Lupanine (D-Lupanine) is a natural ketonic derivative of Sparteine with a ganglioplegic activity. Lupanine shows binding affinity for nicotinic receptor with a K i value of 500 nM [1].
In Vivo, Lupanine (100-300 mg/kg for i.p.; 175-700 mg/kg for p.o.) is much less toxic in one single injection in EOPS male Swiss mice (20-22 g) and Hartley guinea-pigs (400-500 g)[1]. Lupanine (1-7.5 mg/kg; i.v.) is more efficient than Sparteine for antagonizing secondary reflex hypertension in carotid occlusion and hypotension resulting from the stimulation of the pneumogastric nerve in both the cat and the dog[1]. Lupanine has an inhibitory action on nicotinic type hypertension produced by injection of Acetylcholine (500 p.g/kg i.v.) in the Atropine-treated dog[1].
In Vitro, Lupanine shows binding affinity for nicotinic receptor with a Ki value of 500 nM. While, Lupanine shows a very weak affinity for the muscarinic receptor with a Ki value of 11000 nM[1]. Lupanine (0-100 μM) is a weak agonist and desensitizer in SH-SY5Y cells, with EC50 and DC50 of 10.7 μM and 28.2 μM, respectively[2].
References:
[1]. K Yovo, et al. Comparative pharmacological study of sparteine and its ketonic derivative lupanine from seeds of Lupinus albus. Planta Med. 1984 Oct;50(5):420-4.
[2]. Green BT, et al. Anagyrine desensitization of peripheral nicotinic acetylcholine receptors. A potential biomarker of quinolizidine alkaloid teratogenesis in cattle. Res Vet Sci. 2017 Dec;115:195-200.
In Vivo, Lupanine (100-300 mg/kg for i.p.; 175-700 mg/kg for p.o.) is much less toxic in one single injection in EOPS male Swiss mice (20-22 g) and Hartley guinea-pigs (400-500 g)[1]. Lupanine (1-7.5 mg/kg; i.v.) is more efficient than Sparteine for antagonizing secondary reflex hypertension in carotid occlusion and hypotension resulting from the stimulation of the pneumogastric nerve in both the cat and the dog[1]. Lupanine has an inhibitory action on nicotinic type hypertension produced by injection of Acetylcholine (500 p.g/kg i.v.) in the Atropine-treated dog[1].
In Vitro, Lupanine shows binding affinity for nicotinic receptor with a Ki value of 500 nM. While, Lupanine shows a very weak affinity for the muscarinic receptor with a Ki value of 11000 nM[1]. Lupanine (0-100 μM) is a weak agonist and desensitizer in SH-SY5Y cells, with EC50 and DC50 of 10.7 μM and 28.2 μM, respectively[2].
References:
[1]. K Yovo, et al. Comparative pharmacological study of sparteine and its ketonic derivative lupanine from seeds of Lupinus albus. Planta Med. 1984 Oct;50(5):420-4.
[2]. Green BT, et al. Anagyrine desensitization of peripheral nicotinic acetylcholine receptors. A potential biomarker of quinolizidine alkaloid teratogenesis in cattle. Res Vet Sci. 2017 Dec;115:195-200.