3-Bromocytisine is a potent agonist of α4β4, α4β2 and α7 nACh receptors (IC50 values are 0.28, 0.30 and 31.6 nM respectively). Displays different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs (EC50 values are 0.008 and 0.05 μM respectively).
| Molecular Weight | 269.14 |
| Formula | C11H13BrN2O |
| CAS Number | 207390-14-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 26.91 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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