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What part of a drug molecule does the receptor attach to?

Ballz_Trippington

Ballz_Trippington

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I'm very sorry if this has been asked to death. I have tried find the answer to this with the search engine but to no avail. I also must apologize for not having a background in chemistry or science at all really.
So what I'm extremely curious about is where for example a chemical like say 4-aco-dmt attaches to its corresponding receptor (what part of the chemicals structure attaches).
I am not sure how to post pictures on BL (please have mercy on this genuinely curious greenlighter).
I would assume that attaches at the "antler" looking portion of 4-aco-dmt's structure but I'm really just guessing.
Any wisdom for the wise souls at BL would be immensely appreciated.
Thank you so much!
 
Drug molecules are usually small molecules, often an fairly simple amine. Receptors are big ol' proteins, vast in comparison. In fact, you should be thinking about which part of a receptor a drug binds to, not the other way around. Hydrogen bonds always involve nitrogen or oxygen atoms, so those are likely to be important in receptor binding. Also to be considered are charged atoms, and lipophobicity/hydrophobicity of portions of the molecule.
 
Sometimes exogenous ligands will bind to the same area of the receptor as the endogenous ligand, particularly commonly when the two compounds are closely structurally related. Other times, drugs will bind elsewhere, non-competitive antagonists being a common example (as the endogenous ligand can still bind (hence "non-competitive"), so the drug must bind elsewhere, causing different changes to the receptor, leading to downstream changes distinct from those of agonists).

ebola
 
babylonboy said:
Hydrogen bonds always involve nitrogen or oxygen atoms, so those are likely to be important in receptor binding.
Click to expand...

Just thought I'd point out/add that fluorine is another common participant in hydrogen bonding. It's presence or absence in a ligand can make a big difference in it's binding. One example of this, admitedly not an excellent one but the one that comes to my mind first is 2,5-dimethoxyamphetamine vs. DOF. Like I said, this is an imperfect example, since DOF has never been trialed in man, but animal trials imply a it is a psychedelic with a potency that lies between 1/4th and 1/6th that of DOI. Compare this to the desfluro analogue of DOF, 2,5-dimethoxyamphetamine, which is not known to be psychedelic at any dose, but has been said to produce a 'speedy' feeling around 150-200mg.
 
I was under the impression that the substance actually solutes into the receptor, no? So I thought that the same way sugar solutes into water (for instance) is the same way a substance binds to a receptor. Was I wrong?
 
Yea I would agree with that more so of a complex formation. Also kind of like a KEY and a LOCK. The key must fit into the lock and then a change can occur.
The key would be the drug and the lock would be the receptor. But it is rather amazing On a molecular note their are many significant changes going on when drugs as well as Endogenous compound act on Receptors. For example Norepinephrine Noradrenaline stimulates postsynaptic Alpha 1 Receptors to transduce signals but for the Signaling to stop a molecule of Noradrenaline has to activate presynaptic alpha 2 receptor to stop further outflow of Noradrenaline this is Auto-Inhibition.

NeuroPharmacology is awesome
 
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