Shown: posts 1 to 24 of 24. This is the beginning of the thread.
Posted by linkadge on June 19, 2005, at 0:21:06
Does anyone know what a sigma 1 receptor is ??
Linkadge
Posted by ed_uk on June 19, 2005, at 10:11:54
In reply to What is a sigma 1 receptor ??, posted by linkadge on June 19, 2005, at 0:21:06
'Sigma sites are a type of nonopiate receptor whose role has been associated with several behaviours, including anxiety, depression, analgesia, learning processes and psychosis.'
'Sigma receptors have been implicated in psychosis, cognition, neuroprotection, and locomotion in the central nervous system.'
This may be of interest.....
(from Shawn T's neurotransmitter.net)
Escitalopram --
Escitalopram (Lexapro) is a serotonin reuptake inhibitor. The drug is the S-enantiomer of citalopram (Celexa). Fabre and Hannon (2003) have suggested that escitalopram's effects might be mediated in part by agonism at sigma-1 and sigma-2 receptors; however, further investigations are required to make a definitive conclusion.
Ravna AW, Sylte I, Dahl SG.
Molecular mechanism of citalopram and cocaine interactions with neurotransmitter transporters.
J Pharmacol Exp Ther. 2003 Oct;307(1):34-41. Epub 2003 Aug 27. [Abstract]Fabre V, Hamon M.
[Mechanisms of action of antidepressants: new data from Escitalopram]
Encephale. 2003 May-Jun;29(3 Pt 1):259-65. [Abstract]........................
Darkhorse used to take opipramol........
opipramol
Description
Potent sigma receptor ligand. Sedative, stabilizing and mood elevating properties.
'Opipramol, which, apart from a sigma-1- and 2-receptor liability, also possesses histamine-H(1)-antagonistic properties in connection with lower affinities for D(2) and 5-HT(2A) showed broad efficacy in generalized anxiety disorder and somatoform disorders. The receptor profile of opipramol and the results of studies of the selective sigma site ligands siramisine and igmesine suggest that opipramol acts pharmacologically and clinically via sigma receptors.'
'The atypical anxiolytic and antidepressive drug opipramol binds with high affinity to sigma1 and somewhat lower affinity to sigma2 sites. After subchronic treatment, opipramol significantly down-regulated sigma2 but not sigma1 sites. This effect was not seen for imipramine, citalopram, and reboxetine under similar conditions. On the other hand, only imipramine reduced the number of sigma1 sites. It is suggested that effects at sigma2 sites are involved in the anxiolytic properties of opipramol.'
'Although opipramol is structurally related to imipramine, it does not represent a tricyclic antidepressant drug as it does not inhibit the neuronal uptake of norepinephrine and/or serotonin. Unlike imipramine it is a rather potent sigma ligand with modest subclass selectivity which is similar in vitro as well as ex vivo. Opipramol is active in several behavioural paradigms indicative of anxiolytic properties at doses (1-10 mg/kg), which are also needed to occupy sigma binding sites. Somewhat higher doses (10-20 mg/kg) are needed for "antidepressant like" effects. The data allow the conclusion that interaction with sigma sites is involved in the anxiolytic and antidepressant effects of opipramol albeit a contribution of its weaker D (2)-antagonistic and 5-HT2-antagonistic properties cannot be totally be excluded.'
J Clin Psychopharmacol. 2001 Feb;21(1):59-65.
Opipramol for the treatment of generalized anxiety disorder: a placebo-controlled trial including an alprazolam-treated group.
Moller HJ, Volz HP, Reimann IW, Stoll KD.
Psychiatrische Klinik der Ludwig-Maximilians-Universitat, Munich, Germany.
Opipramol, a drug widely prescribed in Germany, is a tricyclic compound with no reuptake-inhibiting properties. However, it has pronounced D2-, 5-HT2-, and H1-blocking potential and high affinity to sigma receptors (sigma-1 and sigma-2). In early controlled trials, anxiolytic effects were revealed. However, those studies were performed before the concept of generalized anxiety disorder (GAD) was established. Because of the interesting receptor-binding profile and promising results of the early clinical trials, the authors performed a state-of-the-art placebo-controlled trial using alprazolam as an active control. Three hundred seven outpatients with GAD were included. After a 7-day single-blind placebo washout, patients were randomly assigned to receive either opipramol (final dose, 200 mg/day), alprazolam (2 mg/day), or placebo and were treated for 28 days. The efficacy of both active compounds was higher than the effects with placebo treatment. There were statistically significant differences (p < 0.05, according to the analysis of covariance) in the main outcome criterion (baseline-adjusted final means of an intent-to-treat analysis of the total scores on the Hamilton Rating Scale for Anxiety) and in secondary efficacy parameters, with global improvement of 47% for placebo and significantly more for opipramol (63%) and alprazolam (64%). Regarding safety and tolerability, no substantial differences in the number of adverse events observed between treatment groups were obvious. Sedation seemed more pronounced with alprazolam treatment than with opipramol or placebo. In this trial, it was demonstrated for the first time that opipramol, a strong but nonselective sigma site ligand, possesses anxiolytic efficacy superior to placebo in the treatment of GAD.
Seroquel also binds to sigma receptors........
'.........quetiapine, an atypical antipsychotic with high affinity for H1 and moderate affinity for sigma, alpha1, 5-HT2, alpha2 and D2 receptors.........'
Pentazocine, an opioid analgesic which tends to induce psychotic symptoms, acts as an agonist at sigma receptors. The sigma receptor may have a role in psychotic disorders. Perhaps it's not such a good thing that Lexapro acts as a sigma agonist!?
Dis Nerv Syst. 1975 Jul;36(7):404-5.
Pentazocine psychosis: a case of persistent delusions.
Blazer DG, Haller L.
A case of psychosis secondary to pentazocine is presented. The patient demonstrated hallucinations, preceptual aberrations, a distorted body image and delusional thinking. The delusional ideation persisted for a period of three weeks. Such a case of persistent delusional thinking secondary to pentazocine administration has not been reported previously.
Posted by krybrahaha78 on June 19, 2005, at 11:43:48
In reply to Calling darkhorse! Opipramol? » linkadge, posted by ed_uk on June 19, 2005, at 10:11:54
i heard somewhere that luvoxg affects the sigma receptors.
Posted by Phillipa on June 19, 2005, at 18:30:02
In reply to Re: Calling darkhorse! Opipramol?, posted by krybrahaha78 on June 19, 2005, at 11:43:48
All I know is I think luvox is putting me to sleep before the valium at night but I still wake up. Fondly, Phillipa
Posted by chemist on June 20, 2005, at 1:00:01
In reply to What is a sigma 1 receptor ??, posted by linkadge on June 19, 2005, at 0:21:06
> Does anyone know what a sigma 1 receptor is ??
>
>
> Linkadgehello there, chemist here...from Urani et al., Eur. J. Pharmacology 486 (2004) 151 - 161: ``The $\sigma_{1}$ receptor is a 223-amino acid protein, cloned in several animal species (naeer et al., 1996; Kekuda et al., 1996) that appeared devoid of analogy with any known mammalian protein. Selective $\sigma_{1}$ receptor ligands exert a potent neuromodulation on intracellular Ca$^{2+}$ mobilisations and excitatory neurotransmitter systems, including norandrenergic, glutamatergic and cholinergic responses (for review, see Maurice et al., 1999).''
...
``In a previous study, we have reported that the antidepressant-like efficacy of igmesine or PRE-084, two $\sigma_{1}$ receptor agonists, measured using the forced swim test, were potentiated in mice injected intracerebroventricularly (i.c.v.) with $\beta_{25-35}$-amyloai peptide (Urani et al., 2002). This enhanced efficacy was attributed to decreased progesterone levels in the hippocampus of $\beta_{25-35}$ animals and suggested that $\sigma_{1}$ agonists, due to their enhanced efficacy, may allow to alleviate the depressive symptoms associated with Alzheimer's disease (Urani et al., 2002). In the present study, these observations were confirmed and extended using the Alzheimer's disease model of rats chronically infused with $\beta$-amyloid-(1-40) protein (Nitta et al., 1994, 1997; Yamada et al., 1995, 1999). We examined the antidepressant-like efficacy of $\sigma_{1}$ receptor agonists, and particularly igmesine and the $\sigma_{1}$ receptor-related neuroactive steroid dehydroepiandrosterone sulfate, on the conditioned fear stress response of rats, as previously reported (Nabeshima et al., 1985; Kamei et al., 1997). The effect of $\beta$-amyloid infusion on brain neurosteroid levels was measures in basal and stressful conditions.''
i do hope that this ref. - and those cited, especially the review by Maurice et al., 1999) - is of use...all the best, chemist
Posted by Tom Twilight on June 20, 2005, at 6:47:46
In reply to Re: What is a sigma 1 receptor ?? » linkadge, posted by chemist on June 20, 2005, at 1:00:01
Opipramol sounds like an interesting drug
Its got a UK brand name so I assume its available here.
I wonder why we don't here more about it?
Posted by ed_uk on June 20, 2005, at 11:23:22
In reply to Opipramol available in the UK?, posted by Tom Twilight on June 20, 2005, at 6:47:46
Hi Tom :-)
>Opipramol available in the UK?
No :-(
See here for all drugs available in the UK.......
Kind regards,
Ed.
Posted by darkhorse on June 22, 2005, at 4:43:17
In reply to Calling darkhorse! Opipramol? » linkadge, posted by ed_uk on June 19, 2005, at 10:11:54
Hi Ed,Philipa and everyone :
Sorry for my slowness!!
Yes I took Insidon (Opipramol) when I lived for a while in the Sudan.
It was a very effective for anxiety from the first dose and I really liked it a lot.
I was also taking at the time Prozac and some benzos,but I stopped benzos and Opipramol enhanced my overall peace of mind.
Unfortunatly I stopped it because I left the country and could not find it in any other country I lived in.
It gives a sort of mellow,warm protective feeling without the apathy of the SSRIs,the dependance of the benzos,and the nightmarish Akathisia of the antipsychotics.
It is a pity that it is near extintion on this planet!
By the way its effect is very different from Luvox.
Opipramol may not suit everybody,but it is really a unique drug.
Ed and every body :Do you know where Opipramol exist now?
Best regarde,
Dark Horse .
Posted by rod on June 22, 2005, at 6:22:38
In reply to Re: Calling darkhorse! Opipramol?, posted by darkhorse on June 22, 2005, at 4:43:17
> Ed and every body :Do you know where Opipramol exist now?
Hi there,
Its available in Germany, Austria, Switzerland. Trade Name: Insidon.
I guess there are more countries.....
bye
Roland
Posted by darkhorse on June 22, 2005, at 7:55:53
In reply to Re: Calling darkhorse! Opipramol?, posted by rod on June 22, 2005, at 6:22:38
> > Ed and every body :Do you know where Opipramol exist now?
>
> Hi there,
>
> Its available in Germany, Austria, Switzerland. Trade Name: Insidon.
>
> I guess there are more countries.....
>
> bye
> Roland
>Hi Roland :
Unfortunatly it is not found anymore in Austria (I lived there).
Thanks a lot,
Dark Horse.
Posted by rod on June 22, 2005, at 8:16:51
In reply to Re: Calling darkhorse! Opipramol?, posted by darkhorse on June 22, 2005, at 7:55:53
> Hi Roland :
> Unfortunatly it is not found anymore in Austria (I lived there).
> Thanks a lot,
> Dark Horse.Hi Darkhorse
Na wie gehts? alles bestens? :-D
check out the screenshot I made
http://img64.echo.cx/img64/3003/insidon1qn.jpgIt is available and quite cheap.
Its in the "yellow box" which means that the insurance will only cover the costs if you fulfill special condition(s). Concerta for example is also in the yellow box and the condition is that you have to be a child.
But you can always buy it with a private prescriptin from a doc.About Germany, a person once said (some months ago) its available there.
About Switzerland:
search at http://www.documed.ch/ for Insidongreetings
Roland
Posted by ed_uk on June 22, 2005, at 10:09:51
In reply to Re: Calling darkhorse! Opipramol?, posted by darkhorse on June 22, 2005, at 4:43:17
Hi DH!
>Sorry for my slowness!!
Not a problem at all :-)
>It gives a sort of mellow,warm protective feeling without the apathy of the SSRIs,the dependance of the benzos,and the nightmarish Akathisia of the antipsychotics.
It sounds too good to be true! :-) What dose did you take?
>Do you know where Opipramol exist now?
It looks like Roland may be able to assist :-)
Kind regards
~Ed
Posted by ed_uk on June 22, 2005, at 10:12:24
In reply to Re: Calling darkhorse! Opipramol?, posted by rod on June 22, 2005, at 6:22:38
Hi Roli!
Have you ever taken opipramol? How did you like it?
Thank you :-)
Bye!
~Ed
Posted by rod on June 22, 2005, at 10:36:33
In reply to Re: Calling darkhorse! Opipramol? » rod, posted by ed_uk on June 22, 2005, at 10:12:24
Hi ed!
> Have you ever taken opipramol? How did you like it?
No. Havent tried it. I didnt know about the sigma antagonism and disliked its D2 (to a lesser extrend also D1) antagonism.I might give it a try in the future, but right at the moment im quite satisfied with my "cocktail". And I think I am at the right track at the moment. so no need for Opipramole....
greetings
Roland
Posted by ed_uk on June 22, 2005, at 10:50:15
In reply to Re: Calling darkhorse! Opipramol? » ed_uk, posted by rod on June 22, 2005, at 10:36:33
Hi Roli!
>disliked its D2 (to a lesser extrend also D1) antagonism.....
Yes, that's what would worry me aswell. It's reassuring that DH didn't get akathisia from it though :-)
>right at the moment im quite satisfied with my "cocktail........
It's a good combination for Roli :-D
Greetings!
~Ed
Posted by darkhorse on June 27, 2005, at 6:44:13
In reply to Re: Calling darkhorse! Opipramol? » darkhorse, posted by rod on June 22, 2005, at 8:16:51
Grussgott Roland :
Thank you for your correction.Yes Opipramol is found in Austria.
Can you supply me with a full list of all Antidepressants and benzodiazepines in Austria?Dankeschon!
Dark Horse
Posted by darkhorse on June 27, 2005, at 6:47:05
In reply to Re: Opipramol available in the UK? » Tom Twilight, posted by ed_uk on June 20, 2005, at 11:23:22
Does anyone know in what countries apart from Italy is delorazepam (EN) available?
Ed?
Thanks,
Dark Horse.
Posted by rod on June 27, 2005, at 7:22:49
In reply to Re:To Rod : Calling darkhorse! Opipramol? » rod, posted by darkhorse on June 27, 2005, at 6:44:13
> Grussgott Roland :
>
> Thank you for your correction.Yes Opipramol is found in Austria.
> Can you supply me with a full list of all Antidepressants and benzodiazepines in Austria?
>
> Dankeschon!
>
> Dark HorseHallo!
No, sorry, I wish I had one for myself. The only way I know of is to buy a "collection of drug-monographs" (book, CD or online)
For example at http://www.ami-info.at/
But you can test the fully featured online edition for 14 days for free... just say you are a student ;-)
You can browse the ATC-Code categories. There you can see which benzos, ADs etc. are availablebye
Roland
Posted by darkhorse on June 27, 2005, at 7:50:50
In reply to Re:To Rod : Calling darkhorse! Opipramol? » darkhorse, posted by rod on June 27, 2005, at 7:22:49
Thanks for the info Rod.
Do you live in Wien?Regards,
DH
Posted by ed_uk on June 27, 2005, at 10:41:37
In reply to Delorazepam? Ed?, posted by darkhorse on June 27, 2005, at 6:47:05
Hi DH!
I think delorazepam might be available in Portugal - brand Cipaxil. Not sure if it's still available though.
Was delorazepam particularly good?
Kind regards
~Ed
Posted by darkhorse on June 28, 2005, at 3:34:24
In reply to Re: Delorazepam? Ed? » darkhorse, posted by ed_uk on June 27, 2005, at 10:41:37
> Hi DH!
>
> I think delorazepam might be available in Portugal - brand Cipaxil. Not sure if it's still available though.
>
> Was delorazepam particularly good?
>
> Kind regards
>
> ~EdHi ED!
EN was the 2nd BZ I ever took,and that was in 1990 .
All I remember at the time is that it helped.I was severly depressed and anxious at the time.
I think I was prescribed 0.5mg 3 times a day.
I think 1mg of delorazepam = 1mg of Lorazepam.
You know that when you take a drug for the first time, you can feel immediatly that your body is accepring it.Delorazepam was like that.
Do you know its half- life?All the best!
DH
Posted by ed_uk on June 28, 2005, at 5:06:15
In reply to Re: Delorazepam? Ed? » ed_uk, posted by darkhorse on June 28, 2005, at 3:34:24
Hi Adam,
>Do you know its half- life?
http://www.psychotropics.dk/termplasma/view_Termplasma2.asp?Startchar=D
Kind regards
~Ed
Posted by darkhorse on June 28, 2005, at 6:02:37
In reply to Re: Delorazepam? Ed? » darkhorse, posted by ed_uk on June 28, 2005, at 5:06:15
Posted by Dr. Bob on June 28, 2005, at 12:15:48
In reply to Re:To Rod : Calling darkhorse! Opipramol? » rod, posted by darkhorse on June 27, 2005, at 7:50:50
> Do you live in Wien?
Sorry to interrupt, but I'd like to redirect follow-ups regarding Wien to Psycho-Babble Social. Here's a link:
http://www.dr-bob.org/babble/social/20050624/msgs/520515.html
Thanks,
Bob
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