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Does dopamine bind to TAAR?

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lemonman

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Sep 17, 2017
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Amphetamines

Amphetamines interact and bind to the TAAR receptor.

But what would happen if you had a drug that binded only dopamine to the TAAR receptor?.
 
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lemonman said:
Amphetamines interact and bind to the TAAR receptor.

But what would happen if you had a drug that binded only dopamine to the TAAR receptor?.
Click to expand...

Could you elaborate on your inquiry?
What do you mean by "a drug that binded only dopamine to the TAAR receptor" ?

Do you mean to say "a pharmaceutical that binds only to dopamine" ?
Perhaps "a pharmaceutical that is a TAAR ligand with activity in dopaminergic pathways" ?
I would like to refrain from making assumptions and guesswork, so I kindly await your response before answering.

Best,
Tez
 
Dopamine (and serotonin too) bind at TAAR1 and activate it, but weakly compared to other compounds. (ref)
 
^I'd imagine then that a substrate + VMAT inhibitor could function as a releasing agent even if the substrate itself wasn't active at TAAR1, as long as you could get the intracellular e.g. dopamine to rise high enough..
 
lemonman said:
Amphetamines interact and bind to the TAAR receptor.

But what would happen if you had a drug that binded only dopamine to the TAAR receptor?.
Click to expand...

TAAR1 is the only TAAR that is known to bind dopamine; there are 6 functional human TAARs.
 
sekio said:
Dopamine (and serotonin too) bind at TAAR1 and activate it, but weakly compared to other compounds. (ref)
Click to expand...

According to IUPHAR, the rank order of potency at TAAR1 is tyramine > β-phenylethylamine > octopamine = dopamine. hTAAR1 is also referred to as a high-affinity receptor for dopamine in this review.
 
lemonman said:
What do you guys think about the text below?. I thought that Stimulants activate TAAR1, if so why does the study below say this?


https://www.researchgate.net/public...ated_Receptor_1_Modulation_of_Dopamine_System
Click to expand...

The ref that Sekio linked above explains this, particularly figure 1.
It's worth mentioning that the D2 receptor has much higher neuronal expression in TAAR1 KO mice compared to when it's present. Also, the loss of TAAR1 precludes the formation of TAAR1-D2s receptor heterodimers. For these and other reasons, when considered alone, TAAR1 KO experiments don't actually shed much light on TAAR1's pharmacology because those other factors can't be controlled.

The review I linked above also covers the differences in central dopamine neuron physiology between TAAR1 KO and wild-type mice.
 
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