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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 23 of 23. This is the beginning of the thread.
Posted by linkadge on September 22, 2005, at 14:10:27
Supposedly SSRI's are neurotrophic via activation of SIG-1R receptors. Do any other drugs/herbs have this effect ?
Linkadge
Posted by djmmm on September 22, 2005, at 14:48:52
In reply to which drugs agonise SIG-1R, posted by linkadge on September 22, 2005, at 14:10:27
> Supposedly SSRI's are neurotrophic via activation of SIG-1R receptors. Do any other drugs/herbs have this effect ?
>
> LinkadgeImipramine and Fluvoxamine are both SIG-1R agonists, as are Pentazocine (Talwin), and cocaine.
The only "supplement" I know of that is a SIG-1R agonist is Pregnenolone (precursor to DHEA).. I believe DHEA may be an agonist, also.
Posted by Chairman_MAO on September 22, 2005, at 15:17:02
In reply to which drugs agonise SIG-1R, posted by linkadge on September 22, 2005, at 14:10:27
dextromethorphan is a reasonably potent sigma agonist. DHEA is a sigma1 agonist as well. Naturally speaking, hypericin is one I think.
Howz-a-that?
Posted by linkadge on September 22, 2005, at 16:14:40
In reply to Re: which drugs agonise SIG-1R » linkadge, posted by Chairman_MAO on September 22, 2005, at 15:17:02
Strange, all of the mentioned do posess antidepressant properties in one respect or another.
Hmm.
Linkadge
Posted by blueberry on September 22, 2005, at 19:08:38
In reply to which drugs agonise SIG-1R, posted by linkadge on September 22, 2005, at 14:10:27
Interesting post, except I don't know what SIG-1R is. Can anyone fill me in?
Posted by linkadge on September 22, 2005, at 19:25:55
In reply to Re: which drugs agonise SIG-1R....what is SIG-1R?, posted by blueberry on September 22, 2005, at 19:08:38
Some receptor in the brain, that (when activated) enhances the ability of a growth factor in the brain to extend the length of neurons.
Someone can probably be more techical than that.
Linkadge
Posted by Chairman_MAO on September 22, 2005, at 21:06:21
In reply to Re: which drugs agonise SIG-1R, posted by linkadge on September 22, 2005, at 16:14:40
do not forget that sigma receptors are likely partly responsible for the profound dysphoria one can experience on DXM and pentazocine.
Posted by Declan on September 22, 2005, at 21:51:06
In reply to Re: which drugs agonise SIG-1R » linkadge, posted by Chairman_MAO on September 22, 2005, at 21:06:21
What about dextramoramide (Palfium)? It doesn't do anything to this receptor? For a strong opiate it has some dysphoric/creepy qualities after a bit. Maybe it's just antcholinergic like pethedine.
Declan
Posted by linkadge on September 23, 2005, at 9:14:43
In reply to Re: which drugs agonise SIG-1R, posted by Declan on September 22, 2005, at 21:51:06
So sigma receptor agonism can cause dysphoria?
Luvox causes intense dysphoria in me.
Linkadge
Posted by zeugma on September 23, 2005, at 15:31:35
In reply to really ?, posted by linkadge on September 23, 2005, at 9:14:43
if I'm not mistaken...isn't pentacozine dysporia due to kappa receptor agonism?
-z
Posted by ed_uk on September 23, 2005, at 16:00:54
In reply to Re: really ?, posted by zeugma on September 23, 2005, at 15:31:35
Hi Zeugie!
>isn't pentacozine dysporia due to kappa receptor agonism?
I used to think that..... but I suspect I was wrong.
~ed
Posted by zeugma on September 23, 2005, at 17:25:08
In reply to Re: really ? » zeugma, posted by ed_uk on September 23, 2005, at 16:00:54
hi ed,
why did you change your mind? All sources I've seen impute dysphoria to kappa agonism, and that seems to be a class effect of kappa-agonists and not just to pentacozine.
-z
Posted by Declan on September 24, 2005, at 15:39:17
In reply to Re: really ? » ed_uk, posted by zeugma on September 23, 2005, at 17:25:08
hey z, do you know what other opiates are kappa-agonists?
Declan
Posted by zeugma on September 24, 2005, at 18:36:56
In reply to Re: really ?, posted by Declan on September 24, 2005, at 15:39:17
I'm not a pharmacological expert, but I have come across a reference somewhere that long-term users of morphine can suffer depression as a result of kappa agonism. And I know that the hallucinogen salvinorum A is a kappa partial agonist.
My personal experience with opiates is limited. I was on Strattera last year, and its metabolite, 4-hydroxyatomoxetine, is a kappa partial agonist. I speculated that this was the cause of the incredibly unpleasant anhedonic depression I developed while taking the drug. It recurred each time I tried to restart the drug, and was distinct from the also unpleasant forms of endogeneous depression I'm prone to.
BTW, I did a quick search for info on a med you mentioned, whose name I forget now (trade name began with P). Far from being anticholinergic, it appeared to be pro-cholinergic. Generally speaking, anticholinergics are antidepressant and mania-inducing, while pro-cholinergics are antimanic and depressant. Or so theory says.
-z
Posted by Declan on September 24, 2005, at 19:47:49
In reply to Re: really ? » Declan, posted by zeugma on September 24, 2005, at 18:36:56
That was Palfium. I took it once when I had no habit, and saw a tree, with the most lovely green light in it, real Kubla Khan stuff. Never forgotten it. But lousy for social interaction, unlike most of them.
Declan
Posted by ed_uk on September 25, 2005, at 9:32:42
In reply to Re: really ? » zeugma, posted by Declan on September 24, 2005, at 19:47:49
Hi Dec,
Is Palfium still available in Australia? It was discontinued in the UK a while ago.
~Ed
Posted by ed_uk on September 25, 2005, at 9:35:40
In reply to Re: really ? » ed_uk, posted by zeugma on September 23, 2005, at 17:25:08
Hi Z,
>All sources I've seen impute dysphoria to kappa agonism, and that seems to be a class effect of kappa-agonists and not just to pentacozine.
Most kappa antagonists have many other pharmacological actions eg. mu antagonism, sigma agonism. These actions might be dysphoric. Some kappa agonists such as OxyContin are generally euphoric.
Kind regards
~Ed
Posted by linkadge on September 25, 2005, at 10:13:57
In reply to Re: really ? » zeugma, posted by ed_uk on September 25, 2005, at 9:35:40
Some studies suggest that the sigma agonism is responsable for the neurotrophic effects of certain psychiatric drugs.
Does this mean growing new neurons must be accompanied by dysphoria ?
What is the general role of the sig-1r receptors ?
Linkadge
Posted by ed_uk on September 25, 2005, at 10:41:48
In reply to Re: really ?, posted by linkadge on September 25, 2005, at 10:13:57
Hi Link,
>Does this mean growing new neurons must be accompanied by dysphoria?
I don't think so. Perhaps different sigma receptors are involved? I can't say I know much about sigma receptors.
~Ed
Posted by Declan on September 25, 2005, at 14:28:11
In reply to Re: really ? » Declan, posted by ed_uk on September 25, 2005, at 9:32:42
Hi Ed
I think Palfium was discontinued here when they rationalised the opiate system. They got rid of Dilaudid round the same time, I think.
Declan
Posted by ed_uk on September 26, 2005, at 16:32:31
In reply to Re: really ? » ed_uk, posted by Declan on September 25, 2005, at 14:28:11
Hi Dec,
>They got rid of Dilaudid round the same time, I think.
We've got hydromorphone here: Palladone and Palladone CR. Palladone CR is supposed to last 12 hours.
~ed
Posted by Declan on September 26, 2005, at 17:51:32
In reply to Re: really ? » Declan, posted by ed_uk on September 26, 2005, at 16:32:31
Ed, there is a professor of pharmacology or something here who put forward hydromorphone as the appropriate heroin substitute, thus getting round trade sanctions on the Tasmanian opium growers in the event of violation of the WHO's ban.
Cuppla days in the papers, but nice to see anyway.
Declan
Posted by ed_uk on September 27, 2005, at 15:12:30
In reply to Re: really ? » ed_uk, posted by Declan on September 26, 2005, at 17:51:32
Hi Dec,
Diamorphine (heroin) is in short supply in the UK at the moment. It's usually out of stock at the wholesaler. Doctors are prescribing more fentanyl instead.
~Ed
This is the end of the thread.
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