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Afobazol - novel russion benzodiazepine

I was prescribe to it before doc prescribed me alprazolam. I didn't noticed any effect from it. Maybe it has something to do because i was heavy stimulant user in that time. Cannot say anything about effect. I heard from other people that thy expierenced very mild anxyolitic effect from it.
 
My goodness! Can we please refrain from offtopic nonsense posts?


There was the question about the structure of Afobazol. As not all of us are familiar with IUPAC-nomenclature, I prepared a pic:




For more pharmacological infos check out the 2nd link provided by Enkidu in his first post here (#2).

- Murphy
 
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boohigh said:
I was prescribe to it before doc prescribed me alprazolam. I didn't noticed any effect from it. Maybe it has something to do because i was heavy stimulant user in that time. Cannot say anything about effect. I heard from other people that thy expierenced very mild anxyolitic effect from it.
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I think this stuff is being underdosed.
 
I'm gonna start this one in 2 days, i was wondering what dose would be optimal when looking at those affinities? I think this one has more potential and is being underdosed.

Thx!
 
MurphyClox said:
My goodness! Can we please refrain from offtopic nonsense posts?


There was the question about the structure of Afobazol. As not all of us are familiar with IUPAC-nomenclature, I prepared a pic:




For more pharmacological infos check out the 2nd link provided by Enkidu in his first post here (#2).

- Murphy
Click to expand...


I can see how someone could erroneously see 'benzodiazepine' if they saw a benzene ring attached to 2 nitrogens. Benzos though are way different in structure (7 membered ring, two aromatic groups, tricyclic structure etc PS I know some have 4 rings, but still contain that 3 ringed basic structure))
 
Day 1.
I've taken 2 pills in the morning and ive just taken 1 more pill (10mg doses). Nothing interesting to report yet.
 
MeDieViL said:
Day 1.
I've taken 2 pills in the morning and ive just taken 1 more pill (10mg doses). Nothing interesting to report yet.
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Man, i have checke russian-speaking psychiatrist board and all they saying - it's a placebo pill.
 
boohigh said:
Man, i have checke russian-speaking psychiatrist board and all they saying - it's a placebo pill.
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I beleive its being underdosed.

That leaves me to the next question:
The interaction of afobazole (5-ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole dihydrochloride) and its main metabolite M-11 (2-[2-(3-oxomorpholine-4-yl)-ethylthio]-5-ethoxy benzimidazole hydrochloride) with neuroreceptors was studied using the method of radioligand analysis. The binding of afobazole with s1 (Ki =5.9 x 10(-6) M), MTI (Ki =1.6 x 10(-5) M), and MT3 (Ki =9.7 x 10(-7) M) receptors, as well as with a regulatory site of MAO-A (Ki = 3.6 x 10(-6) M) was revealed. The binding of M-11 with MT3 receptors (Ki = 3.9 x 10(-7) M) was demonstrated. The translocation of s1 receptor from endoplasmatic reticulum to the external membrane was revealed by the confocal microscopy technique on the immmortalized hippocampal HT-22 cells under the condition of 30- and 60-min-long afobazole (10(-8) M) application. Afobazole was shown to inhibit MAO-A reversibly. These properties of afobazole are consistent with our previous findings of the anxiolytic and neuroprotective effects of this drug.
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How much can i take without significantly inhibiting MAOA? (So i can still take MDAI etc).
 
^ I wouldn't risk combining it with MDAI after any level of dosage if I were you.

Hm... An anxiolytic drug with a slew of mechanisms of actions. It will be interesting to see the other drugs that come down the line in this family in a few years.
 
flacky said:
^ I wouldn't risk combining it with MDAI after any level of dosage if I were you.

Hm... An anxiolytic drug with a slew of mechanisms of actions. It will be interesting to see the other drugs that come down the line in this family in a few years.
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It depends, AMT for example can safely be combined with MDMA because its MAO action is insignificant.
 
flacky said:
^ Just erring on the side of safety for HR purposes.
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I know, better be safe then sorry, therefor i'm waiting for someone to tell me wheter its a significant MAOI or not, wont try anything potentially stupid without being sure i'm safe.
 
MeDieViL said:
I know, better be safe then sorry, therefor i'm waiting for someone to tell me wheter its a significant MAOI or not, wont try anything potentially stupid without being sure i'm safe.
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Any updates on how the regimen is going??
 
I stopped taking it due to the MAOA inhibiting properties, i wont resume untill someone can tell me how signigicant it inhibits MAOA, i would like to avoid serotonin syndrome.
 
What I found are just in vitro activities, therefore those numbers should be taken with a grain of salt:

Abstract
Selective anxiolytic afobazole (1 mM) inhibits monoamine oxidase A activity in mitochondria from rat brain and liver (IC50 0.36 and 0.43, respectively). Effect of the compound does not depend on the time of preincubation with mitochondria. Triple washout of mitochondria is followed by complete recovery of initial enzyme activity.
[...]
These results indicate that the drug acts as weak and easily reversible MAO A inhibitor. It remains unclear, whether afobazole interacts with MAO A in vivo. However, the data on region-specific increase in norepinephrine content (predominant MAO A substrate [11,12]) in the frontal cortex of C57Bl mice treated with afobazole [1] indirectly attest to this interaction.
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Ref: Bull Exp Biol Med 2009, 148(1), p.23

The references [1], [11] & [12] from the above quotation are:
[1] V. S. Kudrin: Eksp Klin Farmakol 2006, 69(5), pp.7-10
[11] J. C. Shih: Neurotoxicology 2004, 25(1-2), pp.21-30
[12] M. Yamada and H. Yasuhara: Neurotoxicology 2004, 25(1-2), pp.215-221

Sounds like we shouldn't be too worried about the MAO-A-inhibition. But always better safe then sorry ;)

Peace! Murphy


Edit: Seredenin et al. already determined the MAOI-activity before and published it in Int J Neuropsychopharmacol 2008 11, Suppl 1, p. 304. I have no access to this paper, but I can at least present some numbers:
In vivo experiments showed a modulating effect of this substance on the GABAergic system. According to the results of radioligand assay performed by Seger company (France), afobazole in vitro interacts with σ1-receptors and MT1 and MT3 melatonin receptors and reduces binding of labeled inhibitor of type A monoamine oxidase (MAO A). The efficiency of afobazole interaction with molecular targets estimated by IC50 value was 9.9 nM for MT3 receptors, 6.2 μM for MAO A, 7.1 μM for σ1, and 27 μM for MT1. These data indicate that afobazole produces a complex pharmacological effect due to simultaneous influence on several molecular targets.
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Ref: same as above
 
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