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Old 04-29-2008, 10:10 PM   #1 (permalink)
X33
 
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Default Lots of promising anxiolytic drugs in development.

http://en.wikipedia.org/wiki/Adipiplon

Adipiplon (NG2-73) is an anxiolytic drug developed by Neurogen Corporation. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.

Adipiplon is a subtype selective GABAA partial agonist, which binds preferentially to the ?3 subtype. This is significant as while several previous nonbenzodiazepine drugs have been developed that are selective for ?2/3 over the other subtypes, adipiplon is one of the first drugs selected for clinical development which is able to discriminate between ?2 and ?3, as well as showing little affinity for the ?1 or ?5 subtypes - alpidem is selective for ?3 over ?2, but still has moderate affinity to ?1, whereas adipiplon is highly ?3-selective with little affinity for either ?1, ?2 or ?5.

Adipiplon is being researched as a potential medication for the treatment of anxiety and insomnia, and is currently (as of 200 in Phase IIb trials.[1][2][3]


CGS-9896 is an anxiolytic drug used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.[1]

CGS-9896 is a benzodiazepine receptor partial agonist, which produces long-lasting anxiolytic and anticonvulsant effects in animal studies, but does not produce sedative effects.[2][3] It also increases appetite,[4] and reduces the development of gastrointestinal ulcers following chronic stress.[5]


CGS-20625 is an anxiolytic drug used in scientific research. It has similar effects to, and binds to the same target as benzodiazepine drugs,[1] but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.[2][3]

CGS-20625 produces anxiolytic and anticonvulsant effects, but with no sedative effects even at high doses, and no significant muscle relaxant effects.[4] It is orally active in humans, but with relatively low bioavailability.[5]

Etifoxine (or etafenoxine) is an anxiolytic and anticonvulsant drug.[1] It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.[2] It is more effective than lorazepam as an anxiolytic, but has less side effects.[3]

Unlike benzodiazepines, etifoxine appears to produce its anxiolytic effects by binding to ?2 and ?3 subunits of the GABAA receptor complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines.[4] This difference in binding means that etifoxine can be used alongside benzodiazepines to potentiate their effects without competing for binding sites,[5] however it also means that the effects of etifoxine are not reversed by the benzodiazepine antagonist flumazenil.[6]


Pagoclone is an anxiolytic drug from the cyclopyrrolone family, which is related to other more well known drugs such as the sleeping medication zopiclone. It is one of a relatively recently developed class of medicines known as the nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures.

Pagoclone was originally developed as an anti-anxiety drug, but never commercialised. It is a partial agonist acting at GABAA receptors in the brain. In contrast to zopiclone, pagoclone produces anxiolytic effects with little or no sedative or amnestic actions at low doses.[1] ..............


etc.

I wish I could fast forward time about 10 years, without aging.
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Old 04-29-2008, 11:41 PM   #2 (permalink)
 
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Default Re: Lots of promising anxiolytic drugs in development.

So basically,companies decided rather than deal with the bad reputation of benzos, just make a drug that hits the brain the same way but is classified differently.
I guess thats good news for anyone with a benzophob doctor. They will probably have the same tolerance issues, but won't get that reputation for that for some time, or maybe not at all. The only different one seems to be Etifoxine because of its binding site.

That makes me think of a way to possibly bypass the tolerance problem. If your Gaba A receptors become tolerant to benzos, you could switch to Etifoxine which targets the Gaba B receptor. And once the Gaba B builds tolerance, you switch back to a Gaba A targeting drug.

I'm glad this company is researching so many GABA drugs that aren't just to be sleep aids. They are basically are making Benzos that wont make you sleepy or lose coordination, but really those side effects are minor in my experience. You could compare the difference between nonbenzodiazepines drugs and benzodiazepines drugs to that of all the various SSRI's on the market; same effects, different chemical compound to do it. Too bad they will be expensive as **** when they come out. Might as well find a doctor who will prescribe a benzo then wait for these.

Nice research Adrian, glad to have read about all these.
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Old 04-29-2013, 02:01 PM   #3 (permalink)
 
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Hey, i know that this thread is like 5 years old, however i was prescribed stresam (etifoxine hydrochloride) last week for anxiety. I think it is working nicely. As maybe already mentioned I notice that the effect wears off after a few hours. I have a morning and evening dose. I used to take deanxit in the past but it used to make me very drowsy.
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