1438242-59-1
Chemical Structure
HTL-9936
- CAS No.: 1438242-59-1
- Formula:C20H35N3O3
- Molecular Weight:365.51
IUPAC Name: ethyl (S)-4-(4-((1-methylcyclobutyl)carbamoyl)piperidin-1-yl)azepane-1-carboxylate
InChIKey: AQEAWDQQWHVFAX-KRWDZBQOSA-N
SMILES: CC1(CCC1)NC(C2CCN([C@@H]3CCN(CCC3)C(OCC)=O)CC2)=O
Biological Activity: HTL-9936 is an orally active partial agonist of muscarinic M1 receptor. HTL-9936 has an EC50 of 32 nM for human M1 receptor and an EC50 of 224 nM for human M4 receptor. HTL-9936 activates Gq/11 coupling, promotes inositol phosphate accumulation, ERK1/2 phosphorylation, β-arrestin recruitment and receptor internalization. HTL-9936 can be used in the research of Alzheimer's disease and schizophrenia[1][2][3][4][5][6].
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HTL-9936 | HTL-9936 is an orally active partial agonist of muscarinic M1 receptor. HTL-9936 has an EC50 of 32 nM for human M1 receptor and an EC50 of 224 nM for human M4 receptor. HTL-9936 activates Gq/11 coupling, promotes inositol phosphate accumulation, ERK1/2 phosphorylation, β-arrestin recruitment and receptor internalization. HTL-9936 can be used in the research of Alzheimer's disease and schizophrenia. | |||||||||||||||||||||
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References
- [1]. Broad LM, et al. Identification and pharmacological profile of SPP1, a potent, functionally selective and brain penetrant agonist at muscarinic M receptors. British journal of pharmacology. 2019 Jan;176(1):110-126.
- [2]. Armer R, et al. Recent disclosures of clinical drug candidates. Drug News Perspect. 2006 Jan-Feb;19(1):65-72.
- [3]. Nguyen HTM, et al. Opportunities and challenges for the development of M muscarinic receptor positive allosteric modulators in the treatment for neurocognitive deficits. British journal of pharmacology. 2024 Jul;181(14):2114-2142. [Content Brief]
- [4]. Felder CC, et al. Current status of muscarinic M1 and M4 receptors as drug targets for neurodegenerative diseases. Neuropharmacology. 2018 Jul 01;136(Pt C):449-458. [Content Brief]
- [5]. Johnson CR, et al. Drug Design Targeting the Muscarinic Receptors and the Implications in Central Nervous System Disorders. Biomedicines. 2022 Feb 07;10(2):398. [Content Brief]
- [6]. Brown AJH, et al. From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease. Cell. 2021 Nov 24;184(24):5886-5901.e22. [Content Brief]
