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The activity of Lobelia is dependent upon a liquid alkaloid first isolated by Proctor in 1838 and named Lobeline. Pereira found a peculiar acid which he named Lobelic acid. Also, gum, resin, chlorophyl, fixed oil, lignin, salts of lime and potassium, with ferric oxide. Lobelacrine, formerly considered to be the acrid principle, is probably lobelate of lobeline. The seeds contain a much higher percentage of lobeline than the rest of the plant.
MEDICAL - Lobelia is a vaso-motor stimulant increases the activity of all vegetative processes, spends its force mainly upon the pneumogastric nerve, producing a depressed relaxed condition with oppression of chest and epigastrium, impeded respiration, nausea and vomiting.
Fatigue, relaxation of muscles, nausea, vomiting and dyspepsia are the general indications that point to the use of this remedy in asthma and gastric disorders. Asthma and labored breathing. Asthma and stomach disorders. Bad effects of drunkenness. Suppressed discharges. (Sulph.) Diphtheria. Catarrhal jaundice. (Chion.)
Nausea and vomiting with nearly all the lung troubles or stomach disorders. Lob. stimulates vasomotor nerves, causing increased secretions, relaxation and weakness with sweat with deathly sickness all over with oppressed rattling respiration. Sits with elbows on knees. Prickling all over. Cannot bear the odor of tobacco although addicted to its use.
Auton Neurosci. 2004 Jan 30;110(1):27-35. Related Articles, Links
Influence of lobeline on catecholamine release from the isolated perfused rat adrenal gland.
Lim DY, Kim YS, Miwa S.
Department of Pharmacology, College of Medicine, Chosun University, Gwangju 501-759, South Korea. firstname.lastname@example.org
It has been shown that lobeline (alpha-lobeline) is a lipophilic, nonpyridine, naturally occurring alkaloid obtained from Indian tobacco, Lobelia inflata. The present study was attempted to investigate the effect of lobeline on secretion of catecholamines (CA) evoked by ACh, high K(+), 1.1-dimethyl-4-phenyl piperazinium iodide (DMPP) and (3-(m-chloro-phenyl-carbamoyl-oxy)-2-butynyl trimethyl ammonium chloride (McN-A-343) from the isolated perfused rat adrenal gland and to establish the mechanism of its action. l-Lobeline (30-300 microM) perfused into an adrenal vein for 60 min produced dose- and time-dependent inhibition in CA secretory responses evoked by ACh (5.32 x 10(-3) M), DMPP (10(-4) M for 2 min) and McN-A-343 (10(-4) M for 2 min). However, lower dose of lobeline did not affect CA secretion by high K(+) (5.6 x 10(-2) M), higher dose of it reduced greatly CA secretion of high K(+). l-Lobeline itself did also fail to affect basal catecholamine output. Furthermore, in adrenal glands loaded with lobeline (100 microM), CA secretory response evoked by methyl-1,4-dihydro-2,6-dimethyl-3-nitro-4-(2-trifluoromethylphenyl)-pyridine-5-carboxylate (Bay-K-8644), an activator of L-type Ca(2+) channels was markedly inhibited while CA secretion by cyclopiazonic acid, an inhibitor of cytoplasmic Ca(2+)-ATPase was not affected. However, nicotine (30 microM), given into the adrenal gland for 60 min, initially rather enhanced CA secretory responses evoked by ACh (5.32 x 10(-3) M) and high K(+) (5.6 x 10(-2) M) followed by great inhibition later, while responses evoked by DMPP (10(-4) M for 2 min) and McN-A-343 (10(-4) M for 2 min) were greatly inhibited. Taken together, these results suggest that lobeline inhibits greatly CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors. Lobeline at lower dose does not affect that by membrane depolarization, but at larger dose inhibits that. It is thought that this inhibitory effect of lobeline may be mediated by blocking the calcium influx into the rat adrenal medullary chromaffin cells without the inhibition of Ca(2+) release from the cytoplasmic calcium store, which is relevant to its nicotinic antagonistic activity. It also seems that there is a difference in the mode of action between nicotine and lobeline in rat adrenomedullary CA secretion.
Biochem Pharmacol. 2002 Jan 15;63(2):89-98. Related Articles, Links
A novel mechanism of action and potential use for lobeline as a treatment for psychostimulant abuse.
Dwoskin LP, Crooks PA.
College of Pharmacy, University of Kentucky, Rose Street, Lexington, KY 40536-0082, USA. email@example.com
Lobeline, an alkaloidal constituent of Lobelia inflata LINN., has a long history of therapeutic usage ranging from emetic and respiratory stimulant to tobacco smoking cessation agent. Although classified as both an agonist and an antagonist at nicotinic receptors, lobeline has no structural resemblance to nicotine, and structure--function relationships do not suggest a common pharmacophore. Lobeline inhibits nicotine-evoked dopamine release and [3H]nicotine binding, thus acting as a potent antagonist at both alpha3beta2(*) and alpha4beta2(*) neuronal nicotinic receptor subtypes. However, lobeline does not release dopamine from its presynaptic terminal, but appears to induce the metabolism of dopamine intraneuronally. Reevaluation of the mechanism by which lobeline alters dopamine function reveals that its primary mechanism is inhibition of dopamine uptake and promotion of dopamine release from the storage vesicles within the presynaptic terminal, via an interaction with the tetrabenazine-binding site on the vesicular monoamine transporter (VMAT2). Thus, lobeline appears to perturb the fundamental mechanisms of dopamine storage and release. Based on its neurochemical mechanism, the ability of lobeline to functionally antagonize the neurochemical and behavioral effects of the psychostimulants amphetamine and methamphetamine was examined. Lobeline was found to inhibit the amphetamine-induced release of dopamine in vitro, and amphetamine-induced hyperactivity, drug discrimination, and self-administration. However, lobeline does not support self-administration in rats, suggesting a lack of addiction liability. Thus, lobeline may reduce the abuse liability of these psychostimulants. The development of lobeline and lobeline analogs with targeted selectivity at VMAT2 represents a novel class of therapeutic agents having good potential as efficacious treatments for methamphetamine abuse
J Pharm Pharmacol. 1993 Jun;45(6):545-50.
Pharmacological properties of beta-amyrin palmitate, a novel centrally acting compound, isolated from Lobelia inflata leaves.
Subarnas A, Tadano T, Oshima Y, Kisara K, Ohizumi Y.
Department of Pharmaceutical Molecular Biology, Tohoku University, Sendai, Japan.
Effects of beta-amyrin palmitate isolated from the leaves of Lobelia inflata were studied on the central nervous system of mice and were compared with those of antidepressant drugs, mianserin and imipramine. In the forced swimming test, beta-amyrin palmitate, like mianserin and imipramine, reduced the duration of immobility of mice significantly in a dose-dependent manner (5, 10 and 20 mg kg-1). beta-Amyrin palmitate (5, 10 and 20 mg kg-1) or mianserin (5, 10 and 20 mg kg-1) elicited a dose-related reduction in locomotor activity of mice and antagonized locomotor stimulation induced by methamphetamine. In contrast, imipramine (5, 10 and 20 mg kg-1) increased locomotor activity and potentiated methamphetamine-induced hyperactivity. beta-Amyrin palmitate showed no effect on reserpine-induced hypothermia, whilst mianserin (10 mg kg-1) and imipramine (10 and 20 mg kg-1) antagonized the reserpine-induced effect. Unlike imipramine, beta-amyrin palmitate and mianserin did not affect haloperidol-induced catalepsy, tetrabenazine-induced ptosis and apomorphine-induced stereotypy. beta-Amyrin palmitate and imipramine had no effects on the head-twitch response induced by 5-hydroxytryptophan, whereas mianserin (5, 10 and 20 mg kg-1) decreased it in a dose-dependent manner. A potentiating effect of beta-amyrin palmitate (5, 10 and 20 mg kg-1) on narcosis induced by sodium pentobarbitone was stronger than that of imipramine (10, 20 and 40 mg kg-1) but weaker than that of mianserin (2.5, 5 and 10 mg kg-1). These results suggest that beta-amyrin palmitate has similar properties in some respects to mianserin and might possess a sedative action