Levetiracetam (UCB L059) is an antiepileptic, it is also a selective M2 muscarinic acetylcholine receptors (mAChR) inhibitor. Levetiracetam displays potent seizure protection in animal models of chronic epilepsy but lacks activity in acute seizure models. Levetiracetam binds synaptic vesicle protein 2A (SV2A).
| Molecular Weight | 170.21 |
| Formula | C8H14N2O2 |
| CAS Number | 102767-28-2 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL Water ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related AChR/AChE Products |
|---|
| Tacrine
Tacrine is a potent acetylcholinesterse (AChE) inhibitor (IC50=109 nM), also acting as a CYP1A2 substrate agent. |
| THRX-160209
THRX-160209 is a potent antagonist at the M(2) muscarinic acetylcholine (ACh) receptor subtype that was designed using a multivalent strategy, simultaneously targeting the orthosteric site and a nearby site known to bind allosteric ligands. |
| Catestatin
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. |
| α-Conotoxin MII
α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. |
| COG 133 TFA
COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. |
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