chemistry

TGF-8027

TGF-8027 is a chemistry topic covered in the lgStudy science library. This page brings together a partial reference excerpt, illustrations, worked examples, real-world applications and a short study plan, so you can understand TGF-8027 rather than just read about it. In short: TGF-8027, or TGF-8-027, also known as N-[1-(2-hydroxyphenyl)ethyl]-2,5-dimethoxy-4-cyanophenethylamine, is a highly selective serotonin 5-HT2A receptor agonist and putative serotonergic psychedelic of the phenethylamine, 2C, and 25-NB (NBOH) families. It is one of the most selective serotonin 5-HT2A receptor agonists known and shows much greater selectivity than earlier agents like 25CN-NBOH, DMBMPP, and LPH-5.

Key takeaways

TGF-8027 belongs to chemistry; place it in that map before memorising details.
Learn the definition first, then one example that makes the definition concrete.
Connect TGF-8027 to a quantity you can measure, compute or draw — that is where exam questions come from.
Reproduce the core statement of TGF-8027 from memory before moving on to harder problems.

Reference excerpt

TGF-8027, or TGF-8-027, also known as N-[1-(2-hydroxyphenyl)ethyl]-2,5-dimethoxy-4-cyanophenethylamine, is a highly selective serotonin 5-HT2A receptor agonist and putative serotonergic psychedelic of the phenethylamine, 2C, and 25-NB (NBOH) families. It is one of the most selective serotonin 5-HT2A receptor agonists known and shows much greater selectivity than earlier agents like 25CN-NBOH, DMBMPP, and LPH-5. The drug produces psychedelic-like effects in rodents and hence may be hallucinogenic in humans. TGF-8027 was first described in the literature in 2025.

Interactions

Pharmacology

Pharmacodynamics TGF-8027 acts as a highly selective serotonin 5-HT2A receptor full agonist. Its affinities (Ki) were 7.4 nM at the serotonin 5-HT2A receptor, 390 nM at the serotonin 5-HT2B receptor, and 1,100 nM at the serotonin 5-HT2C receptor. The drug's EC50Tooltip half-maximal effective concentration and EmaxTooltip maximal efficacy values in terms of Gq dissociation were 3.3 nM (91%) at the human serotonin 5-HT2A receptor, 7,600 nM (45%) at the human serotonin 5-HT2B receptor, and 160 nM (123%) at the human serotonin 5-HT2C receptor. It was also assessed at these receptors with other assays. In addition, TGF-8027 was screened at a large panel of other targets, including receptors and transporters, and showed relatively little affinity at these sites. With regard to selectivity for the human serotonin 5-HT2A receptor over the human serotonin 5-HT2C receptor, TGF-8027 showed 149-fold selectivity in terms of affinity, 48.5-fold selectivity in terms of Gq dissociation, 84.5-fold selectivity in terms of calcium flux, and 2,450-fold selectivity in terms of IP1 accumulation. It is far more selective as an agonist of the serotonin 5-HT2A receptor over the serotonin 5-HT2C receptor than previous selective serotonin 5-HT2A receptor agonists such as 25CN-NBOH, DMBMPP, and rac-LPH-5 (fold selectivity for Gq dissociation in the same study of 10.0, 13.5, and 4.4, respectively). Previous research had not rigorously assessed the selectivity of these earlier compounds via employment of multiple selectivity assays. TGF-8027 was less selective for the mouse serotonin 5-HT2A receptor over the mouse serotonin 5-HT2C receptor, but still showed about 15-fold selectivity for the former over the latter in terms of Gq dissociation. In accordance with its serotonin 5-HT2A receptor activation, the drug robustly induces the head-twitch response, a behavioral proxy of psychedelic effects, in mice. As such, it would be expected to produce psychedelic effects in humans. The compound is a racemic mixture of (+)- and (–)-enantiomers, with the (–)-enantiomer being a more potent serotonin 5-HT2A receptor agonist but the (+)-enantiomer being more selective for activation of the serotonin 5-HT2A receptor over the serotonin 5-HT2C receptor.

Chemistry TGF-8027, also known as N-[1-(2-hydroxyphenyl)ethyl]-2,5-dimethoxy-4-cyanophenethylamine, is a substituted phenethylamine and a 2C and 25-NB (NBOH) derivative. It is specifically the derivative of 25CN-NBOH in which the benzyl group has been α-methylated. The compound is a racemic mixture of (+)- and (–)-enantiomers. A series of other analogues of TGF-8027 have also been reported, some of which show further improved serotonin 5-HT2A receptor selectivity relative to TGF-8027 itself.

History TGF-8027 was first described in the scientific literature by John McCorvy's lab and colleagues in 2025. The group also included Adam Halberstadt. The serotonin 5-HT2A and 5-HT2C receptors show considerable homology, which has made development of selective serotonin 5-HT2A receptor agonists difficult. TGF-8027 was discovered via a rational structure-guided design that took advantage of an identified single-residue difference between the serotonin 5-HT2A receptor and the serotonin 5-HT2C receptor in transmembrane 2 (TM2) of the extended binding pocket. The group also reported a series of other selective serotonin 5-HT2A receptor agonists in addition to TGF-8027, some of which showed even further improved selectivity. TGF-8027 was selected for more in-depth characterization over other compounds, for instance in the head-twitch response assay, because it showed among the highest selectivity and potency at the mouse serotonin 5-HT2A receptor in addition to the human serotonin 5-HT2A receptor.

Society and culture

Legal status

Canada TGF-8027 may be a controlled substance in Canada under phenethylamine blanket-ban language.

United States TGF-8027 is not an explicitly controlled substance in the United States. However, it could be considered a controlled substance under the Federal Analogue Act if intended for human consumption.

Illustrations

Worked examples

Example 1 — a first encounter with TGF-8027

Start with the simplest possible case. Write down what TGF-8027 claims or describes in one sentence, then invent the smallest concrete situation in which that sentence is true. In chemistry, the smallest case is usually a single object, a single equation or a single measurement. Check that every symbol or term in your sentence has a meaning in that case.

Example 2 — changing one variable

Take the situation from Example 1 and change exactly one quantity: double it, halve it, or set it to zero. Predict what should happen to TGF-8027 before you calculate. Comparing your prediction with the result is the fastest way to find out whether you understand the idea or only the words.

Example 3 — an exam-style question

Typical questions about TGF-8027 ask you to (a) state it precisely, (b) apply it to given data, and (c) explain a limitation. Practise writing all three answers in under five minutes; the third part is what separates a full-mark answer from an average one.

Applications of TGF-8027

In research: TGF-8027 appears in chemistry research whenever the underlying quantities have to be modelled precisely. Papers usually cite it as a starting assumption and then explore where it breaks down.
In technology and industry: Engineering practice reuses TGF-8027 in design rules, simulations and safety margins. Knowing the idea lets you read a specification sheet and understand why the numbers look the way they do.
In the classroom: TGF-8027 is common in secondary-school and first-year university syllabi. It links to neighbouring topics 2-Hydroxyphenyl compounds, 25-NB (psychedelics), 5-HT2A agonists, so understanding it makes those chapters shorter.
In everyday life: Look for TGF-8027 outside the textbook — in sport, cooking, traffic, electronics or the sky above you. An example you found yourself is remembered far longer than one you were given.

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How to study TGF-8027 in 20 minutes

Read the reference excerpt below once, without taking notes.
Close the page and write down what TGF-8027 means in your own words.
Compare your version with the excerpt and mark what you missed.
Work through the three examples above with pen and paper.
Explain TGF-8027 out loud to somebody else — or to Teacher Smith in the lgStudy chat.

Frequently asked questions

What is TGF-8027 in simple terms?

Why does TGF-8027 matter?

Because it connects several chemistry ideas at once: it gives you a definition you can apply, a quantity you can calculate, and a way to check whether a result is plausible.

How should I study TGF-8027?

Read the excerpt, restate it from memory, then work through the examples and applications listed on this page. The five-step study plan above takes about twenty minutes.

What does this page cover?

It gives you a compact reference excerpt plus original lgStudy explanations, examples, applications and study material on TGF-8027.