Archived: GL's Pharmacology Jargon Reference Guide

[Gun Lover]

Hai BLTC

It has come to my attention that many who frequent BLTC are often overwhelmed by some of the higher-level pharmacological discussion that takes place here sometimes. I'm going to attempt to explain what some of this jargon means, and hope it helps some of you. If it still seems daunting, just remember, the hardest part of getting into pharmacology is the excessive jargon.

Jargon Reference Guide:

Ligand - loosely defined as a signal triggering molecule, binding to a site on a target protein such as a receptor. All neurotransmitters are ligands for one or more receptors.

Ions - charged particles (Na⁺, K⁺, Mg²⁺, Ca²⁺, etc). What people mean when they say the brain is a biochemical electric machine, well this is the "electric" part.

Ionotropic Receptor – also known as a Ligand-gated ion channel, these are a sequence of proteins that open a tiny pore through which ions can travel into the neuron once a ligand binds to it. This picture helps explain
.
As you can see, when a ligand binds to the active site on the receptor, its shape changes and ions are allowed to flow.

Neuron - A special type of cell that is an integral part of the nervous system. They allow signaling from cell to cell.

Synaptic Cleft - The area in between two neurons that contains the actual drugs and neurotransmitters.


BTW -- vesicles are just little balls that carry around stuff (like neurotransmitters) inside your cells.

Neurotransmitters (NTs) - relatively small, simple molecules whose function is to facilitate electrical signaling between neurons in the synaptic cleft through physical and chemical means.

Dopamine (DA) - Among its other functions, dopamine is the most important molecule in the brain's reward system. Feelings of confidence, satisfaction, motivation, accomplishment, and attention are all largely controlled by DA. Drugs like cocaine and amphetamine cause there to be an abnormal excess of DA in the synaptic cleft, thus eliciting a recreational effect due to stimulation of the reward system.

Serotonin (5-HT) - 5-HT is the shorthand way of writing the chemical name of serotonin, 5-hydroxytryptamine. Serotonin plays a gigantic role in life: everything from heart development, controlling appetite & temperature, bone growth, and behavior is largely mediated by 5-HT. All psychedelics have efficacy at the serotonin type 2A receptor (5-HT_2A) to help elicit their effects. Depression is thought to be caused by low levels of 5-HT, thus doctors often prescribe SSRIs (selective serotonin reuptake inhibitors) to increase the amount of 5-HT neurotransmission.

Norepinephrine (NE) - Also known as noradrenaline, this neurotransmitter contributes to a change in heart rate, breathing patterns, and arousal. Along with DA, it is the basis of the reward system. This is the major neurotransmitter that is most responsible for the fight-or-flight mechanism.

Histamine - The primary NT in controlling the immune response, this NT is has a variety of functions including sleep regulation, alertness, gastric acid secretion, and inhibition of NT release. There are four different receptors for histamine, H₁-H₄, and each does a different function. By blocking the H₁ receptor with an antihistamine like benadryl, histamine can no longer bind to H₁, decreasing wakefulness. This is why H₁ antagonists are commonly used as sleep aids (diphenhydramine, doxylamine). More interestingly, the H₃ receptor which is the mostly expressed HR in the brain, modulates the release of many neurotransmitters in the brain. H₃ antagonists actually elicit stimulant and nootropic effects, likely due to the disinhibition of histamine-controlled NT release.

Catecholamines - a name referring to any of the three endogenous NTs that contain catechol: Dopamine, Epinephrine, and Norepinephrine. Here's a picture I made that explains it:


Endorphin - a portmanteau of "endogenous" and "morphine." This class of molecules are one of our bodies' natural opioid receptor ligands. Endorphins make you feel good because they bind to the MOR.

Endomorphin - more recently discovered than endorphins, these two endogenous opioids (endomorphin-1 & endomorphin-2) actually have the highest known affinity for the Mu-Opioid receptor than any other endogenous opioid.

Dynorphin - This is the second class endogenous opioids and has affinity for the kappa-opioid receptor. It plays a role in stress, analgesia, pain, and appetite.

Enkephalin - The third class of endogenous opioids. There are two different endogenous enkephalins, [Met]-enkephalin and [Leu]-enkephalin. The only structural difference between the two are the different amino acids at the end Methionine and Leucine. They both act similarly and are strong agonists of the Delta-Opioid receptor and weak agonists at the Mu-Opioid receptor.

Opiate - a naturally derived opioid receptor ligand originating from papaver somniferum, the opium poppy. Examples are morphine, codeine, and thebaine.

Opioid - any substance that acts upon any of the four major opioid receptors (Sigma, Kappa, Mu, Nociceptin). All opiates are opioids, but not all opioids are opiates.

Mu-Opioid Receptor (MOR) - this is the receptor responsible for blocking pain signals and what allows opioids to make us feel so fucking good. Specifically, the MOR type 2 receptor is responsible for that amazing euphoria. When an agonist binds to the MOR, the GABA molecules that regulate the release of dopamine in surrounding neurons are "hyperpolarized." Essentially, MOR agonists stop GABA from preventing dopamine neurotransmission, causing dopamine to start firing insanely fast, providing the high.

Kappa-Opioid Receptor (KOR) - activation of this receptor generally causes dysphoria, but partial agonists such as the primary active compound in Salvia, Salvinoran A, prove that activation of this receptor can also cause delirium, dissociation, and hallucinations.

Delta-Opioid Receptor (DOR) - Though not extremely well-studied, along with the MOR this receptor is responsible for most all pain-killing actions within the body. Interestingly, while DOR activation is responsible for mild pain relief, co-administration with a MOR agonist prevents the potentially fatal respiratory depression that classical opioid ODs are known for. Theoretically, if you also took a DOR agonist, you could dose an amount of heroin that would normally kill you and still be fine.

GABA - stands for gamma-aminobutyric acid. This is the principal inhibitory NT. GABA is ubiquitous; it helps mediate almost all of our conscious and subconscious functions. Too much GABA transmission, and you become very inebriated. Too little and you start convulsing and seizing. Recreationally speaking, the GABA type A (GABA_A) receptor is the one responsible for the pleasant effects of alcohol and benzodiazepines.

Blood-Brain Barrier (BBB) - A highly lipophilic (fat-loving) membrane that prevents polar molecules/drugs from reaching the brain. This is why you can't just get high by injecting dopamine and serotonin themselves (they are too polar to cross the BBB and thus don't get you high).

Endogenous - originating from within the body. NTs are endogenous compounds.

Exogenous - originating outside the body. These are usually drugs, but exogenous NTs have applications in medicine as well (epinephrine, etc.)

Affinity - a measure of how strongly a drug binds to a receptor. The binding affinity of a drug is often given in the units K_i. Remember, the lower the K_i, the higher the affinity. Also keep in mind AFFINITY ≠ EFFICACY.

Efficacy - a measure of how well a drug activates the receptor.

Agonist - a drug that displays both affinity and efficacy at a given receptor site.

Partial Agonist - a drug that has less affinity than the receptor's endogenous NT and displays some efficacy. For instance, LSD binds with less affinity to certain serotonin receptors than serotonin itself.

Full Agonist - a drug that binds with equal or greater affinity to a given receptor than its main endogenous NT. For instance, 2,5-Dimethoxy-4-Bromo-Amphetamine a.k.a. DOB binds with greater affinity to the serotonin 2B receptor than serotonin.

Antagonist - a drug that displays affinity towards a receptor, but has no efficacy.

Inverse agonist – a drug that has affinity for a receptor, but has the opposite effect of an agonist.

Here is a nice picture to better help you understand agonism/antagonism:


GPCR - a.k.a. G-protein coupled receptor. These are the receptors that most interesting to psychopharmacologists because they are the most prevalent type of receptor that NTs activate. For a more in-depth mechanism of how they work, see this thread.

Metabotrobic Receptor - in this type of receptor, a ligand binds, changes the receptor's shape, and triggers a cascade of intracellular actions that eventually cause a change in the cell. They often work in concert with ionotropic receptors present inside the cell. All the GPCRs are metabotropic.

Median Lethal Dose (LD₅₀): Used to measure the acute toxicity of a given substance, this ratio conveys the dosage at which 50% of the subjects tested died. Usually given in mg/kg, for instance around 95mg of cocaine per kilogram is the dose at which 50% of a given test subject (mice, in this case) died.

Bioavailability (BA) - the extent to which, and sometimes rate at which, the active drug or metabolite enters the bloodstream thereby gaining access to the active receptor site. (Credit to Merck/Rizzo)

Sympathomimetic - any drug that mimics the action of a neurotransmitter. A good example is Salbutamol. This drug effectively mimics the NT epinephrine but has a much better bioavailability and activity as an exogenous ligand.

Metabolite - when a drug enters the body it is subjected to these specialized proteins called enzymes. In essence, these enzymes digest the chemical, altering its structure allowing it to be more easily excreted. The resultant molecule that has been attacked by one or more enzyme(s) is called a metabolite. Sometimes the metabolite is a more potent drug than the substance originally ingested, but often it is not. Regardless of its relative potency to the original drug ingested, if a metabolite is psychoactive, it is known as an active metabolite.

Prodrug - a substance that when metabolized, turns into the desired active drug. The classic example of this is GBL. GBL is attacked by the lactamase enzyme upon entering the body and then forms GHB, a sympathomimetic GABA analogue.

Allosteric Modulator - a drug that binds to a receptor but not on its active site. Instead of competing with the endogenous ligand for that receptor, it merely binds to a different place on the receptor, changing the conformation of the active site at which the endogenous NT binds. In the case of benzodiazepines, they attach to the GABA_A receptors and increase the efficacy of normal GABA. This results in the GABA_A receptor being activated for longer periods of time, inducing a greater inhibitory effect.

Vasoconstriction - constriction (narrowing) of the blood vessels. 5-HT plays a major role in this.

Vasodilation - dilation (widening) of the blood vessels. This is done mainly through the actions of another NT, histamine.

-Ergic - a suffix acknowledging the activation of whatever NT comes before it. For instance, a GABAergic drug is one that acts upon GABA -- a drug such as alcohol. A serotonergic is a drug such as LSD.

-RI - a suffix that stands for "reuptake inhibitor." Examples: DARI (dopamine reuptake inhibitor), SSRI (selective serotonin reuptake inhibitor), and SNRI (serotonin-norepinephrine reuptake inhibitor). Reuptake inhibition of any given NT means that they stay in the synaptic cleft longer, increasing signaling activity, instead of being quickly reabsorbed by a surrounding neuron where they will have no effect. Cocaine doesn't actually act like a neurotransmitter to induce its effect, it actually inhibits the reuptake of serotonin, norepinephrine, and dopamine, and thus is known as a SNDRI (a.k.a. triple reuptake inhibitor).

I know I've likely left some key terms out, so please ask me to clarify any others if necessary.

[psychomanthis]

Props for educating the masses once more dude. If you keep this up soon we will be able to enjoy in-depth discussions with the whole BLTC community.

You could also add a list of the most common neurotransmitters with their abbreviations . DA = Dopamine, NE = nor-epinephrine etc.

Perhaps also a short description of the most common receptors and what effects they are associated with. 5-HT_2A associated with psychedelics, MOR associated with euphoria in opiates etc.

[Gun Lover]

Originally Posted by psychomanthis

Props for educating the masses once more dude. If you keep this up soon we will be able to enjoy in-depth discussions with the whole BLTC community.

You could also add a list of the most common neurotransmitters with their abbreviations . DA = Dopamine, NE = nor-epinephrine etc.

Perhaps also a short description of the most common receptors and what effects they are associated with. 5-HT_2A associated with psychedelics, MOR associated with euphoria in opiates etc.

Great idea, I'll edit the OP.

[AdMech]

Posting in epic thread. Nicely done!

[Gun Lover]

Added a bunch moar:

DA
5-HT
NE
MOR
GABA
endorphin
opiate
opioid
vasoconstriction/dilation
-ergic
-RI

[Rude Louis]

This thread gave me flashbacks to high school AP Chemistry and Biology. Fond memories.

[iMagiNation]

Fuck yeah. Good list. I'll see if I can't remember a few things to put up. Here's one:

LD-50: The dosage at which 50% of the subjects tested died. (you can put it in your own words or make it sound fancier if you want)

Also, bioavailability. This one is from the merck manual:

"Extent to which - and sometimes rate at which - the active moiety (drug or metabolite) enters systemic circulation thereby gaining access to the site of action."

Actually if you guys want I can copy a bunch of terms and stuff used in the Rx section of the merck manual to come up with some stuff to add to the list.

[Gun Lover]

Originally Posted by iMagiNation

Fuck yeah. Good list. I'll see if I can't remember a few things to put up. Here's one:

LD-50: The dosage at which 50% of the subjects tested died. (you can put it in your own words or make it sound fancier if you want)

Also, bioavailability. This one is from the merck manual:

"Extent to which - and sometimes rate at which - the active moiety (drug or metabolite) enters systemic circulation thereby gaining access to the site of action."

Good ones. Will add.

Originally Posted by iMagiNation

Actually if you guys want I can copy a bunch of terms and stuff used in the Rx section of the merck manual to come up with some stuff to add to the list.

Man, I forgot I downloaded a copy of Goodman and Gilman's Manual of Pharmacology and Therapeutics, the "bible of pharmacology." Shit, I'll have to dig that up and fix/clarify some of the definitions.

If you feel like looking through the Merck, that'd be cool.

[iMagiNation]

We should start up a super secret zoklet e-book trading ring. Because I've got a fuckton of pretty good ebooks ranging on everything from science to spirituality and I think it would be fun to trade some.

[Gun Lover]

Originally Posted by iMagiNation

We should start up a super secret zoklet e-book trading ring. Because I've got a fuckton of pretty good ebooks ranging on everything from science to spirituality and I think it would be fun to trade some.

Sounds cool. I have very few decent e-books

I also wound up adding LD50, bioavailability, prodrug, metabolite, and sympathomimetic.

[&Zenith]

Gun Lover: et al. is used to refer to multiple people solely, the abbreviation you are looking for is etc in the bit about epinephrine.

Originally Posted by iMagiNation

We should start up a super secret zoklet e-book trading ring. Because I've got a fuckton of pretty good ebooks ranging on everything from science to spirituality and I think it would be fun to trade some.

I have no books of relevance to trade, but here's a thanks for the thought and possible follow-through. Actually, I have some by Ragnar Benson that I haven't read through yet, but may be of interest to someone.

On an aside, how is "GABA" pronounced? I imagine it would be something like "gahbah" for brevity and for the sake of being able to add -ergic without sounding too idiotic. "G-A-B-A-ergic olol"

[Gun Lover]

Originally Posted by &Zenith

Gun Lover: et al. is used to refer to multiple people solely, the abbreviation you are looking for is etc in the bit about epinephrine.

You're right, fixt

On an aside, how is "GABA" pronounced? I imagine it would be something like "gahbah" for brevity and for the sake of being able to add -ergic without sounding too idiotic. "G-A-B-A-ergic olol"

Yeah, it's pronounced "gahbuh."

[AdMech]

Is it possible for an affinity to be 0? If not, is there a theoretical lower (upper) limit?

Also, if you want us to nitpick, lemme know; it seems churlish when faced with such a wealth of information, but on the other hand, I'm a perfectionist and, all told, would rather be told I missed a letter (or whatever) than not. I bring this up just 'cause editing is one of my few small talents.

[Mogli]

Excellent post, OP. The only other thing I can think of is allosteric regulation (classic example is benzodiazepines at the GABA-a receptor)

[Gun Lover]

Originally Posted by AdMech

Is it possible for an affinity to be 0? If not, is there a theoretical lower (upper) limit?

Well, since K_i is the distance between the active binding residues and the ligand, it is impossible for the two molecules to occupy the exact same space.

The closest/highest affinity you can get is the length of a covalent bond (around 130 picometers, IIRC) between the ligand and an amino acid in the active receptor site. These type of drugs are known as irreversible agonists/antagonists. They actually form a covalent bond with the active site and continue their signaling until the receptor undergoes endocytosis. Such an example is Oxymorphazone.

EDIT: I am illiterate. When a Ki value is given, the units are in moles, not meters. Duh

Also, if you want us to nitpick, lemme know; it seems churlish when faced with such a wealth of information, but on the other hand, I'm a perfectionist and might be but all told would rather be told I missed a letter, or whatever, than not.

Go ahead, especially if I'm wrong about some info. I typed most of this up on a whim, with most of it sitting on my hard drive for the longest time. I know it isn't perfect and I'm too drunk to proofread all that well.

[AdMech]

Originally Posted by Gun Lover

Well, since K_i is the distance between the active binding residues and the ligand, it is impossible for the two molecules to occupy the exact same space.

The closest/highest affinity you can get is the length of a covalent bond (around 130 picometers, IIRC) between the ligand and an amino acid in the active receptor site. These type of drugs are known as irreversible agonists/antagonists. They actually form a covalent bond with the active site and continue their signaling until the receptor undergoes endocytosis. Such an example is Oxymorphazone.

Excellent! Thanks for your cogent and lucid explanation. I should have figured that out; I once knew the first bit, about what exactly K_i is referring to, but it was totally gone until you refreshed my memory.

The stuff about irreversible agonists/antagonists is totally new to me, though, and that's cool as hell... I feel like a kid in the pharmacology candy store, who just spotted a bar of pure knowledge with crunchy cool-fact clusters. I was actually imagining a brain-destroying drug, but it turns out that nah, these are actually used - though I wonder how commonly; I don't think I've ever even heard of any diverted oxymorphazone - and receptors can be recycled. Whew.

[FON]

Thanks, OP. Zoklet needs more threads like this

[Gun Lover]

Glad you liked it, FON and Mogli.

Originally Posted by AdMech

Excellent! Thanks for your cogent and lucid explanation. I should have figured that out; I once knew the first bit, about what exactly K_i is referring to, but it was totally gone until you refreshed my memory.

Glad I was able to help

Originally Posted by AdMech

The stuff about irreversible agonists/antagonists is totally new to me, though, and that's cool as hell... I feel like a kid in the pharmacology candy store, who just spotted a bar of pure knowledge with crunchy cool-fact clusters.

Originally Posted by AdMech

I was actually imagining a brain-destroying drug, but it turns out that nah, these are actually used - though I wonder how commonly; I don't think I've ever even heard of any diverted oxymorphazone - and receptors can be recycled. Whew.

Its clinical use is quite limited, I'd imagine. It is probably mostly used to map the distribution of opioid receptors in the brain.

Psychomanthis and I had a nice conversation about the mechanism of opioid tolerance a while back.

Also, receptor internalization via endocytosis happens all the time. It's completely necessary and natural and definitely something that needs to be added to the list.

Originally Posted by 1337

Perhaps you can go into addiction depleting the body's endogenous neurotransmitters, or just the physical effects of addiction on the brain in general. How about serotonin syndrome, and drugs to not mix, how they interact, etc? I'm not too sure if this is going to be that thorough or is just our little primer.

I think those topics are better suited for another thread. I know I started to go in depth about some things in the OP, but I was really just trying to give examples.

Originally Posted by 1337

Excellent work, of course. I got wood.

Thanks

[Konglomo]

What about histamine? I almost feel like I'm stepping out of my league here, but doesn't it play an important role as a neurotransmitter.

[Gun Lover]

Originally Posted by Konglomo

What about histamine? I almost feel like I'm stepping out of my league here, but doesn't it play an important role as a neurotransmitter.

It is quite important for the immune system but not very instrumental in behavioral effects. To be honest, I really don't know much about it other than all histamine receptors are GPCRs.

If I were to include histamine, I might as well include acetylcholine and others that are indeed relevant to pharmacology, but not exactly BLTC.

I really should have titled this "GL's Psychopharmacology Jargon Reference Guide," as I was really only meaning to define terms relevant to how drugs effect behavior

I'll look into it a bit, though

[Konglomo]

Originally Posted by Gun Lover

It is quite important for the immune system but not very instrumental in behavioral effects. To be honest, I really don't know much about it other than all histamine receptors are GPCRs.

If I were to include histamine, I might as well include acetylcholine and others that are indeed relevant to pharmacology, but not exactly BLTC.

I really should have titled this "GL's Psychopharmacology Jargon Reference Guide," as I was really only meaning to define terms relevant to how drugs effect behavior

I'll look into it a bit, though

Like I said, I may be out of my league. My education on such matters only extends to high school biology and chemistry classes.

I know histamine plays a part in heroin and meth rushes when used intravenously. Mostly the flushing of skin, but I have no idea if it carries the drug.

[Lysergic Rain]

Originally Posted by Gun Lover

Sounds cool. I have very few decent e-books

I also wound up adding LD50, bioavailability, prodrug, metabolite, and sympathomimetic.

I also have a lot of good e-books

Add something about isomers

http://en.wikipedia.org/wiki/Dextroamphetamine vs http://en.wikipedia.org/wiki/Levoamphetamine is the best example I can think of

[King Owl]

Yeah, chirality would be an excellent one to add - especially enunciating the difference between enantiomers and diastereomers

[iMagiNation]

Originally Posted by Gun Lover

If I were to include histamine, I might as well include acetylcholine and others that are indeed relevant to pharmacology, but not exactly BLTC.

Whachuu talking about Willis? Choline and histamine are totally relevant to BLTC: on one hand we have anticholigenics like benadryl, scopolamine, etc, and on the other we have nootropics like piracetam and then our on backs we have opiates which cause itchies through histamines. All of those are relevant.

Also, I didn't really see it (might just be fucked up) but something about up vs down regulation? Or excitotoxicity?

[Gun Lover]

Originally Posted by Konglomo

Like I said, I may be out of my league. My education on such matters only extends to high school biology and chemistry classes.

I know histamine plays a part in heroin and meth rushes when used intravenously. Mostly the flushing of skin, but I have no idea if it carries the drug.

I didnt know that, definitely worth a look.

Originally Posted by King Owl

Yeah, chirality would be an excellent one to add - especially enunciating the difference between enantiomers and diastereomers

Yeah, Originally I was going to. I will when I don't have to type on a damn iPhone. Also, I stand corrected Rizzo. I'll get on it sometimes soon.

[psychomanthis]

Originally Posted by iMagiNation

Whachuu talking about Willis? Choline and histamine are totally relevant to BLTC: on one hand we have anticholigenics like benadryl, scopolamine, etc, and on the other we have nootropics like piracetam and then our on backs we have opiates which cause itchies through histamines. All of those are relevant.

My thoughts exactly, also we must not forget the sedating effects of first generation antihistamines.

However too include all this information would make this thread more like GL's Pharmacology Jargon dictionary instead of guide. So to remedy this problem i suggest GL issues a weekly column discussing the various aspects of psychopharmacology in an attempt to further increase the community's scientific understanding of the various mechanisms by which drugs influence the human mind and body.

I would like to see this. Hell, i'd post one myself but while my knowledge of such subjects is considerable it is outshown by the vast amount of raw information GL is able to pump out

[FON]

Originally Posted by psychomanthis

So to remedy this problem i suggest GL issues a weekly column discussing the various aspects of psychopharmacology in an attempt to further increase the community's scientific understanding of the various mechanisms by which drugs influence the human mind and body.

This would be brilliant. I don't blame GL if he doesn't want to but a thread like that would be invaluable to the community.

[Chris Hansen]

Awesome guide man! Thanks a ton! I love knowing all I can about pharms and what they do to my body and how they work so this type of thing is right up my alley.

[Gun Lover]

Originally Posted by FON

This would be brilliant. I don't blame GL if he doesn't want to but a thread like that would be invaluable to the community.

Thanks for all the good reviews, guys. I'm really pleased to see all the genuine interest we have on this forum.

While I can't promise you all a weekly thread of this magnitude, I definitely am not stopping here. I've still got a bunch to learn, but I promise I'll start making more threads that explain various topics as clearly as I can. Perhaps I could live with a monthly deadline

I'm thinking the next one will be more about basic organic structures and how they interact with protein structures. I know many people here have never taken an organic chemistry course (I'm only in o-chem 1 ) and are bewildered by skeletal drawings. I'll attempt to explain them along with protein structure and how it relates to pharmacology.

[iMagiNation]

Well Idk if you guys are aware but Konglomo and I are trying to start up a BLTC ezine, based roughly off of my Dose zine project. Perhaps I will send some PMs to regulars that I think could contribute and see who would be interested. I'm probably going to make a thread soon I just need to get an outline written down off what we're looking at, scope wise.

...this could be really fun. who's down?

[JC Denton]

Nice job.

Looks like it's a work in progress. Here's some suggestions.

Norepinephrine (NE) - Also known as noradrenaline, this neurotransmitter contributes to a change in heart rate, breathing patterns, and arousal. Along with DA, it is the basis of the reward system. This is the major neurotransmitter that is most responsible for the fight-or-flight mechanism.

Don't forget epinephrine/adrenaline.

Also the term Catecholamine, the blanket term for DA, NE, and epinephrine. I've seen it used here before.

Also, trace amines (ie. PEA, tryptamine, tyramine, etc.). A lot of drugs have some affect on TAAR.

GABA - stands for gamma-aminobutyric acid. This is the principal inhibitory NT. GABA is ubiquitous; it helps mediate almost all of our conscious and subconscious functions. Too much GABA transmission, and you become very inebriated. Too little and you start convulsing and seizing. Recreationally speaking, the GABA type A (GABAA) receptor is the one responsible for the pleasant effects of alcohol and benzodiazepines.

Put in Glutamate, the main excitatory neurotransmitter as opposed to GABA - main inhibitory. Maybe talk about excitation/inhibition, and sympathetic/parasympathetic NS too.

Endorphin - a portmanteau of "endogenous" and "morphine." These are one of our bodies' natural opioid receptor ligands.

I'd expand on this to include all the different endorphins (ie. enkephalin, endomorphin, dynorphin, nociceptin, opiorphin, etc.)

Mu-Opioid Receptor (MOR) - this is the receptor responsible for blocking pain signals and what allows opioids to make us feel so fucking good. Specifically, the MOR type 2 receptor is responsible for that amazing euphoria.

Perhaps also mention other opioid receptors like delta and kappa.


yea, let me know if you need help with anything. I've like 300+ pages of pharmacology and biology notes.

[psychomanthis]

Originally Posted by Gun Lover

Thanks for all the good reviews, guys. I'm really pleased to see all the genuine interest we have on this forum.

While I can't promise you all a weekly thread of this magnitude, I definitely am not stopping here. I've still got a bunch to learn, but I promise I'll start making more threads that explain various topics as clearly as I can. Perhaps I could live with a monthly deadline

I'm thinking the next one will be more about basic organic structures and how they interact with protein structures. I know many people here have never taken an organic chemistry course (I'm only in o-chem 1 ) and are bewildered by skeletal drawings. I'll attempt to explain them along with protein structure and how it relates to pharmacology.

Good stuff

[dephdiddy]

Originally Posted by OMr_duckO

Nice job.

Put in Glutamate, the main excitatory neurotransmitter as opposed to GABA - main inhibitory. Maybe talk about excitation/inhibition, and sympathetic/parasympathetic NS too.

is this a valid reason for why gabapentin gives me diarrhea of the mouth. i just go on and on and on and on.

[Friendly Odors?]

Wow this thread is informative

[JC Denton]

Originally Posted by dephdiddy

is this a valid reason for why gabapentin gives me diarrhea of the mouth. i just go on and on and on and on.

lol nah, despite being a GABA analogue, it has no affect on GABA receptors.

But I know what you mean. I think it just inhibits or slows down practically all neurotransmitters by reducing calcium currents. Though pharmacologists still aren't sure what the exact mechanism is.

[panthrax]

My, my! What a gorgeous thread! Earned an archive.

+1

[panthrax]

Gun Lover, would you mind me placing this guide on my website? Of course, all accreditation will go towards you.

[mksnowboarder]

This was a very good thread. I knew how benzos act at the receptor sites, but did not know that a molecule that behaves so is called an allosteric modulator.

And everyone that had suggestions for GL - go make your own thread, or explain those things in this one. It's unreasonable to expect him to do that much on his own, and he'd get bored and burn out if he tried. Plus I'm impatient.

And, alas, I have no eBooks to trade, but I would happily accept yours as gifts. Please PM me if you have some good ones; I lose all my such files as my computers die.

mike

[iMagiNation]

Originally Posted by panthrax

My, my! What a gorgeous thread! Earned an archive.

+1

Thank god we have a moderator that actually archives shit now. FUCK. So many good threads have gone by without being archived.

[mksnowboarder]

Originally Posted by 1337

^Who the fuck are you? Certainly not "The Boss" anymore.

You might not mean to come off as a completely conceited asshole with this post, but you do.

I really don't give a shit how I come off to you. I come here to learn, and to teach others when I can, not to cultivate a positive image of me in your head. Who the fuck are you, anyways?

If only we had a moderation staff who pruned off topic posts!

mike