acetylcholine,alzheimer's

SIB 1553A is an orally available and selective agonist of nicotinic acetylcholine receptors (nAChRs), which are subtype-selective ligands for nicotinic acetylcholine receptors.SIB-1553A is a cognitive enhancer that may be used in the study of neurodegenerative-related diseases such as Alzheimer's disease.

SCH 57790 is a novel and selective muscarinic M(2) receptor antagonist that releases acetylcholine and enhances cognition in experimental animals for the treatment of Alzheimer's disease.

JNJ-39393406 is an α7 nicotinic acetylcholine receptor positive allosteric modulator for the study of tobacco dependence and Alzheimer's disease.

SIB-1553A hydrochloride is an orally available, selective nicotinic acetylcholine receptor agonist and a selective neuronal nAChR ligand.SIB-1553A hydrochloride enhances cognition and may be useful in the study of Alzheimer's disease and cognitive impairment.

Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.

Arecoline is a natural alkaloid derived from areca nut in the palm family and is a potent nicotine and partial agonist of muscarinic acetylcholine receptors. Arecoline has anti-anxiety and anti-parasitic activity, can induce oxidative stress and can be used to study Alzheimer's disease and Alzheimer's disease.

sn-Glycero-3-phosphocholine (Choline glycerophosphate) is a natural choline compound found in the brain and in milk. It is also a parasympathomimetic acetylcholine precursor which may have a potential for the treatment of Alzheimer's disease and dementia. sn-Glycero-3-phosphocholine rapidly delivers choline to the brain across the blood–brain barrier and is a biosynthetic precursor of the acetylcholine neurotransmitter. It is a non-prescription drug in most countries due to its Generally Recognised As Safe (GRAS) status [1]. Studies have investigated its efficacy for cognitive disorders including stroke and Alzheimer's disease. An Italian multicentre clinical trial on 2, 044 patients suffering from recent stroke were supplied Glycerylphosphorylcholine in doses of 1, 000 mg day for 28 days and 400 mg three times per day for the five ensuing months. The trial confirmed the therapeutic role of alpha-GPC on the cognitive recovery of patients based on four measurement scales, three of which reached statistical significance [2].

VU0357017 hydrochloride (ML071 hydrochloride) is highly selective M1 agonists act at an allosteric site to activate the receptor (EC50: 477 ± 172 nM; Pec50: 6.37 ± 0.15).

Nebracetam hydrochloride (WEB 1881 FU hydrochloride) is an agonist nootropic M1-muscarinic. Nebracetam hydrochloride induces a rise of intracellular Ca2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca2+]i.

Lupanine ((+)-Lupanine), a naturally occurring quinolizidine alkaloid, potently affinity and activates nicotinic acetylcholine receptor (nAChR) (Ki=500 nM), and shows significant neuroprotection against soluble amyloid β-oligomers (SO-Aβ) toxicity in cellular models in association with the anti-apoptotic PI3K Akt Bcl-2 signaling pathway with anti-Alzheimer's disease potential. Improves glucose homeostasis by affecting KATP channels and enhancing insulin secretion with therapeutic potential for type 2 diabetes.

AZD1446 tosylate, also known as TC-6683, is a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders. AZD1446 tosylate showed favorable pharmaceutical properties and in vivo efficacy in animal models has been identified as a potential treatment for cognitive deficits associated with psychiatric or neurological conditions and had been evaluated in phase 2 clinical trials as a treatment for Alzheimer's disease.

Alpha-Conotoxin EIIB is a peptide toxin derived from Conus ermineus that selectively binds to neuronal nicotinic acetylcholine receptors (nAChR) with a dissociation constant (Ki) of 2.2 nM. This compound is utilized in neurological research, including the study of schizophrenia, drug addiction, Alzheimer's disease, and Parkinson's disease [1].

AZD1446 HCl, also known as TC-6683, is a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders. AZD1446 HCl showed favorable pharmaceutical properties and in vivo efficacy in animal models has been identified as a potential treatment for cognitive deficits associated with psychiatric or neurological conditions and had been evaluated in phase 2 clinical trials as a treatment for Alzheimer's disease.

SEN12333 is an α7 nicotinic acetylcholine receptor (nAChR) agonist

Blarcamesine (AVex-73) is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease.

Zanapezil (TAK-147) is a powerful and selective inhibitor of acetylcholine esterase (AChE). It demonstrates significant and reversible inhibition of AChE activity in rat cerebral cortex homogenates (IC50 = 51.2 nM). Furthermore, Zanapezil exhibits moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. This compound holds promise for the investigation of the initial stages of Alzheimer's disease (AD).

JTP-4819 is a potent and selective prolyl endopeptidase (PEP) inhibitor with potential for treating Alzheimer's disease. At nanomolar concentrations, it inhibited the degradation of substance P, arginine-vasopressin, and thyrotropin-releasing hormone by PEP in supernatants of the rat cerebral cortex and hippocampus. Repeated administration of JTP-4819 reversed the aging-induced decrease in brain substance P-like and thyrotropin-releasing hormone-like immunoreactivity, suggesting it may improve the imbalance of peptidergic neuronal systems that develops with senescence by inhibiting PEP activity. Additionally, JTP-4819 increased acetylcholine release from the frontal cortex and hippocampus, regions closely associated with memory, in both young and aged rats.

Dicyclomine hydrochloride is a muscarinic antagonist used as an antispasmodic and in urinary incontinence.

α-Glycosidase-IN-1 (compound MZ7) is a potent inhibitor of α-GLY (α-glycosidase) with an IC50 of 44.72 nM and a Ki of 44.74 nM. It also inhibits human carbonic anhydrase isozymes I (hCA I) and II (hCA II) with IC50 values of 104.87 nM and 100.04 nM, respectively, and acetylcholine esterase (AChE) with an IC50 value of 654.87 nM. α-Glycosidase-IN-1 is applicable in the study of diabetes, Alzheimer's disease, ulcers, heart failure, epilepsy, and various other diseases.

Lecozotan (SRA-333) is a potent and selective 5-HT antagonist developed for Alzheimer's disease treatment. This compound significantly increases the release of glutamate and acetylcholine in the hippocampus and dentate gyrus areas upon potassium ion stimulation, exhibiting cognitive enhancement properties. Long-term use of Lecozotan does not lead to tolerance or dysfunction of the 5-HT(1A) receptor, demonstrating its stable pharmacological properties. Additionally, acute administration can improve learning and memory abilities in rats without affecting their anxiety levels or behavior depression.

(S)-VQW-765 ((S)-AQW-051) is an orally active, selective, and effective partial agonist of the α7 nicotinic acetylcholine receptor (nAChR), with potential applications in treating cognitive disorders related to neurological diseases, including Alzheimer's disease and schizophrenia.

nAChR agonist 1 (DUN71755) is a brain-permeable and orally efficacious positive allosteric α7 nicotinic acetylcholine receptor (α7 nAChR)modulator.

Encenicline (EVP-6124) is a selective α7 nicotinic acetylcholine receptor (nAChRs) agonist being developed to treat cognitive impairment in schizophrenia and Alzheimer's disease.