chemistry

Roluperidone

Roluperidone 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 Roluperidone rather than just read about it. In short: Roluperidone (former developmental code names MIN-101, CYR-101, MT-210) is a 5-HT2A and σ2 receptor antagonist under development by Minerva Neurosciences for the treatment of schizophrenia. One of its metabolites also has some affinity for the H1 receptor.

Key takeaways

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

Reference excerpt

Roluperidone (former developmental code names MIN-101, CYR-101, MT-210) is a 5-HT2A and σ2 receptor antagonist under development by Minerva Neurosciences for the treatment of schizophrenia. One of its metabolites also has some affinity for the H1 receptor. Pre-clinical findings provide evidence of the effect of roluperidone on brain-derived neurotrophic factor ("BDNF"), which has been associated with neurogenesis, neuroplasticity, neuroprotection, synapse regulation, learning and memory. As of May 2018, the drug was in phase III clinical trials. In May 2020, the shares of Minerva Neurosciences plummeted 67% after the trial "failed to meet its primary endpoint of reduction in negative symptoms, and key secondary endpoints of improvement in personal and social performance measurements." However, in August 2022 Minerva submitted a New Drug Application (NDA) to the Food and Drug Administration (FDA) for the approval of roluperidone for the treatment of schizophrenia. The NDA submission in 2022 followed successful completion of a phase III clinical trial which was published in early 2022. Minerva believed that the findings of this second trial supported the claim that the drug was an effective agent for the treatment of negative symptoms in schizophrenia. However, in October 2022, FDA sent Minerva a refusal to file letter pertaining to the New Drug Application for roluperidone for treating negative symptoms in schizophrenia patients.

Chemistry

Synthesis

The Boc protection of 4-aminomethylpiperidine [7144-05-0] (1) gives tert-Butyl 4-aminomethylpiperidine-1-carboxylate hydrochloride [359629-16-6] (2). The free-radical halogenation of ethyl o-toluate [87-24-1] (3) led to ethyl 2-(bromomethyl)benzoate [7115-91-5] (4). The reaction between the two intermediates led to 2-[(1-tert-Butoxycarbonylpiperidin-4-yl)methyl]isoindolin-1-one [359629-19-9] (5). Deprotection yielded 2-(Piperidin-4-ylmethyl)-3H-isoindol-1-one;hydrochloride (6). Alkylation of the secondary nitrogen with 2-chloro-4'-fluoroacetophenone [700-35-6] (7) completed the synthesis of Roluperidone (8).

See also Serotonin 5-HT2A receptor antagonist List of investigational antipsychotics Risperidone Paliperidone Iloperidone Glemanserin Pruvanserin Volinanserin Lenperone Lidanserin MIN-117 MIN-202

References

Illustrations

Worked examples

Example 1 — a first encounter with Roluperidone

Start with the simplest possible case. Write down what Roluperidone 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 Roluperidone 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 Roluperidone 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 Roluperidone

In research: Roluperidone 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 Roluperidone 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: Roluperidone is common in secondary-school and first-year university syllabi. It links to neighbouring topics 4-Fluorophenyl compounds, 5-HT2A antagonists, Antipsychotics, so understanding it makes those chapters shorter.
In everyday life: Look for Roluperidone 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 Roluperidone in 20 minutes

Read the reference excerpt below once, without taking notes.
Close the page and write down what Roluperidone 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 Roluperidone out loud to somebody else — or to Teacher Smith in the lgStudy chat.

Frequently asked questions

What is Roluperidone in simple terms?

Why does Roluperidone 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 Roluperidone?

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 Roluperidone.