Neostigmine bromide (Prostigmin) is a reversible acetylcholinesterase inhibitor and a parasympatho-mimetic. By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors. It binds to the anionic site of cholinesterase. The compound blocks the active site of acetylcholinesterase so the enzyme can no longer break down the acetylcholine molecules before they reach the postsynaptic membrane receptors. This allows for the threshold to be reached so a new impulse can be triggered in the next neuron. In myasthenia gravis there are too few acetylcholine receptors so with the acetylcholinesterase blocked, acetylcholine can bind to the few receptors and trigger a muscular contraction.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||Water 30 mg/mL|
|Related AChR/AChE Products|
|Scopolamine hydrobromide trihydrate
Scopolamine hydrobromide trihydrate is a competitive muscarinic acetylcholine receptor with an IC50 of 55.3 ± 4.3 nM.
Choline Glycerophosphate is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue.
MK-7622 is a cholinesterase inhibitor, it is also a muscarinic M1 receptor positive allosteric modulator.
Acotiamide is a potent, selective and reversible inhibitor of human and canine stomach-derived acetylcholinesterase (AChE).
Huperzine A is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor extracted from traditional Chinese herb.
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