Other Cholinergics

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C5923 (−)-Cotinine ≥98% Major metabolite of nicotine in humans.
C001 Acetylethylcholine mustard hydrochloride >97% (GC), powder Acetylethylcholine mustard is a precursor for ethylcholine mustard aziridinium ion (AF-64A); irreversible ligand for the high affinity choline transport system; specific presynaptic long action cholinotoxin; inhibitor of choline acetyl-transferase.
SML0318 Alvameline tartrate ≥97% (HPLC) Alvameline (Lu 25-109) is a muscarinic M1 receptor agonist and M2/M3 receptor antagonist that was under investigation for the treatment of Alzheimer′s disease. Alvameline (Lu 25-109) improved cognitive function following traumatic brain injury (TBI) in rats, but failed to show significant positive results in clinical trials.
A138 Aminobenztropine solid High affinity muscarinic ligand that has been used for affinity purification of muscarinic cholinergic receptors.
SML0497 BQCA ≥98% (HPLC) BQCA is a potent muscarinic M1 receptor positive allosteric modulator with selectivity for M1 over M2-M5. It potentiates M1 activity in in vitro and in vivo assays and is orally bioavailable. Muscarinic 1 (M1) receptors are expressed in brain regions responsible for attention and memory, including hippocampus, cortex, and striatum. BQCA binds allosterically to M1 to enhance the binding and efficacy of ACh at the receptor. M1 activation is a proposed mechanism for increasing information processing in disease states, such as Alzheimer′s. M1 agonists are being studied as potential therapeutic agents to treat Alzheimer’s disease and the cognitive and negative symptoms of schizophrenia. BQCA has been shown to improve performance in cognition tasks and increase cerebral blood flow.
B121 Bromoacetylcholine bromide  
C1629 Choline bitartrate Acyl group acceptor
488593 Choline bromide-(methyl-13C) 99 atom % 13C  
C1879 Choline chloride ≥98% The enzymatic activities of butyrylcholinesterase (BChE) and paraoxonase 1 (PON1), two serum enzymes synthesized by the liver and related with inflammation, were decreased in a sepsis animal model injected with LPS. Choline chloride administered intravenously at 20 mg/kg body weight prevents the LPS-mediated decreases in the activities of these two enzymes .
D3190 Dithiobiuret 97%, solid  
SML0224 HI-6 ≥98% (HPLC) HI-6 is an efficient oxime cholinesterase reactivator that is used as an antidote for organophosphates (Ops) exposure.
H108 Hemicholinium-3 solid, ≥95% (HPLC) Potent and selective choline uptake blocker.
L9919 LY2033298 ≥98% (HPLC) LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 potentiates ACh-M4 binding, with no effect at M1/3/5 receptors. LY2033298 can also bind to the M ACh receptor, and mediate either positive or negative allosteric effects depending on the ligand used to probe receptor activity.
L134 Linopirdine ≥98% (HPLC) Stimulates release of acetylcholine and other neurotransmitters; cognitive enhancer.
SML1059 MMB-4 ≥98% (HPLC) MMB-4 is an oxime that can reactivate cholinesterases that have been inactivated by exposure to organophosphates such as sarin or soman. Administration of MMB-4 and atropine normalizes many respiratory parameters in guinea pigs following soman inhalation.
SML0624   PE 154 ≥97% (HPLC) Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are known to associate with β-amyloid plaques, and histological co-localization of AChE and Ab peptides is well established in Alzheimer’s disease. PE-154 is a fluorescent inhibitor of both AChE and BChE with IC50 values of 280 pM and 16 nM. PE-154 stains Aβ plaques in both rodent and human tissue samples, and does not cross react with phospho-tau.
PZ0300 PF-06764427 ≥98% (HPLC) PF-06764427 is a selective azaindole muscarinic receptor M1 positive allosteric modulator.
P0111 Phenserine ≥98% (HPLC), solid (-)-Phenserine, a phenylcarbamate derivative, is a selective, non-competitive inhibitor of acetylcholinesterase (AChE). (-)-Phenserine produces rapid, potent, and long-lasting AChE inhibition, in vivo. It is significantly less toxic than (-)-physostigmine. (-)-Phenserine improves cognitive performance in both young learning-impaired and elderly rats. Reduced secretion of β-amyloid (Abeta) has been observed in cell lines exposed to (-)-phenserine, occurring through translational regulation of β-amyloid precursor protein (beta-APP) mRNA via a non-cholinergic mechanism. These in vitro findings appear to translate in vivo into animal models and humans.
SML0881   Rivastigmine tartrate ≥98% (HPLC) Rivastigmine is an orally available, brain penetrant, reversible cholinesterase inhibitor that enhances cognitive function in patients with Alzheimer′s and Parkinson′s diseases. Rivastigmine inhibits both butyrylcholinesterase and acetylcholinesterase.
SML0453 TBPB ≥98% (HPLC) TBPB is a highly selective Muscarinic M1 receptor allosteric agonist. It activates M1 through an allosteric site rather than the orthosteric acetylcholine binding site, which is likely critical for its selectivity. Muscarinic 1 (M1) receptors are expressed in brain regions responsible for attention and memory, including hippocampus, cortex, and striatum. M1 activation is a proposed mechanism for increasing information processing in disease states, such as Alzheimer′s. M1 agonists are being studied as potential therapeutic agents to treat Alzheimer’s disease and the cognitive and negative symptoms of schizophrenia.
T7556 Tropine 2-(phenylthio)butanoate oxalate salt ≥98% Potent analgesic. Causes increased release of acetylcholine at central muscarinic synapses.
V3265 VU0029767 ≥98% (HPLC) VU0029767 is a selective, positive allosteric modulator at the muscarinic M1 acetylcholine receptor. It shifts concentration-dependent response to acetylcholine at least five-fold, but does not compete at the ACh binding site. VU0029767 also potentiates the effects of allosteric agonist TBPB.
T0195   α-Bungarotoxin-tetramethylrhodamine from Bungarus multicinctus (Formosan Banded Krait) Useful for detecting the distribution of nicotinic acetylcholine receptors at neuromuscular junctions.
α-Bungarotoxin is a high-affinity antagonist for nicotinic acetylcholine receptors (AChRs) from muscle but not the neurons. Labeling α-Bungarotoxin with tetramethylrhodamine enables the detection of bungarotoxin-binding receptors at neuromuscular junctions.
T5644   β-Bungarotoxin from Bungarus multicinctus (Formosan Banded Krait) β-Bungarotoxin is reported to block potassium (K+) currents in frog and mouse motor nerves8. Furthermore, this toxin inhibits phorbol-ester-induced phosphorylation of synapsin I, GAP-43 and MARCKS in rat brains9.
Phospholipase A2 neurotoxin; destroys synaptic vesicles and inhibits acetylcholine release.