Saxat från Reddit hittade jag en lång lista på många GABA analogier som verkar väldigt intressanta.
En del Phenibut analogier, många andra Pregabalin analogier som inte nådde hela vägen i mål efter en uppföljare när patentet gick ut.
Vi får hoppas att de släpps publikt på sikt.
**---List of GABA drugs examples---**
Phenibut (β-phenyl-GABA) is a famously known analog of GABA with a phenyl group at the beta position of the structure which allows it to cross the blood brain barrier to produce an effect. Unlike some other compounds Phenibut is not a prodrug to GABA. It was created in the USSR (now Russia) in the 1960s by Vsevolod Perekalin, A newspaper highlighted the event on Oct 23, 1968 stating *"Soviet chemist claimed Monday he has developed a harmless miracle drug that overcomes sadness, fear, alarm, fatigue, timidity, irritation and "bad mood" and "recommended the drug to help offset the effects of "mechanization" in modern Soviet life. ", he referred to Phenibut as Phenigama Perekalin indicated the drug would be useful in the Soviet Union to prevent the effects of industrialization from lowering the average worker's productivity. "Modern life often has a traumatic effect on the psyche," Perekalin said. "Traveling on trolleys, in automobiles, buses, trains, airplanes, and the traffic around us all day has a rather strong effect on our ears and psychology."*
Hopantenic acid (N-pantoyl-GABA) (Pantogam) is an analog of GABA and Vitamin B5 that is an approved drug in a few countries for conditions similar to Phenibut.
Picamilon (N-nicotinoyl-GABA) is an analog and prodrug of GABA. After crossing the BBB Picamilion breaks down into GABA and Vitamin B3 in the brain and is approved drug in some countries. It was developed by the USSR (now Russia) in 1969.
4-Fluorophenibut (β-4-fluorophenyl-GABA) is the fluorinated analog of Phenibut. Typically adding a fluorine group in the right position to a substance will enhance it's binding affinity but can also change some of it's effects. It is a strong GABA-B agonist stronger than Phenibut but weaker than Baclofen. It is generally described as being 4x-10x stronger than Phenibut itself. It binds to GABA-B approx. 5x more efficiently than Phenibut and over 100x more efficently compared to it's effects at GABA-A. Baclofen is 4-chlorophenyl-GABA or Fluorophenibut with the fluorine group replaced by a chlorine.
Tolibut or Methylphenibut (β-4-methylphenyl-GABA) is the methylated analog of Phenibut. Typically adding a methyl group in the right position to a substance will enhance it's binding affinity but can also change some of it's effects. Tolibut is not as commonly found as Phenibut or Fluorophenibut, possibly because it's synthesis guides were not published/made as public as others as well as difficulty/expenses with synthesis.
3,4,5-Trimethoxyphenibut (4-Amino-3-(3,4,5-trimethoxyphenyl)butanoic acid) is an analog of Phenibut allegedly developed around 2015-2016 by a Canadian based research chemical supplier but that is disputed as possibly being a rediscovered synthesis paper guarded by chemist enthusiasts that gets passed around privately as the same company was able to synthesize Tolibut and the synthesis guide for Trimethoxyphenibut analogs have not been public and therefore Trimethoxyphenibut is rarely found. There are no confirmed reports of human use of Trimethoxyphenibut, it is unknown what effects it may have but some have hypothesized for it to be completely inactive but this has not been proven either way.
Tetrabut / Tetrazole ((1H-Tetrazol-1-yl)-3-phenylbutyric acid) is a Tetrazole analog of GABA and somewhat Phenibut (4-amino-3-phenylbutyric acid) created by a Russian research group in 2017-2018 along with Tetrazole analogs of Tolibut, Baclofen, Pregabalin, Gabaptentin and Brivaracetam although other direct tetrazole analogs of GABA itself have existed since the 1990s. The effects of Tetrazole analogs of GABA are unknown and have been hypothesized to act differently than their parent compounds, possibly as inhibitors but this as not been proven either way.
β-hydroxy-γ-aminobutyric acid (β-hydroxy-GABA) (gamma-Amino-beta-hydroxybutyric acid) is an analog of GABA and an active metabolite of GABA itself meaning it is produced naturally by the human brain. Nonendogenous GABOB can penetrate the BBB easier than nonendogenous GABA itself.
4-Methylpregabalin (β-4-methyl-isobutyl-GABA) is a gabapentinoid analog of Pregabalin created by Pfizer while researching alternatives to Pregabalin since their patent was about to run out. It is simply the 4-positon methlayed analog of Pregabalin. Generally methylation of a substance makes it stronger in effect which appears to be true for Methylpregabalin and is estimated at being 2x-4x stronger than Pregabalin itself.
Pivagabine (N-pivaloyl-GABA) was sold as a prescription in Italy for anxiety and has been hypothesized to act as a prodrug to GABA or may modulate the corticotropin-releasing factor (CRF).
Tolgabide (SL-81.0142) is an analog and prodrug of GABA and is similar in structure and action to Progabide.
Imagabalin is a gabapentinoid analog of Pregabalin created by Pfizer while researching alternatives to Pregabalin since their patent was about to run out. Despite showing great results in clinical trials it's development was cancelled by Pfizer.
Atagabalin is an analog of gabapentin created by Pfizer but has since ceased development.
Mirogabalin is a gabapentinoid much stronger in effect compared to Pregabalin that is prescribed in Japan.
PD-217,014 is a gabapetinoid stronger than Pregabalin and Gabapentin created by Pfizer while researching alternatives to Pregabalin since their patent was about to run out. It showed effectiveness for neuropathic pain and stronger action than Gabapentin but was not further developed.
Saclofen (sulfonobaclofen) is an analog of Baclofen but instead acts as a GABA-B antagonist and so may be researched in the future as a treatment to reverse the effect of GABA-B drugs.
Phaclofen (phosphonobaclofen) is an analog of Saclofen that is hypothesized to work similarly but does not penetrate the blood brain barrier on it's own making it ineffective.
En del Phenibut analogier, många andra Pregabalin analogier som inte nådde hela vägen i mål efter en uppföljare när patentet gick ut.
Vi får hoppas att de släpps publikt på sikt.
**---List of GABA drugs examples---**
Phenibut (β-phenyl-GABA) is a famously known analog of GABA with a phenyl group at the beta position of the structure which allows it to cross the blood brain barrier to produce an effect. Unlike some other compounds Phenibut is not a prodrug to GABA. It was created in the USSR (now Russia) in the 1960s by Vsevolod Perekalin, A newspaper highlighted the event on Oct 23, 1968 stating *"Soviet chemist claimed Monday he has developed a harmless miracle drug that overcomes sadness, fear, alarm, fatigue, timidity, irritation and "bad mood" and "recommended the drug to help offset the effects of "mechanization" in modern Soviet life. ", he referred to Phenibut as Phenigama Perekalin indicated the drug would be useful in the Soviet Union to prevent the effects of industrialization from lowering the average worker's productivity. "Modern life often has a traumatic effect on the psyche," Perekalin said. "Traveling on trolleys, in automobiles, buses, trains, airplanes, and the traffic around us all day has a rather strong effect on our ears and psychology."*
Hopantenic acid (N-pantoyl-GABA) (Pantogam) is an analog of GABA and Vitamin B5 that is an approved drug in a few countries for conditions similar to Phenibut.
Picamilon (N-nicotinoyl-GABA) is an analog and prodrug of GABA. After crossing the BBB Picamilion breaks down into GABA and Vitamin B3 in the brain and is approved drug in some countries. It was developed by the USSR (now Russia) in 1969.
4-Fluorophenibut (β-4-fluorophenyl-GABA) is the fluorinated analog of Phenibut. Typically adding a fluorine group in the right position to a substance will enhance it's binding affinity but can also change some of it's effects. It is a strong GABA-B agonist stronger than Phenibut but weaker than Baclofen. It is generally described as being 4x-10x stronger than Phenibut itself. It binds to GABA-B approx. 5x more efficiently than Phenibut and over 100x more efficently compared to it's effects at GABA-A. Baclofen is 4-chlorophenyl-GABA or Fluorophenibut with the fluorine group replaced by a chlorine.
Tolibut or Methylphenibut (β-4-methylphenyl-GABA) is the methylated analog of Phenibut. Typically adding a methyl group in the right position to a substance will enhance it's binding affinity but can also change some of it's effects. Tolibut is not as commonly found as Phenibut or Fluorophenibut, possibly because it's synthesis guides were not published/made as public as others as well as difficulty/expenses with synthesis.
3,4,5-Trimethoxyphenibut (4-Amino-3-(3,4,5-trimethoxyphenyl)butanoic acid) is an analog of Phenibut allegedly developed around 2015-2016 by a Canadian based research chemical supplier but that is disputed as possibly being a rediscovered synthesis paper guarded by chemist enthusiasts that gets passed around privately as the same company was able to synthesize Tolibut and the synthesis guide for Trimethoxyphenibut analogs have not been public and therefore Trimethoxyphenibut is rarely found. There are no confirmed reports of human use of Trimethoxyphenibut, it is unknown what effects it may have but some have hypothesized for it to be completely inactive but this has not been proven either way.
Tetrabut / Tetrazole ((1H-Tetrazol-1-yl)-3-phenylbutyric acid) is a Tetrazole analog of GABA and somewhat Phenibut (4-amino-3-phenylbutyric acid) created by a Russian research group in 2017-2018 along with Tetrazole analogs of Tolibut, Baclofen, Pregabalin, Gabaptentin and Brivaracetam although other direct tetrazole analogs of GABA itself have existed since the 1990s. The effects of Tetrazole analogs of GABA are unknown and have been hypothesized to act differently than their parent compounds, possibly as inhibitors but this as not been proven either way.
β-hydroxy-γ-aminobutyric acid (β-hydroxy-GABA) (gamma-Amino-beta-hydroxybutyric acid) is an analog of GABA and an active metabolite of GABA itself meaning it is produced naturally by the human brain. Nonendogenous GABOB can penetrate the BBB easier than nonendogenous GABA itself.
4-Methylpregabalin (β-4-methyl-isobutyl-GABA) is a gabapentinoid analog of Pregabalin created by Pfizer while researching alternatives to Pregabalin since their patent was about to run out. It is simply the 4-positon methlayed analog of Pregabalin. Generally methylation of a substance makes it stronger in effect which appears to be true for Methylpregabalin and is estimated at being 2x-4x stronger than Pregabalin itself.
Pivagabine (N-pivaloyl-GABA) was sold as a prescription in Italy for anxiety and has been hypothesized to act as a prodrug to GABA or may modulate the corticotropin-releasing factor (CRF).
Tolgabide (SL-81.0142) is an analog and prodrug of GABA and is similar in structure and action to Progabide.
Imagabalin is a gabapentinoid analog of Pregabalin created by Pfizer while researching alternatives to Pregabalin since their patent was about to run out. Despite showing great results in clinical trials it's development was cancelled by Pfizer.
Atagabalin is an analog of gabapentin created by Pfizer but has since ceased development.
Mirogabalin is a gabapentinoid much stronger in effect compared to Pregabalin that is prescribed in Japan.
PD-217,014 is a gabapetinoid stronger than Pregabalin and Gabapentin created by Pfizer while researching alternatives to Pregabalin since their patent was about to run out. It showed effectiveness for neuropathic pain and stronger action than Gabapentin but was not further developed.
Saclofen (sulfonobaclofen) is an analog of Baclofen but instead acts as a GABA-B antagonist and so may be researched in the future as a treatment to reverse the effect of GABA-B drugs.
Phaclofen (phosphonobaclofen) is an analog of Saclofen that is hypothesized to work similarly but does not penetrate the blood brain barrier on it's own making it ineffective.
