2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Direclidine

Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders.

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Direclidine

Direclidine Chemical Structure

CAS No. : 1803346-98-6

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Based on 1 publication(s) in Google Scholar

Direclidine Related Antibodies

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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Description

Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders[1].

IC50 & Target[1]

mAChR4

 

In Vitro

Direclidine (i.e., NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor. It has no specified IC50/EC50/Ki values, is orally effective, and there is no clear literature mentioning whether it crosses the blood-brain barrier. It has extremely low affinity for M1, M2, M3, and M5 receptors and binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Its mechanism of action involves specifically activating the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Detailed in vitro/in vivo data on the key active ingredient have not yet been publicly disclosed (only the completion of Phase I clinical trials has been mentioned, but the results have not been published). Its core function is to improve symptoms associated with neuropsychiatric disorders, and its main research area is the treatment of schizophrenia and other neuropsychiatric disorders. It has no natural source and is an artificially designed and synthesized small molecule compound[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Direclidine Related Antibodies
Clinical Trial
Molecular Weight

346.47

Formula

C19H30N4O2
CAS No.
SMILES

CCOC(N1C[C@@]2(CC1)C[C@@H](N3CCC(C4=CC=NN4C)CC3)C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Direclidine Related Classifications

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Direclidine1803346-98-6NBI-1117568 HTL-0016878NBI1117568NBI 1117568HTL0016878HTL 0016878HTL-0016878mAChRMuscarinic acetylcholine receptormuscarinic M4 receptorpositive allosteric modulatorInhibitorinhibitorinhibit

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