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Pozanicline

nicotinic receptors

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11 replies to this topic

#1 zeroskater6979

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Posted 25 February 2012 - 04:59 PM


Pozanicline (ABT-089) is a drug developed by Abbott, which acts as a partial agonist at neural nicotinic
acetylcholine receptors. It is subtype-selective, binding primarily to the α4β2 and also α6β2 subtypes.[1][2] It has nootropic andneuroprotective effects,[3][4][5] and animal studies suggested that it might be useful for the treatment of ADHD.[6] Subsequent human trials have shown ABT-089 to both be effective for this application,[7] and also to have particularly low tendency to cause side effects compared to other drugs in the class,[8][9] making it a promising candidate for clinical development. (Wikipedia)

What do you guys think about the nicotinic receptors as a sight to exploit for cognitive enhancement purposes? Would anyone be willing to experiment with this and other related drugs? It definitely looks promising, thoughts?

#2 singularvision

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Posted 23 March 2012 - 12:21 AM

yeah, I've heard good things about this one. would def be willing to give it a try

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#3 Baten

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Posted 23 March 2012 - 06:56 AM

Sounds very interesting indeed.

#4 zeroskater6979

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Posted 23 March 2012 - 02:50 PM

here's another alpha nicotinic receptor agonist that's pretty far down the pipeline with good results:
Ispronicline (TC-1734, AZD-3480) (AstraZeneca) is a drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to theα4β2subtype. It has antidepressant, nootropic and neuroprotective effects, and is under development for the treatment of dementia and Alzheimer's disease. Clinical trials so far have shown ispronicline to be effective and well tolerated, with the main side effects being dizziness and headache

#5 gamesguru

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Posted 23 March 2012 - 02:56 PM

Wouldn't nicotinic agonists theoretically induce nicotinic receptor down-regulation? Like GABAergic and dopaminergic agonists, they have their roles as medicine in advanced disease[anxiety for gaba, thought disorders for dopamine], but I don't think they will be useful for healthy people. I could be wrong, but I'm not losing sleep over these two "nootropic" compounds.

#6 KoolK3n

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Posted 19 July 2013 - 01:40 PM

Wouldn't nicotinic agonists theoretically induce nicotinic receptor down-regulation? Like GABAergic and dopaminergic agonists, they have their roles as medicine in advanced disease[anxiety for gaba, thought disorders for dopamine], but I don't think they will be useful for healthy people. I could be wrong, but I'm not losing sleep over these two "nootropic" compounds.


New study: http://www.ncbi.nlm....3290324/related

#7 Reformed-Redan

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Posted 19 July 2013 - 04:16 PM

Alpha-7-nicotininc receptors are really interesting. Nootropic potential seems to be high; but, restoration of normal cognitive functioning seems higher in individuals with certain deficits.

#8 KoolK3n

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Posted 19 July 2013 - 06:49 PM

Alpha-7-nicotininc receptors are really interesting. Nootropic potential seems to be high; but, restoration of normal cognitive functioning seems higher in individuals with certain deficits.


AZD3408 binds to the alpha4beta2 receptor. Nicotine upregulates both. What's ur opinion on Nicotine used as a nootropic?

Edited by KoolK3n, 19 July 2013 - 06:53 PM.


#9 3AlarmLampscooter

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Posted 19 July 2013 - 07:12 PM

Alpha-7-nicotininc receptors are really interesting. Nootropic potential seems to be high; but, restoration of normal cognitive functioning seems higher in individuals with certain deficits.


AZD3408 binds to the alpha4beta2 receptor. Nicotine upregulates both. What's ur opinion on Nicotine used as a nootropic?


I've been using nicotine recently, in the form of e-cig fluid in gel capsules. Got to say I like it overall. Seems to help decently with concentration and motivation. Totally non-addicitve alone, I have been off it for 6 days with no cravings. The cardiac effects are a real problem with longer term use though. I'm interested in combining with guanfacine if I can find some...

Edit: GTS-21/DMXB-A, Rivanicline and ABT-418 are all also quite promising, and related. I'd be really interested in a group buy of one of these new nicotinic agonists.

Edited by 3AlarmLampscooter, 19 July 2013 - 07:19 PM.


#10 Reformed-Redan

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Posted 19 July 2013 - 08:27 PM

Alpha-7-nicotininc receptors are really interesting. Nootropic potential seems to be high; but, restoration of normal cognitive functioning seems higher in individuals with certain deficits.


AZD3408 binds to the alpha4beta2 receptor. Nicotine upregulates both. What's ur opinion on Nicotine used as a nootropic?


I've been using nicotine recently, in the form of e-cig fluid in gel capsules. Got to say I like it overall. Seems to help decently with concentration and motivation. Totally non-addicitve alone, I have been off it for 6 days with no cravings. The cardiac effects are a real problem with longer term use though. I'm interested in combining with guanfacine if I can find some...

Edit: GTS-21/DMXB-A, Rivanicline and ABT-418 are all also quite promising, and related. I'd be really interested in a group buy of one of these new nicotinic agonists.

PRL should be interesting enough. 1k posts. :D

#11 KoolK3n

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Posted 19 July 2013 - 11:10 PM

I've been using nicotine recently, in the form of e-cig fluid in gel capsules. Got to say I like it overall. Seems to help decently with concentration and motivation. Totally non-addicitve alone, I have been off it for 6 days with no cravings. The cardiac effects are a real problem with longer term use though. I'm interested in combining with guanfacine if I can find some...


Cool. I wonder if the hypertension from Nicotine can be alleviated with Clonidine/Guanfacine. I was just thinking of this combo last night too. Is Guanfacine even available without a prescription? It's not my intention to continually endorse AllDayChemist but their offer on Clonidine is stellar. I think it's $60 for 540 yes 540 capsules of 150ug each. I would really like for someone to verify the quality of the pills via lab testing. I am always concerned with it being underdosed or having nothing advertised in it. Anyways, I never would have thought Nicotine to be the most cost effective AchA7 & A4B2 enhancing agent. What was/is your daily nicotine dosage?

Edited by KoolK3n, 19 July 2013 - 11:12 PM.


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#12 3AlarmLampscooter

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Posted 19 July 2013 - 11:19 PM

I've been using nicotine recently, in the form of e-cig fluid in gel capsules. Got to say I like it overall. Seems to help decently with concentration and motivation. Totally non-addicitve alone, I have been off it for 6 days with no cravings. The cardiac effects are a real problem with longer term use though. I'm interested in combining with guanfacine if I can find some...


Cool. I wonder if the hypertension from Nicotine can be alleviated with Clonidine/Guanfacine. I was just thinking of this combo last night too. Is Guanfacine even available without a prescription? It's not my intention to continually endorse AllDayChemist but their offer on Clonidine is stellar. I think it's $60 for 540 yes 540 capsules of 150ug each. I would really like for someone to verify the quality of the pills via lab testing. I am always concerned with it being underdosed or having nothing advertised in it. Anyways, I never would have thought Nicotine to be the most cost effective AchA7 & A4B2 enhancing agent. What was/is your daily nicotine dosage?


I ended up finding 10mg orally twice a day to work fairly well. The bioavailability of nicotine orally is quite poor, so this obviously translates to a much lower dose in the blood. Online pharmacies stock plenty of prescription meds legally, the only problem is when stuff is DEA scheduled, which guanfacine is not. Getting scheduled compounds without a prescription obviously requires either face to face interaction with an unlicensed pharmaceutical representative or the deep web, and commission of a federal crime. That's why you'll see clonidine for sale, but not modafinil.




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