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Belviq (lorcaserin): A brand-new weight loss drug, with interesting properties...

Privateer

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Cross-post from OD. I figured it was more suited for here anyway.

So Arena Pharmaceuticals has been developing this compound for a longgg time with the idea that it's going to be a blockbuster. The regulation process went extraordinarily slowly, which is why I guess it's not a household name. It's the first totally new weight-loss molecule approved by the FDA in something like 15 years, but that's relatively old news. More recently relevant is that the DEA just gave it the final thumbs up for Schedule IV approval, due to its ability to provide hallucinations and habitual use. That was on May 7th, so the launch of this new drug should slip in as early as June 7th. And it should be a big launch too, owing to its "potential blockbuster" status. There's gonna be a whole lot of these pills out there at once.

Okay but so, why should you care? Well first check out this structure:



It looks like something out of the ADD "draw random molecules" thread, right? As for pharmacology, lorcaserin is a 5-HT2C full agonist. That's what gives it its appetite loss properties, but it also seems to give it some other interesting properties.

Check this out from the PI form:

9.2 Abuse In a human abuse potential study in recreational drug abusers, supratherapeutic oral doses of lorcaserin (40 and 60 mg) produced up to two- to six-fold increases on measures of “High”, “Good Drug Effects”, “Hallucinations” and “Sedation” compared to placebo. These responses were similar to those produced by oral administration of the positive control drugs, zolpidem (15 and 30 mg) and ketamine (100 mg). In this study, the incidence of the adverse reaction of euphoria following lorcaserin administration (40 and 60 mg; 19%) is similar to the incidence following zolpidem administration (13-16%), but less than the incidence following ketamine administration (50%). The duration of euphoria following lorcaserin administration persisted longer (> 9 hours) than that following zolpidem (1.5 hours) or ketamine (2.5 hours) administration

So as I'm reading this, the DEA just Schedule IV'd a drug that can make you trip for 9 hours if you take as little as double the daily dose at once. I think this drug could become a pretty big problem if it ends up being recreationally used; I could see it being used on its own and also with other drugs as a combination. The appetite loss might be annoying but it also might be a recreationally beneficial effect. I think it should be emphasized that, unlike fenfluramine, this compound has no activity at 5-HT2B receptors, so there should be little risk of cardiovascular effects. What do you all think, is lorcaserin going to be a household name in a couple years?
 

Epsilon Alpha

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I'd be interested in seeing the tolerance profile of this drug. If its anything like the more traditional psychedelics then we probably don't have much to worry about for addiction/ abuse for MOST people I mean there are people who get their kicks from diphenhydramine so anything is possible.

Also, I am shocked to see that a 5HT2C agonist is recreational most of the reading I've done on it suggests that 5HT2C antagonism has an antidepressant effect. Do they mention any sort of crash in the full text or other side effects that might deter abuse? I mean 5HT2C agonism reduces DA/NE transmission in several areas of the brain associated with reward/wanting.

I don't have journal access over the summer so I'm out to lunch on this one. But, great post OP :)
 
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sekio

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Priapism (painful erections greater than 6 hours in duration) is a potential effect of 5-HT2C receptor agonism.
If not treated promptly, priapism can result in irreversible damage to the erectile tissue. Men who have an erection lasting greater than 4 hours, whether painful or not, should immediately discontinue the drug and seek emergency medical attention.
BELVIQ should be used with caution in men who have conditions that might predispose them to priapism [...]

Hm. Strange side effect profile for a diet drug. Hallucinations, euphoria, sedation, and... boners.
 

electrodevo

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Hm. Strange side effect profile for a diet drug. Hallucinations, euphoria, sedation, and... boners.

Never heard of the boner aspect of 5-HT2C agonists, heh.

In the wiki, it is mentioned that locaserin is is not only a 5-HT2C agonist (where the appetite suppression happens), but a 5-HT2B agonist and partial 5-HT2A agonist as well. The partial 5-HT2A agnoism would be a part of the explanation for hallucinations at higher doses I guess. Many 5-HT2B agonists are quite hard on the heart (see: fenfluramine)... I guess this one hasn't been so far at clinical doses, but I'm not sure this is the best substance to get your recreational kicks on.
 

endotropic

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Never heard of the boner aspect of 5-HT2C agonists, heh.

In the wiki, it is mentioned that locaserin is is not only a 5-HT2C agonist (where the appetite suppression happens), but a 5-HT2B agonist and partial 5-HT2A agonist as well. The partial 5-HT2A agnoism would be a part of the explanation for hallucinations at higher doses I guess. Many 5-HT2B agonists are quite hard on the heart (see: fenfluramine)... I guess this one hasn't been so far at clinical doses, but I'm not sure this is the best substance to get your recreational kicks on.

There's no way this is a 5-HT2B agonist right? Even the FDA isn't that stupid?

Edit: Here's the potency/affinity data from the FDA:

Table 5. Lorcaserin Potency (EC50) and Binding Affinity (Ki) to Human 5-HT2A, 5-HT2B, and 5-HT2C Receptor Subtypes
Serotonin Receptor Subtype EC50, nM Ki, nM
5HT2C___________________39________13
5HT2B___________________2380______147
5HT2A___________________553_______92


You probably won't hit 2B unless you really push the dose. Only four fold selectivity for 2A compared to 2B though.
 
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Riemann Zeta

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Sadly, I doubt this one will be an enjoyable or interesting psychedelic, despite the minor 5-HT2A contribution. I think the only reason it is scheduled is that it is an "anorexic." Since every single other anorectic drug has been yanked from the market, regulatory agencies are very suspicious of new anorectics, which is why virtually none get approved. Hell, it seems that the FDA/DEA policy is to schedule any newly released drug that enters the central nervous system with a minimum classification of Schedule V. For example, all of the novel anti-epileptics released in the last 5 years--perampanel, retigabine, lacosamide and pregabalin--were put in Schedule V, despite lacking any addictive potential or even any enjoyable psychoactive effect (although some people do find pregabalin to be somewhat pleasant).

Anyway, this loraserin sounds more like it possesses all of the side effects of a DOX-class psychedelic amphetamine without a lot of the visual psychedelic effects.
 

RobotRipping

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shit a 5-ht2c antagonist - that doesn't sound good at all. though it's not binding to it that strongly and also hitting b and a, may give it some interesting properties, but most psychs that hit 5-ht2c strongly (like a psych with high affinity for 5-ht2a but 1/4 for 5-ht2c or any lower proportion) for me causes anxiety, nausea and dysphoria. psychedelic boner time.
 

Gaius

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It's not an antagonist. If you read the OP again you'll see it's actually a full agonist (which I find very confusing for obvious reasons).
 

ebola?

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. I think the only reason it is scheduled is that it is an "anorexic."

I dunno. I'd like to think that assessment of "liking" the compound had something to do with it...a lot of people do enjoy ambien (which had a comparable score on the inventories used).

ebola
 

Privateer

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Some more research about lorcaserin:

Lorcaserin, a 5-HT2C Agonist, Decreases Nicotine Self-Administration in Female Rats (2011)
http://jpet.aspetjournals.org/content/338/3/890.abstract

Evaluation of the Abuse Potential of Lorcaserin, a Serotonin 2C (5-HT2C) Receptor Agonist, in Recreational Polydrug Users
http://www.nature.com/clpt/journal/v89/n5/full/clpt201120a.html

Funnily enough, the abstract of this second one paints a more dreary picture of lorcaserin's abuse potential than the DEA's review. Maybe the DEA was pushing it because of lorcaserin's anorectic properties.

supratherapeutic doses of lorcaserin were associated with significant levels of dislike by users as compared with placebo, zolpidem, and ketamine. Perceptual effects were minimal after administration of lorcaserin and significantly lower than after administration of either ketamine or zolpidem. The findings suggest that, at supratherapeutic doses, lorcaserin is associated with distinct, primarily negative, subjective effects and has low abuse potential.
 

oar9fi

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"Stop, collaborate and listen" -Vanilla Ice
I just saw the commercial for this and looked at the website (not that I have any interest in using the stuff for ANY purpose)
Copy & pasted directly http://belviq.com:
Mental problems: Taking too much BELVIQ may cause hallucinations, a feeling of being high or in a very good mood, or feelings of standing outside your body
They don't beat around the bush about making I making it sound recreational.
 

Xorkoth

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Sadly, I doubt this one will be an enjoyable or interesting psychedelic, despite the minor 5-HT2A contribution. I think the only reason it is scheduled is that it is an "anorexic." Since every single other anorectic drug has been yanked from the market, regulatory agencies are very suspicious of new anorectics, which is why virtually none get approved. Hell, it seems that the FDA/DEA policy is to schedule any newly released drug that enters the central nervous system with a minimum classification of Schedule V. For example, all of the novel anti-epileptics released in the last 5 years--perampanel, retigabine, lacosamide and pregabalin--were put in Schedule V, despite lacking any addictive potential or even any enjoyable psychoactive effect (although some people do find pregabalin to be somewhat pleasant).

Anyway, this loraserin sounds more like it possesses all of the side effects of a DOX-class psychedelic amphetamine without a lot of the visual psychedelic effects.

Pregabalin is one of my favorite substances, it makes me feel *amazing*. I've only tried it a few times though, I actively have it on my radar to acquire however.
 

abracadabra girl

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Hallucinations doesn't necessarily mean fun. But if it is, then I want some! Is it FDA approved yet?

Edit: Never mind.

"euphoria was observed in 0.17% of patients taking BELVIQ and 0.03% taking
placebo...
reports of depression/mood problems occurred in 2.6% BELVIQ-treated vs. 2.4%
placebo-treated and suicidal ideation occurred in 0.6% BELVIQ-treated
vs. 0.4% placebo-treated patients."

So it's 3 times more likely to make you suicidal than euphoric.
 
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