| Bioactivity | Tacrine hydrochloride (hydrate) is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively. |
| Target | IC50: 31 nM (AChE), 25.6 nM (BChE) |
| Invitro | Tacrine hydrochloride (hydrate) (12.5 to 37.5 nM) inhibits venom acetylcholinesterase as well as human serum butyrylcholinesterase in a concentration-dependent manner. The IC50 is 31 nM for snake venom AChE and 25.6 nM for human BChE[1]. |
| In Vivo | Pretreatment with Tacrine hydrochloride (hydrate) also modifies absolute levels of cocaine self-administration during reacquisition. Body weight declines approximately one-half percent over four days of treatment with intravenous Tacrine hydrochloride (hydrate). Delivery of Tacrine hydrochloride (hydrate) by osmotic pump does not alter either linear- or repeated- cocaine-induced locomotor activity. There is no significant main effect or interaction with Tacrine hydrochloride (hydrate) treatment on active lever responding during reinstatement. Post hoc comparisons indicate that rats self-administering cocaine has significantly lower alkaline phosphatase levels, relative to TTacrine hydrochloride (hydrate)- but not saline- treated rats evaluated by conditioned-place preference[2]. |
| Name | Tacrine hydrochloride (hydrate) |
| CAS | 206658-92-6 |
| Formula | C13H14N2.xHCl.xH2O |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Ahmed M, et al. Inhibition of two different cholinesterases by tacrine. Chem Biol Interact. 2006 Aug 25;162(2):165-71. [2]. Grasing K, et al. Enduring effects of tacrine on cocaine-reinforced behavior: Analysis by conditioned-place preference, temporal separation from drug reward, and reinstatement. Pharmacol Res. 2015 Jul;97:40-7. |