1829530-11-1
Chemical Structure
Alofropodect
Synonym(s): CPL500036
- CAS No.: 1829530-11-1
- Formula:C19H15N7
- Molecular Weight:341.37
InChIKey: VODQJEUBIZNJSP-UHFFFAOYSA-N
SMILES: CC1=NC=C(C)N2N=C(C3=NC4=NC(C5=CC=CC=C5)=CN4C=C3)N=C21
Biological Activity: Alofropodect is an orally active, blood-brain barrier permeable phosphodiesterase 10A (PDE10A) inhibitor with IC50 values of 1 nM (Reference 1) and 35 nM (Reference 2). Alofropodect acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC50 of 9.2 μM. Alofropodect alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. Alofropodect induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. Alofropodect can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Alofropodect | Alofropodect is an orally active, blood-brain barrier permeable phosphodiesterase 10A (PDE10A) inhibitor with IC50 values of 1 nM (Reference 1) and 35 nM (Reference 2). Alofropodect acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC50 of 9.2 μM. Alofropodect alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. Alofropodect induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. Alofropodect can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Matloka M, et al. A PDE10A inhibitor CPL500036 is a novel agent modulating striatal function devoid of most neuroleptic side-effects. Front Pharmacol. 2022;13:999685. Published 2022 Nov 9. [Content Brief]
- [2]. Lenda T, et al. Antiparkinsonian-like effects of CPL500036, a novel selective inhibitor of phosphodiesterase 10A, in the unilateral rat model of Parkinson's disease. Eur J Pharmacol. 2021;910:174460. [Content Brief]
