Uses
(±)-Acetylcarnitine Chloride is a drug absorption-enhancing agent in the gastrointestinal tract.
Biological Activity
(±)-acetylcarnitine chloride is an agonist for cholinergic.acetylcholine receptor (achr) is an integral membrane protein receptor for acetylcholine. there are two kinds of achrs: nicotinic acetylcholine receptors and muscarinic acetylcholine receptors.(±)-acetylcarnitine chloride is a cholinergic agonist and an intermediate in lipid metabolism [1]. in retinal ganglion cells, acetylcarnitine and acetylcholine inhibited gabaergic responses to exogenous gaba and gabaergic inhibitory postsynaptic currents [2].in dogs with coronary ligation, (-)-carnitine chloride (lcc) (300 mg/kg) and acetyl (-)-carnitine chloride (alcc) (300 mg/kg) inhibited the ventricular arrhythmia. also, lcc and alcc improved oxidative phosphorylation rate and the mitochondrial function [1]. in the mouse hot plate test, acetyl-l-carnitine (alcar) (100 mg/kg) exhibited analgesia. while, u-73122 and neomycin (the phospholipase c (plc) inhibitors) blocked the increase of the pain threshold induced by alcar. licl that impairing phosphatidylinositol synthesis antagonized the antinociception in a dose-dependent way. pma and pdbu (pkc activators) blocked the increase of the pain threshold in a dose-dependent way. these results suggested that alcar analgesia required the participation of the plc-ip3 pathway [3].
Biochem/physiol Actions
Weak cholinergic receptor agonist; intermediate in lipid metabolism.
in vivo
In rats, the infusion of 2 mg (±)-Acetylcarnitine chloride decreases blood flow through the hind limb vasculature 50%. (±)-Acetylcarnitine chloride also potentiates the inhibitory effect of adrenaline on the isolated rabbit duodenum[3].
Purification Methods
Recrystallise the chloride from isopropanol. Dry it over P2O5 under high vacuum. The S-betaine crystallises from EtOH/Et2O with m 145o(dec) and is hygroscopic; it has [] D -19.5o (c 6, H2O). [Krimberg & Wittandt Biochem Z 251 231 1932, Strack et al. Z Physiol Chem 238 191 1936, Beilstein 4 III 1630, 1632.]
References
[1]. imai s, matsui k, nakazawa m, et al. anti-arrhythmic effects of (-)-carnitine chloride and its acetyl analogue on canine late ventricular arrhythmia induced by ligation of the coronary artery as related to improvement of mitochondrial function. br j pharmacol, 1984, 82(2): 533-542.
[2]. b?hring r, standhardt h, martelli ea, et al. gaba-activated chloride currents of postnatal mouse retinal ganglion cells are blocked by acetylcholine and acetylcarnitine: how specific are ion channels in immature neurons? eur j neurosci, 1994, 6(7): 1089-1099.
[3]. galeotti n, bartolini a, calvani m, et al. acetyl-l-carnitine requires phospholipase c-ip3 pathway activation to induce antinociception. neuropharmacology, 2004, 47(2): 286-294.
