Psycho-Babble Neurotransmitters Thread 836314

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beta2- and beta3-adrenoceptors

Posted by undopaminergic on June 24, 2008, at 22:23:38

Activation of beta2- and beta3-adrenergic receptors greatly enhances the uptake of aromatic amino acids into the CNS across the blood-brain-barrier. Since several of these amino acids are precursors to the monoamine neurotransmitters - dopamine, noradrenaline and serotonin - the potential practical implications are obvious.

In other words, systemic (ie. tablets rather than inhalers) beta2-adrenergic-agonists such as clenbuterol and salbutamol/albuterol (Ventoline) may be interesting additions to a psychopharmacological regimen. In rare cases, they may even be sufficient as monotherapy.

 

Re: beta2- and beta3-adrenoceptors

Posted by undopaminergic on June 25, 2008, at 1:20:26

In reply to beta2- and beta3-adrenoceptors, posted by undopaminergic on June 24, 2008, at 22:23:38

Furthermore, it appears that the kidneys will reduce their L-dopa consumption substantially in response to beta2-adrenergic stimulation - thus leaving more L-dopa for the brain.

It seems plausible that other organs may respond with similar abstinence to beta2-agonism.

 

Re: beta2- and beta3-adrenoceptors

Posted by dbc on June 26, 2008, at 14:25:56

In reply to Re: beta2- and beta3-adrenoceptors, posted by undopaminergic on June 25, 2008, at 1:20:26

I imagine this would have a major effect on things like blood pressure and might be a bit risky.

 

Re: beta2- and beta3-adrenoceptors » undopaminergic

Posted by Horned One on June 29, 2008, at 11:12:16

In reply to beta2- and beta3-adrenoceptors, posted by undopaminergic on June 24, 2008, at 22:23:38

I remember someone at work taking salbutamol tablets for severe asthma. I don't think it had the effect you were hoping for based on the pharmacology. It made her extremely nervous, agitated, jumpy, almost to the point of having a movement disorder. Her face and neck muscles used to jerk uncontrollably. She also had a severe hand tremor. In short she looked and acted like a speed freak. Ironically I was taking amphetamine at the time and had the same sort of tremors.

I don't know whether it altered her mood, but I couldn't help but notice her overwhelming anxiety and restlesness.

-Horny

 

Re: beta2- and beta3-adrenoceptors

Posted by undopaminergic on June 30, 2008, at 13:22:44

In reply to Re: beta2- and beta3-adrenoceptors, posted by dbc on June 26, 2008, at 14:25:56

> I imagine this would have a major effect on things like blood pressure and might be a bit risky.
>

Beta2-adrenoceptors dilate blood vessels, thus lowering pressure, but they also increase heart rate, which raises blood pressure. The net effect may be either lowered or increased blood pressure, depending on dose and other factors.

Treatment with beta2-agonists after a heart attack (myocardial infarction) is generally more beneficial than the standard protocol, which is treatment with beta1-antagonists ("beta-blockers"). One of the reasons for that is that beta2-agonists dilate coronary blood vessels, thus enhancing myocardial perfusion and oxygenation.

It's my conclusion that beta2-adrenergic stimulation is pretty safe from a cardiovascular point of view, except perhaps under certain pathological conditions.

Beta3-adrenoceptors seem to be even more effective (than beta2-ones) in enhancing the uptake of aromatic amino acids across the blood-brain-barrier and into the CNS. They also stimulate lipolysis, and may therefore be useful in getting rid of surplus fatty tissue. To my current knowledge, beta3-adrenoceptors are of little or no cardiovascular significance (although I suspect a more thorough investigation would reveal some minor involvement).

 

Re: beta2- and beta3-adrenoceptors

Posted by undopaminergic on June 30, 2008, at 14:29:29

In reply to Re: beta2- and beta3-adrenoceptors » undopaminergic, posted by Horned One on June 29, 2008, at 11:12:16

> I remember someone at work taking salbutamol tablets for severe asthma. I don't think it had the effect you were hoping for based on the pharmacology. It made her extremely nervous, agitated, jumpy, almost to the point of having a movement disorder. Her face and neck muscles used to jerk uncontrollably. She also had a severe hand tremor. In short she looked and acted like a speed freak. Ironically I was taking amphetamine at the time and had the same sort of tremors.
>
> I don't know whether it altered her mood, but I couldn't help but notice her overwhelming anxiety and restlesness.
>
> -Horny

I was aware that these drugs often produce some tremor and nervousness that are most pronounced upon initiation of use and diminishing in intensity with continued treatment. The case you described seems more extreme.

Although in certain cases, salbutamol or another beta2-agonist might be sufficient as monotherapy, that seems very unlikely in more refractoy cases, where such a drug might be a useful sdjunct.

My plan is to test whether beta2-agonists can render precursor amino acids effective. Most of the precursor amino acids I've tried have had very little - if any - effect, and the rest produced little but adverse effects. I wonder if, for instance, salbutamol + L-dopa, or salbutamol + tryptophan would be more useful than the amino acids alone?

 

Re: beta2- and beta3-adrenoceptors

Posted by Amigan on July 6, 2008, at 14:56:25

In reply to Re: beta2- and beta3-adrenoceptors, posted by undopaminergic on June 30, 2008, at 14:29:29

It sounds like an interesting experiment.

 

Re: beta2- and beta3-adrenoceptors

Posted by jrbecker76 on July 21, 2008, at 23:52:12

In reply to beta2- and beta3-adrenoceptors, posted by undopaminergic on June 24, 2008, at 22:23:38

> Activation of beta2- and beta3-adrenergic receptors greatly enhances the uptake of aromatic amino acids into the CNS across the blood-brain-barrier. Since several of these amino acids are precursors to the monoamine neurotransmitters - dopamine, noradrenaline and serotonin - the potential practical implications are obvious.
>
> In other words, systemic (ie. tablets rather than inhalers) beta2-adrenergic-agonists such as clenbuterol and salbutamol/albuterol (Ventoline) may be interesting additions to a psychopharmacological regimen. In rare cases, they may even be sufficient as monotherapy.

a beta-3 adrenoreceptor agonist, amibegron, is currently in late-stage clinical trials for depression/anxiety. Unfortunately, I have a feeling it will be announced as discontinued soon.

JB

 

Re: beta2- and beta3-adrenoceptors

Posted by undopaminergic on August 10, 2008, at 7:18:13

In reply to Re: beta2- and beta3-adrenoceptors, posted by Amigan on July 6, 2008, at 14:56:25

> It sounds like an interesting experiment.

Unfortunately, it didn't seem to enhance the efficacy of L-dopa, at least not with 8 mg salbutamol + 50 mg L-dopa (with benserazide). Perhaps I will revisit this concept once I acquire a suitable beta3-agonist.

On the other hand, it improved the condition of my skin. It think it may have a slight slimming action too, but I'm not sure, as buprenorphine+methylphenidate were already doing a good job at that.

 

Re: beta2- and beta3-adrenoceptors

Posted by Amigan on August 10, 2008, at 15:45:03

In reply to Re: beta2- and beta3-adrenoceptors, posted by undopaminergic on August 10, 2008, at 7:18:13

Thanks for sharing your findings with us.


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