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Restrict the search for
acetylcholine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
SRT1720 is a small-molecule compound, which has the ability of activating the sirtuin subtype SIRT1. It’s not a direct activation. SRT1720 exhibits multiple off-target activities against receptors, enzymes, transporters, and ion channels. SRT1720 affects mitochondrial respiration in a Sirt1- and PGC-1α-dependent manner. SRT1720 has been demonstrated to enhance insulin sensitivity and improve measures of mitochondrial capacity and oxidative metabolism. SRT1720 also significantly inhibits VEGF-dependent multiple myeloma cell migration. SRT1720 is an experimental drug that was studied by Sirtris Pharmaceuticals. At 2013 year, GlaxoSmithKline was closed down Cambridge, MA-based Sirtris Pharmaceuticals.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Targeting alpha7 neuronal acetylcholine receptors (nAChRs) with selective agonists and positive allosteric modulators (PAMs) is considered a therapeutic approach for managing cognitive deficits in schizophrenia and Alzheimer's disease. A-867744 is a novel type II positive allosteric modulator of α7 nAChR, which was developed by Abbott Laboratories, and has a good potency and selectivity.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Isopteropodine is an Uncaria pentacyclic oxindol alkaloid. It is exhibited antibacterial activity against Gram-positive bacteria. The moderate anti-proliferative effect of isopteropodine was demonstrated on the acute lymphoblastic leukaemia cells. Isopteropodine positively modulate the function of rat muscarinic M1 and 5-HT2 receptors expressed in Xenopus oocyte but further studies are necessary to elucidate the exact mechanism by which isopteropodine positively modulates muscarinic M1 and 5-HT2 receptor functions. Isopteropodine blocked the impairment of passive avoidance performance caused by the nicotinic receptor antagonist mecamylamine and the N-methyl-D-aspartate (NMDA) receptor antagonist (+/-)-3-(2-carboxypiperazin-4-yl)- propyl-1-phosphonic acid (CPP) in mouse model. Moreover, it is possible that the glutamatergic systems are implicated in the anti-amnesic effect of isopteropodine.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
A-844606 is a selective α7 nicotinic acetylcholine receptor (nAChR) partial agonist (EC50 values are 1.4 and 2.2 μM at human and rat receptors respectively). Displays no measurable effect on α4β2 nAChRs. Stimulates α7 nAChR-induced ERK1/2 phosphorylation in PC12 cells. A-844606 is being investigated as the drug potentially usefull in the treatment of cognition disorders.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Bupropion is an atypical antidepressant that also has usefulness as a smoking-cessation aid. Because hydroxybupropion, a major metabolite of bupropion, is believed to contribute to its antidepressant activity, this metabolite may also contribute to the smoking-cessation properties of bupropion. Compared to bupropion hydroxybupropion inhibit norepinephrine (NE) uptake with similar potency. The effects of bupropion and enantiomers of hydroxybupropion on human nAChR subtypes indicate that the (2S,3S) isomer is more potent than the (2S,3R) isomer or racemic bupropion as an antagonist of alpha(4)beta(2) subtypes of nicotinic acetylcholine receptor (nAChR). In addition, both isomers of hydroxybupropion possess weaker antagonist activity to the alpha3/beta4 and alpha4/beta4 subtypes of nAChR.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
PNU-282987 is a potent and selective a7 nAChR agonist. This compound showed high affinity for the rat a7 nAChR (Ki = 26 nM) and activity at the a7–5-HT3 chimera (EC50 = 128 nM). In addition, PNU-282987 was found to be inactive at all tested monoamine, muscarine, glutamate, and GABA receptors at 1 uM concentration, except 5-HT3 receptors (Ki = 930 nM). The highly selective and potent a7 nAChR agonist PNU-282987 enhances GABAergic synaptic activity in the hippocampus in vitro, and reverses amphetamine induced auditory gating deficit in anesthetized rats. In addition, PNU-282987 improves the inherent gating deficit observed in a subset of rats and enhances amphetamine induced hippocampal activity. These results support the concept that a7 nAChR agonists represent a novel, potential pharmacotherapy in treatment of schizophrenia. It also has being shown that acute lung injury is reduced by PNU-282987 through changes in the macrophage profile.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Status:
Other
Class (Stereo):
CHEMICAL (MIXED)
Conditions:
Delsoline is a Nicotinic receptor antagonist, ganglion blocker; exhibits weak affinity at brain α-bungarotoxin-sensitive nicotinic acetylcholine receptors.
