17 nM and 0.45 nM, respectively. It also reversibly inhibits MAO-B with a pIC50 of 8.93. Moreover, PZ-1922 mitigates scopolamine (SCOP)-induced memory deficits in rats as observed in the novel object recognition (NOR) test and hinders Aβ-induced memory impairment in the T-maze test [1].

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg/kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg/kg and prevents memory deficits induced by the AMPA/kainate glutamate receptor antagonist NBQX at 0.1 mg/kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

TZ4M, a 2,4-thiazolidinedione (TZD)-based anti-ADV agent, exhibits neuroprotective effects and acetylcholinesterase (AChE) inhibition in human plasma. It enhances memory and cognitive function in adult rats within a scopolamine-induced Alzheimer-type model [1].

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy[1]. Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons[1]. Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine[1]. [1]. Etherington LA, et al. Selective inhibition of extra-synaptic α5-GABAA receptors by S44819, a new therapeutic agent. Neuropharmacology. 2017;125:353-364.

Vitisin A ((+)-Vitisin A) is a resveratrol tetramer that can be isolated from the roots of Vitis vinifera and possesses antioxidant, anticancer, antiapoptotic, neuroprotective, and anti-inflammatory activities.It ameliorates the impaired learning and memory functions of scopolamine-induced amnesia in ICR mice, and can be used in the study of degenerative diseases.

Rivanicline hemioxalate, also known as RJR-2403 hemioxalate or (E)-Metanicotine hemioxalate, is a chemical compound acting as a neuronal nicotinic receptor agonist with pronounced selectivity for the α4β2 receptor subtype, showing over 1,000-fold greater selectivity for this subtype (Ki=26 nM) compared to α7 receptors (Ki=3.6 μM). Its in vitro studies demonstrate no significant activation of nAChRs in PC12 cells, muscle type nAChRs, or muscarinic receptors at concentrations up to 1 mM. Furthermore, Rivanicline displayed less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy, and failed to antagonize nicotine-induced stimulation of muscle or ganglionic nAChR functions, with an IC50 value greater than 1 mM. Chronic exposure to Rivanicline at 10 microM led to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine. In vivo studies revealed that Rivanicline significantly reversed scopolamine-induced amnesia and improved working and reference memory in a rat model, while being 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses. Metanicitone’s potency was approximately five times lower than nicotine in tail-flick tests following subcutaneous administration, yet slightly more potent upon central administration.

p-fin4 is a peptide inhibitor targeting the interaction between STEP Phosphatase and GluA2 AMPA receptor, exhibiting a Ki of 0.4 μM. This compound has been shown to reverse memory deficits and exert anxiolytic and antidepressant effects in scopolamine-treated rats, suggesting its potential as a lead compound for developing novel cognitive enhancers and behavioral modulators [1].

Aniracetam (Ro 13-5057)(Ro 13-5057), a nootropic and neuroprotective drug, selectively modulates the AMPA receptor and nAChR.

Soyasaponin Ba may represent viable candidates for effective vaccine adjuvants due to their higher and lower or non-haemolytic effects.Soyasaponins Ab and Bb prevent scopolamine-induced memory impairment in mice without the inhibition of acetylcholinester

Tenuifoliside B is a natural product from the roots of Polygala tenuifolia.And is a target lactate dehydrogenase inhibitor. Tenuifoliside B has cognitive improving and cerebral protective effects. it can inhibit potassium cyanide (KCN)-induced hypoxia and scopolamine-induced memory impairment in mice.

Littorine is a tropane alkaloid found in a variety of plants including Datura and Atropa belladonna. It is closely related in chemical structure to atropine, hyoscyamine, and scopolamine, which all share a common biosynthetic pathway.

PD07 is an orally active acetylcholinesterase (AChE) inhibitor, exhibiting an IC50 of 0.29 μM against human AChE, and demonstrates inhibition of cholinesterases (ChEs), β-site amyloid precursor protein cleaving enzyme 1 (BACE1) with an IC50 of 13.42 μM, as well as Aβ1–42 aggregation in vitro. Additionally, PD07 possesses antioxidant properties with a DPPH radical inhibition IC50 value of 26.46 μM and has been shown to ameliorate memory and cognitive deficits in scopolamine-induced amnesic rats. This compound is relevant for Alzheimer’s disease research [1].

5-HT6R/MAO-B modulator 1 is an antagonist of 5-HT6R at Gs signaling and an irreversible inhibitor of MAO-B that exhibits glial protective activity. 5-HT6R/MAO-B modulator 1 exhibits induction of scopolamine-induced memory deficits.

Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and mechanical stimulation in a rat model of carrageenin-induced inflammation when administered at a dose of 2 nmol injected into the nucleus accumbens.[3][4] Galanin (5 μg, i.c.v.) also inhibits acetylcholine release induced by scopolamine in the ventral hippocampus of freely moving rats. [5]

Enerisant (TS-091) is an orally active, selective and potent histamine H3 receptor antagonist that modulates histamine H3 receptors in mice in a dose-dependent manner.Enerisant promotes pro-cognitive effects and reverses scopolamine-induced cognitive deficits.

p3Ysh-3, a peptide inhibitor targeting the STEP Phosphatase-GluA2 AMPA receptor interaction, exhibits a Ki of 1.09 μM. It effectively reverses memory deficits and demonstrates anxiolytic and antidepressant effects in scopolamine-treated rat models, positioning itself as a promising lead compound for the development of novel cognitive enhancers and behavioral modulators [1].