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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 5 of 5. This is the beginning of the thread.
Posted by tinker on May 6, 2002, at 7:52:27
Hi I am looking at a spread sheet called Effects of Antidepressants on Neurotransmitters/Receptors from the Journal Of Clinical Psychopharmocology 16:3 (1996). Has anyone seen this sheet that could provide some answers to questions. What is meant by Blockade x (1), and Blockade x (2), and Blockade D(2), and what is DA reuptake. 5HT reuptake is listed for zoloft at 1-10, but for doxepin at 100-1000. What exactly does that mean. Is it that doxepin allows more reuptake of seratonin, and that zoloft inhibits this more? Any help or suggestions welcome.
Posted by katekite on May 6, 2002, at 17:04:26
In reply to Have you seen effects on neurotranmitters?, posted by tinker on May 6, 2002, at 7:52:27
The low numbers, 1,2 etc, most likely refer to types of receptors. ie serotonin (also known as 5HT) has over 15 identified receptors, some of them are thought to be involved in the therapeutic response to these meds.
Dopamine is abbreviated DA.
Reuptake refers to the process that gets rid of active neurotransmitter (NT), so anything that inhibits the process allows the NT to be around and helpful for longer. (if its helpful for you).
The other things i'm not sure of.... try looking up the drug itself on yahoo with the word 'mechanism'.
kate
Posted by Elizabeth on May 7, 2002, at 1:31:22
In reply to Have you seen effects on neurotranmitters?, posted by tinker on May 6, 2002, at 7:52:27
I'd need to see the article in order to figure out what some of those things are -- the information in your post doesn't provide enough context. I can tell you a few things:
5-HT is short for 5-hydroxytryptamine, AKA serotonin. DA is short for dopamine. D(2) probably refers to type 2 dopamine receptors (which are blocked by antipsychotic drugs and by certain tricyclic antidepressants).
The 5-HT reuptake values that you gave for Zoloft and doxepin are probably measures of their potency as serotonin reuptake inhibitors. These numbers (experimentally calculated, hence they give ranges rather than exact constants) are dissociation constants and are inversely related to the affinity for the receptor. So Zoloft is the more potent serotonin reuptake inhibitor of the two: if you take 100 mg of Zoloft, and your friend takes 100 mg of doxepin, the blockade of serotonin reuptake in your brain will be much more than in your friend's brain.
-elizabeth
Posted by tinker on May 7, 2002, at 6:38:54
In reply to Re: Have you seen effects on neurotranmitters?, posted by katekite on May 6, 2002, at 17:04:26
Looking further at the spread sheet called Effects of Antidepressants on Neurotransmitters/Receptors: the following is at the bottom of the sheet. "The ratio of Ki(nM)>100,000= then it gives values, and a second set of values is included after 1/Ki(M),0.001. My question is how do you know which set of values applies. Zoloft (Sertraline) has ++ beside NE reuptake, this could mean 10-1000 under the first set or 0.1-1 under the second set. Under 5 HT Reuptake it has ++++ which could mean 1-10 or 10-100. I am trying to find out the difference between clomapramine and zoloft. The pharmacist gave me this table. But I'm not sure how to apply the numbers. Any insights would be much appreciated.
Posted by Jodeye on May 7, 2002, at 12:43:31
In reply to Neurotransmitter/Receptor Tables, posted by tinker on May 7, 2002, at 6:38:54
> Looking further at the spread sheet called Effects of Antidepressants on Neurotransmitters/Receptors: the following is at the bottom of the sheet. "The ratio of Ki(nM)>100,000= then it gives values, and a second set of values is included after 1/Ki(M),0.001. My question is how do you know which set of values applies. Zoloft (Sertraline) has ++ beside NE reuptake, this could mean 10-1000 under the first set or 0.1-1 under the second set. Under 5 HT Reuptake it has ++++ which could mean 1-10 or 10-100. I am trying to find out the difference between clomapramine and zoloft. The pharmacist gave me this table. But I'm not sure how to apply the numbers. Any insights would be much appreciated.
Hi,
I am not sure what your numbers mean, but I beleive that a phrase such as "Substance X has a Ki50 of 10,000 nM" would mean that 10,000 nM of Substance X in your blood would effectively bind to 50% of the receptors in question.
nM = nano mole. (a quantity of molecules).
Ki = Inhibition constant.
Ki50 = 50% of the receptors in question have been bound to.Hope this helps, because it's not really clear to me either.
--Jodeye
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