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Naltrexone upregulates GABA receptors!

gaba benzodiazepines upregulation receptors withdrawal paws naltrexone opioids

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#1 HelpMeOut

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Posted 28 January 2018 - 10:00 PM


I have found following information a while ago. It seems that Naltrexone is a negative modulator of GABAA receptors. I also saw that on wikipedia. Will low-dose-naltrexone help the upregulation of GABAA receptors after benzodiazepine usage?

 

 

Abstract

Several lines of behavioral and neurochemical evidence indicate GABA(A)-antagonistic properties of naloxone. Here, the effects of naloxone on rat brain GABA(A)/benzodiazepine receptor function in vitro were investigated. Naloxone, naltrexone and morphine (10-1,000 microM) reduced GABA-induced (10 microM) 36Cl- uptake in corticohippocampal synaptoneurosomes. Furthermore, the concentration-response curve for GABA-induced 36Cl- uptake (GABA 3-100 microM) was shifted to the right both by naloxone and morphine (1,000 microM). Naloxone also reduced the 36Cl- uptake induced by GABA + diazepam (3 microM + 1 microM) but not that induced by amobarbital (500 microM). The naloxone-induced (1,000 microM) reduction of GABA-mediated (10 microM) 36Cl- uptake was reversed by amobarbital (10-1,000 microM) but not by flumazenil (10-1,000 microM) or morphine (0.1-1,000 microM). These results indicate that naloxone, naltrexone and morphine are weak negative modulators of GABA(A)/benzodiazepine receptor function. The naloxone effect most likely does not involve opiate receptors or the benzodiazepine site on GABA(A) receptor complexes.

(https://www.ncbi.nlm...pubmed/10821435)

 

 

... and

 

 

Abstract

Rats were made sensitive to the effects of the opioid antagonist naltrexone by treating them once weekly with cumulative doses of the drug (1, 3, 10, 30 and 100 mg/kg). Sensitization was monitored by measuring salivation following naltrexone administration. During the first week of treatment, no salivation was noted following any dose of naltrexone. Over a period of 8 weeks, however, increasing amounts of salivation were noted, with the most salivation occurring at the higher doses. Animals treated for 8 weeks with saline never salivated following injections. Following the development of sensitivity to naltrexone, the rats were sacrificed and their brains were assayed for GABA receptor function. GABA-stimulated chloride uptake, a measure of GABA receptor function, was unchanged in the cortex, but was increased in the cerebellum. These results suggest that the effects of naltrexone on cerebellar GABA receptors may be involved in the development of enhanced sensitivity to opioid antagonists.

(https://www.ncbi.nlm.../pubmed/1310130)

 



#2 normalizing

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Posted 12 May 2018 - 04:09 PM

very interesting. i never thought of naltrexone having anything to do with GABA. but im still confused by these articles and im not sure if it really does upregulate GABA actually. can someone else put their professional opinion on this?



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#3 Omega 3 Snake Oil

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Posted 01 September 2018 - 01:04 AM

My insomnia and dysautonomia (both of which I think have to do with degeneration of GABA receptors in my hypothalamus) worsened while I was on LDN, 4.5 mg per night. I always thought there was a connection...



#4 normalizing

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Posted 02 September 2018 - 07:46 PM

you clearly have no clue about anything omega snake shit


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#5 Hyperflux

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Posted 04 December 2018 - 02:25 AM

I tried it twice so far, didn't do anything for benzo tolerance/withdrawal. I jumped straight into 4.5mg though for the test, LH and dopamine boost. Basically you feel like you're in heroin-lite withdrawals for 4 hours then you become superhuman. The feeling afterwards feels like I took tianeptine + dextroamphetamine.


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#6 John250

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Posted 04 December 2018 - 06:05 PM

I tried it twice so far, didn't do anything for benzo tolerance/withdrawal. I jumped straight into 4.5mg though for the test, LH and dopamine boost. Basically you feel like you're in heroin-lite withdrawals for 4 hours then you become superhuman. The feeling afterwards feels like I took tianeptine + dextroamphetamine.


I still have a bottle of low dose naltrexone from irc.bio but have been afraid to use it due to feeling like crap part. Did you take it at night? Did you start lower at 1.5mg like recommended and titrate up? Supposedly you don’t feel shitty by that mechanism. It’s dupp to be taken at night. I just can’t afford a poor nights sleep and hate trying anything new before bed Incase I have an adverse reaction.





Also tagged with one or more of these keywords: gaba, benzodiazepines, upregulation, receptors, withdrawal, paws, naltrexone, opioids

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