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Restrict the search for
acetylcholine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Lobelanidine is one of lobelia alkaloids that are the constituents of Lobelia inflata. Lobelia Chinensis Lour. (L. chinensis) is a plant of the Campanulaceae family that is commonly known as "xi-mi-cao", and "she-she-cao". It has been widely used as an antidote, diuretic, and hemostat in traditional Chinese medicine for decades. Lobelanidine is known for its emetic and anticancer activity.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
3.beta-3-[2-(Diethylamino)ethoxy]androst-5-en-17-one hydrochloride or U18666A, an amphipathic cationic amine, is a cell permeable research tool drug that inhibits cholesterol synthesis and trafficking, and also a weak inhibitor of hedgehog (Hh) signaling. U18666A had been used in several models both in vivo and in vitro to mimic Niemann-Pick type C disease (NPC) and for assessing the importance of molecular trafficking through the lysosomal pathway in other conditions such as atherosclerosis, Alzheimer's disease, and prion infections. U18666A also provided animal models for such disorders as petite mal (absence) epilepsy and cataracts. U18666A inhibits the enzyme desmosterol reductase responsible for reducing the desmosterol in cholesterol biosynthesis, and also blocks LDL-(low density lipoprotein) cholesterol transport from the lysosomes into the endoplasmic reticulum thereby increasing the level of caveolina-1 located within the plasma membrane caveolae. U18666A was shown to be a potent antagonist of alpha4beta2 neuronal nicotinic acetylcholine receptors and may be useful as a tool in the functional characterization and pharmacological profiling of nAChRs.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
(-)-vesamicol is an active enantiomer of vesamicol (AH5183 or [(-)-trans-2-(4-phenylpiperidino)cyclohexanol]). It inhibits the uptake of acetylcholine into cholinergic neuronal storage vesicles. Vesicular acetylcholine transporter (VAChT) is inhibited by (-)-vesamicol, which binds tightly to an allosteric site.
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 (UNKNOWN)
Targets:
Conditions:
Strychnine-N-oxide is the major metabolite of Strychnine. Strychnine, the major alkaloid present in $trychnos:nuxypmicagseeds has been reported to stimulate
the entire central nervous system with preference for the
spinal cord. It is a powerful convulsant and because of
this property, it is an important pharmacological tool as
it plays a unique role as an inhibitor of post synaptic
inhibitory impulses. It is useful to study inhibitory
transmitter and receptor types. However, because of its
extreme toxicity, strychnine does not have any therapeutic
application in the Western system of medicine. Strychnine-N-oxide is less toxic and less convulsive than strychnine itself. However, strychnine N-oxide is not
being used as a therapeutic agent now probably because of the threat of convulsions at higher doses. Strychnine-N-oxide is a muscarinic allosteric agent.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Muscarine or muscarin, a water-soluble toxin, which initially was isolated from the mushroom species Amanita muscar. Muscarine mimics the action of the acetylcholine by binding to the muscarinic acetylcholine receptors and acts as an agonist.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
A-582941 was found to exhibit high-affinity binding and agonism at alpha-7 nicotinic acetylcholine receptor (α7-nAChR), with acceptable pharmacokinetic properties and excellent distribution to the central nervous system. In vitro and in vivo studies indicated that A-582941 activates signaling pathways known to be involved in cognitive function such as ERK1/2 and CREB phosphorylation. A-582941 enhanced cognitive performance in behavioral assays including the monkey delayed matching-to-sample, rat social recognition, and mouse inhibitory avoidance models that capture domains of working memory, short-term recognition memory, and long-term memory consolidation, respectively. AbbVie is developing α7-nAChR agonists including A-582941 as neuroprotective agents for the treatment of cognitive disorders such as Alzheimer's disease and schizophrenia. Development is at the preclinical stage.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Dihydro-β-erythroidine is a competitive nicotinic acetylcholine receptor antagonist with moderate selectivity for the neuronal α4 receptor subunit. Dihydro-β-erythroidine have curare-like effects at peripheral nicotinic receptors, which include severe respiratory depression. Thus in vivo behavioral studies using Dihydro-β-erythroidine are limited. Dihydro-β-erythroidine antagonizes behavioral effects of nicotine in vivo. After s.c. administration, Dihydro-β-erythroidine was potent in blocking nicotine's effects except for antinociception. Intrathecal injection of Dihydro-β-erythroidine was effective in blocking the antinociceptive effect of nicotine.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
(-)-vesamicol is an active enantiomer of vesamicol (AH5183 or [(-)-trans-2-(4-phenylpiperidino)cyclohexanol]). It inhibits the uptake of acetylcholine into cholinergic neuronal storage vesicles. Vesicular acetylcholine transporter (VAChT) is inhibited by (-)-vesamicol, which binds tightly to an allosteric site.
