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chemistry

SB-221284

SB-221284 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 SB-221284 rather than just read about it. In short: SB-221284 is a selective serotonin 5-HT2C and 5-HT2B receptor antagonist which is used in scientific research. Its affinities (Ki) are 2.2 to 2.5 nM for the serotonin 5-HT2C receptor, 2.5 to 12.6 nM for the serotonin 5-HT2B receptor, and 398 to 550 nM for the serotonin 5-HT2A receptor (where it is also an antagonist).

SB-221284 — main illustration
SB-221284 — illustration

Key takeaways

  • SB-221284 belongs to chemistry; place it in that map before memorising details.
  • Learn the definition first, then one example that makes the definition concrete.
  • Connect SB-221284 to a quantity you can measure, compute or draw — that is where exam questions come from.
  • Reproduce the core statement of SB-221284 from memory before moving on to harder problems.

Reference excerpt

SB-221284 is a selective serotonin 5-HT2C and 5-HT2B receptor antagonist which is used in scientific research. Its affinities (Ki) are 2.2 to 2.5 nM for the serotonin 5-HT2C receptor, 2.5 to 12.6 nM for the serotonin 5-HT2B receptor, and 398 to 550 nM for the serotonin 5-HT2A receptor (where it is also an antagonist). The drug has 160- to 250-fold selectivity for the serotonin 5-HT2C receptor over the serotonin 5-HT2A receptor. It is said to have been the first serotonin 5-HT2C receptor ligand to show 100-fold selectivity over the serotonin 5-HT2A receptor. SB-221284 has shown anxiolytic-like effects in animals. Conversely, it has been said to be inactive in terms of antidepressant-like, antiobsessional-like, antipanic-like, and sedative effects. It also showed no proconvulsant or hyperphagic effects in animals, phenotypes that are notably observed with serotonin 5-HT2C receptor knockout. The preferential serotonin 5-HT2C receptor agonist meta-chlorophenylpiperazine (mCPP) and the serotonin reuptake inhibitor fluoxetine have been found to acutely reduce social interaction in rodents. SB-221284 was found to reverse the acute decreases in social interaction produced by mCPP and fluoxetine. The drug has also been found to block mCPP-induced hypolocomotion. Both SB-221284 and the selective serotonin 5-HT2C receptor antagonist SB-242084 have been found to enhance the nucleus accumbens dopamine release and hyperlocomotion induced by NMDA receptor antagonists like phencyclidine (PCP) and dizocilpine (MK-801). Conversely, both drugs had no effect on locomotor activity or dopamine release in the nucleus accumbens by themselves. However, another study reported that SB-221284 by itself did enhance locomotion. SB-221284 was first described in the scientific literature by 1996. It was researched by GlaxoSmithKline as a possible non-sedating anxiolytic and reached the preclinical research stage of development. However, it was found to be a potent inhibitor of a number of human cytochrome P450 enzymes (particularly CYP1A2), which precluded further development of the drug. Other sources have stated that SB-221284 was not further developed due to "toxicity" and that other drugs were pursued instead as SB-221284 was a "fairly weak" serotonin 5-HT2C receptor antagonist.

References

Illustrations

SB-221284 illustration

Worked examples

Example 1 — a first encounter with SB-221284

Start with the simplest possible case. Write down what SB-221284 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 SB-221284 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 SB-221284 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 SB-221284

In research
SB-221284 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 SB-221284 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
SB-221284 is common in secondary-school and first-year university syllabi. It links to neighbouring topics 3-Pyridyl compounds, 5-HT2B antagonists, 5-HT2C antagonists, so understanding it makes those chapters shorter.
In everyday life
Look for SB-221284 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 SB-221284 in 20 minutes

  1. Read the reference excerpt below once, without taking notes.
  2. Close the page and write down what SB-221284 means in your own words.
  3. Compare your version with the excerpt and mark what you missed.
  4. Work through the three examples above with pen and paper.
  5. Explain SB-221284 out loud to somebody else — or to Teacher Smith in the lgStudy chat.

Frequently asked questions

What is SB-221284 in simple terms?

SB-221284 is a selective serotonin 5-HT2C and 5-HT2B receptor antagonist which is used in scientific research. Its affinities (Ki) are 2.2 to 2.5 nM for the serotonin 5-HT2C receptor, 2.5 to 12.6 nM for the serotonin 5-HT2B receptor, and 398 to 550 nM for the serotonin 5-HT2A receptor (where it is…

Why does SB-221284 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 SB-221284?

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 SB-221284.

Tags

  • 3-Pyridyl compounds
  • 5-HT2B antagonists
  • 5-HT2C antagonists
  • Abandoned drugs
  • Carboxamides
  • Indolines
  • Methylthio compounds
  • Trifluoromethyl compounds
  • Ureas

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