La Lobelina è un alcaloide presente nel genere della Lobelia, ed è stato studiato a lungo contro soprattutto la dipendenza da tabacco.
Io dopo qualche anno che fumavo sono riuscito a smettere nel giro di qualche giorno grazie all'uso di questa pianta.
Tuttavia il suo impiego non è solo legato alla cura del tabagismo ma anche e SOPRATTUTTO direi contro l'uso degli psicostimolanti.
La Lobelina agisce come inibitore del VMAT2, che possiamo definire quasi la risacca dove i neurotrasmettitori vengono contenuti prendi del loro utilizzo. La Lobeline però diciamo, temporaneamente fa fuori i neurotrasmettitori senza usarli a mo' di rilascio in stile anfetamine, o in stile coca, catinoni e fenidati vari non ricapta. Quindi lì per lì ci perdete soltanto neurotrasmettitori che saranno smaltiti dai corrispettivi MAO.
La parte interessante è che bruciando i neurotrasmettitori mentre siete sotto una dose alta che ne so di Etilfenidato e volete che cali, vi rollate uno spino di Lobelia e vi sentirete molto più calmi, perchè ciò sta nel VMAT2 viene come bruciato, e avrete un effetto di calo più o meno brusco degli effetti. In pratica tornate base-line con la Lobelia, senza l'uso di benzo o calmanti.
Tuttavia la Lobelina non è solo un inibitore VMAT2, ma anche un antagonista dei recettori nicotinici, e un antagonista oppioceo (mu).VMAT2 is an integral membrane protein that transports monoamines—particularly neurotransmitters such as dopamine, norepinephrine, serotonin, and histamine—from cellular cytosol into synaptic vesicles.[2] In nigrostriatal pathway and mesolimbic pathway dopamine-releasing neurons, VMAT2 function is also necessary for the vesicular release of the neurotransmitter GABA.
Sono stati fatti esperimenti e sembra che sia con alcol, eroina e cocaina e anfetamina riduca l'effetto di queste sostanze, soprattutto ne riduce la cosidetta ROTA, perchè ha un vero e proprio effetto anti-DIPENDENZA.
Parlando invece di esperienze personali, posso dire che fumando Lobelia la Cannabis è in un certo modo addolcita, e dura esattamente la metà, lasciandomi in uno stato molto più sedativo che euforico-psichedelico.
Inoltre, se assumo grandi dosi di caffeina e voglio dormire, mi fumo uno spino di lobelia e mi calmo quasi subito, senza dover pigliare benzo o calmanti. Mai provato con stimolanti più seri, ci sarebbe da fare una prova.
Ecco quello che sono riuscito a trovare dalla letteratura scientifica:
Although lobeline and reserpine each increase the release of [3H]dopamine, they have different effects when administered prior to methamphetamine. Pretreatment with lobeline decreased methamphetamine-induced [3H]dopamine release, while pretreatment with reserpine increased methamphetamine-induced [3H]dopamine release
At higher concentrations, lobeline may block [3H]dopamine efflux through the DAT. Although the relatively high concentrations of lobeline required to achieve this effect may argue against its therapeutic use, results from in vivo experiments suggest that the concentration of lobeline required to decrease methamphetamine self-administration may be in the low micromolar range [7].
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2435375/
These results suggest that lobeline produces a nonspecific rate suppressant effect following acute administration, to which tolerance develops following repeated administration. Importantly, the results also suggest that repeated administration of lobeline specifically decreases responding for d-methamphetamine in a noncompetitive manner. Thus, lobeline may be an effective, novel pharmacotherapy for d-methamphetamine abuse.
http://www.ncbi.nlm.nih.gov/pubmed/11408539
http://www.ncbi.nlm.nih.gov/pubmed/23875705
Studies utilizing VMAT2 knockout mice demonstrate reduced drug-seeking behavior compared to wild-type in locomotor response studies that included a array of drugs, including amphetamine and cocaine.[28, 29]. Collectively, these results support the validity of VMAT2 serving as a target for the development of therapeutic agents that have the ability to augment cessation of psychostimulant abuse [30].
Lobeline also attenuates cocaine self-administration in rats. The effects of lobeline on cocaine-induced hyperactivity in rats is complex. Acutely, lobeline did not decrease the effect of cocaine on hyperactivity. However, repeated administration of lobeline attenuated cocaine-induced hyperactivity and prevented the development of sensitization to cocaine. Interestingly, repeated administration of a lower dose of lobeline (0.3 mg/kg) increased cocaine (10 mg/kg)-induced hyperactivity (Polston, Cunningham et al. 2006). These behavioral studies demonstrate that lobeline has potential as a pharmacotherapy for psychostimulant abuse. In addition, since lobeline attenuates methamphetamine-induced decreases in rat striatal VMAT2 protein, this suggests a possible neuroprotective role against methamphetamine toxicity (Eyerman and Yamamoto 2005). Lobeline is currently undergoing Phase 2 clinical evaluation to determine its effectiveness in humans as a therapeutic agent for methamphetamine abuse.
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3725992/
Eroina:
The present study tested the hypothesis that pretreatment with LOB would attenuate heroin self-administration in rats. The findings from this investigation demonstrated that LOB pretreatment effectively attenuates opiate self-administration in a dose dependent manner. The lowest dose of LOB (0.3 mg/kg) had no effect, while attenuation of heroin self-administration was demonstrated with LOB doses of 1.0 and 3.0 mg/kg. Our findings are in agreement with the findings of Miller et al. (2007) where lobeline was found to be a μ opioid receptor antagonist, due to having a high affinity for μ opioid receptors, thereby producing an inhibitory effect on opiate pharmacology.
Metadone:
Specifically, methadone overdose (death) is much more common than many people realize (Srivastava and Kahan, 2006; Zador, 2007), and the development of potentially safer, substitute pharmacotherapy’s is desired. In this regard, the fact that LOB acts antagonistically on the opiate system may offer a reliable and less dangerous way to manage selective addiction profiles.
Etanolo:
Results showed that lobeline significantly reduced alcohol consumption and alcohol preference during the repeated (recurring and continuous) administration phases, while total fluid consumption remained unchanged. These results provide support that nicotinic receptor based drugs may be useful as potential treatments for alcoholism.
Neurotossine:
In conclusion, in addition to exerting nicotine-like effects, lobeline, as an inhibitor of DAT, may protect dopaminergic neurons against extracellular toxins, such as MPTP (MPP+), by blocking DAT-mediated uptake, and may increase the DA concentration in the synaptic cleft by inhibiting reuptake of DA. Lobeline administration may thus result in the treatment of symptoms and the deceleration of PD progress. Therefore, the combination of several beneficial properties (high blood-brain barrier penetration, DAT inhibition and neurotrophic functions similar to nicotine) suggests that lobeline is a potential preventive or therapeutic agent for the treatment of PD.
https://www.spandidos-publications.com/ ... .2013.1413