Benzos Nitemazepam (7-nitrotemazepam)

[kokaino]

I have found a vendor selling this. This vendor will make custom synthesis, so I asked for Nitemazepam (7-nitro instead of 7-chloro analogue of temazepam).

I'm trying to figure of potency. A nitrogen atom in place of a chlorine would increase potency (by weight), but since the parent drugs, both temazepam and nimetazepam are hypnotics, so this will likely be a hypnotic with a rapid onset. I think about 1-2 mg of nitemazepam = 5 mg nimetazepam = 20 mg temazepam = 10 mg diazepam.

I requested the synthesis of Nitemazepam, but they've got two new benzos along with Nitemazepam. They've got fonazepam and adinozolam

 

[Tryptamite]

Report back experience pls

 

[izo]

I’d say hat the difference between chloro and nitro group at the 7 position isn’t that great, maybe it’s a bit more potent but not that much as you stated in the starting post.

 

[izo]

Maybe around 10% more potent than temazepam. You need some halogen on the 2ˋ position of the phenyl ring for your numbers. Look at clonazepam and diclazepam.

 

[kokaino]

Based on the tracking, I should be getting the gram sampler I ordered tomorrow. The vendor is a huge Chinese laboratory with Ph.D chemists who work for them. I am trying to find an unscheduled (overlooked) morphine or codeine derivative for them to synthesize for me, but I think the government's got 'em all covered (or do they?)

 

[izo]

There are plenty of unscheduled opioids out there, it just takes some work to find them in papers or patents and knowledge which one is a winner.

 

[kokaino]

There are plenty of unscheduled opioids out there, it just takes some work to fin d them in papers or patents and knowledge which one is a winner.

Morphine and all of it's 3,6-diesters and other esters of morphine or codeine (which include morphine diacetate aka diacetylmorphine/diamorphine or 'Heroin', morphine dinicotinate aka dinicotinoylmorphine/nicomorphine or 'Vilan' -all (or most) of the 3,6-diesters of morphine are morphine prodrugs). Other esters of morphine include desomorphine,

The 1912 Convention had made its control measures applicable "To all new derivatives of morphine, of cocaine, or of their respective salts, and to every other alkaloid of opium, which may be shown by scientific research, generally recognized, to be liable to similar abuse and productive of like ill-effects."

Although I'd love to find an unscheduled codeine derivate, it seems like they've got all the basis covered. I am looking at acetyldihydrocodeine and trying to see how we can manipulate that to make something unscheduled. Acetyldihydrocodeine is a derivative of dihydrocodeine, and both are converted into dihydromorphine. Our best bet are nitazene-opioids or a ketobemidone or dextromoramide derivatives or analogues.

21 U.S. Code § 802 subsection 17 :

Subparagraphs A, B, C, D, E, F state:
(A) Opium, opiates*, derivatives of opium and opiates, including their isomers, esters, ethers, salts, and salts of isomers, esters, and ethers, whenever the existence of such isomers, esters, ethers, and salts is possible within the specific chemical designation. Such term does not include the isoquinoline alkaloids of opium.
(B) Poppy straw and concentrate of poppy straw
(C) Coca leaves, except coca leaves and extracts of coca leaves from which cocaine, ecgonine, and derivatives of ecgonine or their salts have been removed.
(D) Cocaine, its salts, optical and geometric isomers, and salts of isomers.
(E) Ecgonine, its derivatives, their salts, isomers, and salts of isomers.
(F) Any compound, mixture, or preparation which contains any quantity of any of the substances referred to in subparagraphs (A) through (E).

* includes morphine, diamorphine, nicomorphine, desomorphine, codeine, heterocodeine, and related substances

21 U.S. Code § 813 subsection 32 - Treatment of controlled substance analogues
Subparagraphs A, B, C
(A) Except as provided in subparagraph (C), the term “controlled substance analogue” means a substance —
I: the chemical structure of which is substantially similar to the chemical structure of a controlled substance in schedule I or II;
II: which has a stimulant, depressant, or hallucinogenic effect on the central nervous system that is substantially similar to or greater than the stimulant, depressant, or hallucinogenic effect on the central nervous system of a controlled substance in schedule I or II; or
III: with respect to a particular person, which such person represents or intends to have a stimulant, depressant, or hallucinogenic effect on the central nervous system that is substantially similar to or greater than the stimulant, depressant, or hallucinogenic effect on the central nervous system of a controlled substance in schedule I or II.
(B) The designation of gamma butyrolactone or any other chemical as a listed chemical pursuant to paragraph (34) or (35) does not preclude a finding pursuant to subparagraph (A) of this paragraph that the chemical is a controlled substance analogue. (C) Such term does not include —
I: a controlled substance;
II: any substance for which there is an approved new drug application;
III: with respect to a particular person any substance, if an exemption is in effect for investigational use, for that person, under section 355 of this title to the extent conduct with respect to such substance is pursuant to such exemption; or
IV: any substance to the extent not intended for human consumption before such an exemption takes effect with respect to that substance.

That enlarged part is the loophole.

 

[kokaino]

Since benzodiazepines are Schedule IV, these laws do not apply. Thus any derivative or analogue is legal until specifically name it a "controlled substance", and subsequently go on to schedule the drug.

Now that we have a benzo (a child of temazepam X nimetazepam, Nitemazepam), we need a temazepam X triazolam offspring (a 'Temazolam') lol.

 

[kokaino]

Maybe around 10% more potent than temazepam. You need some halogen on the 2ˋ position of the phenyl ring for your numbers. Look at clonazepam and diclazepam.

I think you might be right. A fluorine atom on the 2' position would give me a potency in the 0.5-2 mg range.

 

[izo]

Other esters of morphine include desomorphine,

This makes no sense.

A fluorine atom on the 2' position would give me a potency in the 0.5-2 mg range.

Im not hundred percent sure of this but to me it seems that a 2‘-fluoro along with a 7-nitro group makes for an even twice as strong compound as compared to the other halogens. 1mg of flunitrazepam is comparable to 2mg clonazepam. When there isn’t a nitro group on benzo ring but another halogen it’s more like clonazepam potency wise. Can somebody confirm this.

 

[kokaino]

This makes no sense.



Im not hundred percent sure of this but to me it seems that a 2‘-fluoro along with a 7-nitro group makes for an even twice as strong compound as compared to the other halogens. 1mg of flunitrazepam is comparable to 2mg clonazepam. When there isn’t a nitro group on benzo ring but another halogen it’s more like clonazepam potency wise. Can somebody confirm this.

See I think that flunitrazepam is overrated like no other drug. The parent drug, nitrazepam (Mogadon) is better and more recreational in my experience with both drugs (I've used both dozens of times). Nitrazepam 10mg provides the same level of anxiety relief as 1mg flunitrazepam or 0.5mg clonazepam. However, as hypnotic agents, flu-and nitrazepam are expected to be felt more profoundly when it comes to sedative, muscle relaxant, anterograde amnesia, and motor-impairment.

 

[morphonorconic]

I’ve wondered when adinazolam might appear in the RC scene. For those who don’t know, adinazolam was synthesized in the hopes of discovering a triazole benzo with marked antidepressant properties, similar to but greater than those produced by alprazolam. And if I’m not mistaken, the same dude is credited with the discovery of both compounds.

Both nitemazepam and adinazolam seem promising, but I’ve said that about previous RC benzos and been disappointed, so I suppose we’ll see.

 

[kokaino]

I’ve wondered when adinazolam might appear in the RC scene. For those who don’t know, adinazolam was synthesized in the hopes of discovering a triazole benzo with marked antidepressant properties, similar to but greater than those produced by alprazolam. And if I’m not mistaken, the same dude is credited with the discovery of both compounds.

Both nitemazepam and adinazolam seem promising, but I’ve said that about previous RC benzos and been disappointed, so I suppose we’ll see.

No benzodiazepine is an antidepressant. Evidence is low quality, usually, but empirical evidence and pharmacologists pretty much across the board agree that benzodiazepines are actually a cause for depressive disorders.

 

[kokaino]

In fact, a human study comparing the subjective effects and abuse potential of adinazolam (30 mg and 50 mg) with diazepam, lorazepam and a placebo showed that adinazolam causes the most "mental and physical sedation" and the greatest "mental unpleasantness".

SOURCE

 

[izo]

I know of the adinazolam wiki article but also wonder why trying to make an antidepressant out of alprazolam. It is a good benzodiazepine, nothing more, nothing less.

 

[kokaino]

I know of the adinazolam wiki article but also wonder why trying to make an antidtepressant out of alprazolam. It is a good benzodiazepine, nothing more, nothing less.

I think it was an attempt to try to reach a wider patient base and a pharmaceutical company's (makers of Xanax) way to convince incompetent physicians that Xanax was somehow different from all other benzos, including its immediate family (triazolo-benzos), in that it had antidepressant effects based on several low-quality, cherry-picked studies funded in part by Up-John Co. All profit driven nonsense, and no science.

I agree that alprazolam is a good (great) anxiolytic benzo at functional, therapeutic doses (0.25-0.5 mg for the benzo-naive or low tolerant). However, it is otherwise relatively lacking in other areas benzos are utilized for aside from anxiolysis (as myorelaxants, anticonvulsants, hypnotics, etc). In comparison to clonazepam, diazepam, and lorazepam, it is a poor anticonvulsant. It is also lacking in muscle relaxant properties relative to clonazepam, diazepam, and lorazepam in this regard, as well. Due to its intermediate onset of effects (30-60 minutes post-ingestion; mean ~45 mins - same as clonazepam), it makes for a poor hypnotic compared to fast-acting oral diazepam 10 mg (15-30 minutes post-ingestion) or sublingual lorazepam 1 mg (5-10 mins post-ingestion). Although sublingual alprazolam 1 mg would make for a hypnotic agent (but only in sublingual form).

In case of panic disorders, 0.5 mg sublingual alprazolam is comparable to 1 mg sublingual lorazepam in treating an oncoming panic attack.

Overall, I think alprazolam in sublingual form is ideal for panic attacks, and tablets for daytime, functional anxiolysis. Otherwise, there are superior options in all areas in which a benzodiazepine is indicated.

 

[Fertile]

The 7-Nitro moiety confers increased a1 affinity and promote serotonin release and so nitrazepam is deemed to be twice a potent as diazepam (for example).

The problem is that the onset of the 7-nitro analogues is slower and so if you produce a benzo with a 7-nitro combined with features that reduce duration (like the 3 -OH in this case) then their window activity is small compared to onset.

Of course, their could be something unusual about this example. I note it was first produced in 1977 but no nation has licensed it for medical use.

It's also worth noting that nitrobenzodiazepines are significantly more toxic than other examples and so it could be rather risky to produce a low-potency analogue - people might have sufficient tolerance to NEED a lot but end up reaching a toxic dose. WHY it's toxic, I do not know. It could be due to it's serotonin releaseing property and/or the 7-nitro being metabolized to the 7-amino which could be mutagenic.

 

[stom10]

I’ve wondered when adinazolam might appear in the RC scene. For those who don’t know, adinazolam was synthesized in the hopes of discovering a triazole benzo with marked antidepressant properties, similar to but greater than those produced by alprazolam. And if I’m not mistaken, the same dude is credited with the discovery of both compounds.

Both nitemazepam and adinazolam seem promising, but I’ve said that about previous RC benzos and been disappointed, so I suppose we’ll see.

It already sorta has! I believe it mostly was sold as "Xanax replacement" once China stopped shipping out alprazolam powder. (But before they started using flualprazolam with denatonium benzoate as a bitterant for that purpose)

DrugsData.org: Test Results

DrugsData.org lab analysis and drug checking results

www.drugsdata.org

 

[Fertile]

Adinazolam is a prodrug and only about 20% of it is converted into the active (N-desmethyl adinazolam). The medical format was intended to be 20mg.

Brotizolam analogues are rather complex to make but if etizolam is now being produced commercially (in India in particular) then that is the 'next wave' I presume. I mean, the scaffold was widely studied in the 1980s so there are quite a few thusfar uncontrolled analogues.

I have concluded that neither the Chinese chemists nor the RC vendors know anything about medicinal chemistry. The formed don't care much - if something is legal and they can make it, they are happy. But the latter must end up wish a LOT of total losers. There have been a stack of REALLY bad MXE 'replacements'.

I presume that anyone skilled 'in the art' of medicinal chemistry would not wish to be involved with such people - after all, if caught then no more career.

 

[kokaino]

Adinozolam has been compared to other benzos, diazepam and lorazepam (i think it was those two), an,d the study concluded that adinozolam was the "least pleasant". Not a single subject enjoyed their adinozolam doses (30 mg and 60 mg).

Griffiths et al. 1980b; Griffiths et al. 1984a & 1984b; de Wits 1984a; Roche and Griffiths, 1985; Funderburk et al. 1988; Johanson and de Wit, 1989; Evans et al. 1991, and many other studies up until 2016 on benzodiazepine abuse, tolerance, and dependence liability compared to one another and vs other sedative-hypnotics, opioids, and stimulants, including cocaine.

In all the above studies, but for 1980b, showed that diazepam and other benzodiazepines have been found to increase ratings of liking among individuals with a history of alcoholism and/or other substance abuse. In the study by Griffiths et al. 1980b, diazepam (50 - 400 mg) failed to report significant increases in 'drug-liking', 2 hours post administration (orally). The two other benzos, lorazepam (2-16 mg) and nitrazepam (50 - 400 mg), only nitrazepam in doses of 70 mg and up increased 'drug-liking' but not MBG scores (the "euphoria scale"). In all the other studies, diazepam produced dose-dependant 'drug-liking' but didn't increase MBG scores at all.

Not one benzodiazepine increased MBG levels (the "euphoria scale"), except for two in 4 of the studies listed above (Griffiths et al. 1984b; de Wits 1984a; Roche and Griffiths, 1985; Funderburk et al. 1988; Johanson and de Wit, 1989), increased MBG scores significantly (in addition to 'drug-liking'). Those two were temazepam (95-660 mg) and triazolam (1.25-10 mg). In 2 of the studies, orally administered doses, to alcoholic or drug-abusing volunteers of 100 mg and up of temazepam and 2.5 mg and up of triazolam increased both 'drug-liking' and MBG (euphoria) scale significantly. In the other 2 studies, the subjects were healthy volunteers with no history of substance abuse, alcoholism, or any tolerance to sedatives, including ethanol. Diazepam (5-20 mg), flurazepam (15-30 mg), lorazepam (0.5-2 mg), temazepam (15-30 mg) and alprazolam (0.25-1 mg). Temazepam 15 and 30 mg, flurazepam 30 mg, and diazepam 15-20 mg all produced significant 'drug-liking' but only temazepam 30 mg produced a moderate increase in MBG scores.