Balipodect Explained
| Class: | Phosphodiesterase inhibitor
- PDE10A inhibitor; Antipsychotic
|
| Cas Number: | 1238697-26-1 |
| Pubchem: | 46848915 |
| Drugbank: | DB14774 |
| Chemspiderid: | 35035198 |
| Unii: | 6650W303H0 |
| Kegg: | D11245 |
| Chembl: | 3989972 |
| Synonyms: | TAK-063; TAK063 |
| Iupac Name: | 1-(2-fluoro-4-pyrazol-1-ylphenyl)-5-methoxy-3-(2-phenylpyrazol-3-yl)pyridazin-4-one |
| C: | 23 |
| H: | 17 |
| F: | 1 |
| N: | 6 |
| O: | 2 |
| Smiles: | COC1=CN(N=C(C1=O)C2=CC=NN2C3=CC=CC=C3)C4=C(C=C(C=C4)N5C=CC=N5)F |
| Stdinchi: | 1S/C23H17FN6O2/c1-32-21-15-29(19-9-8-17(14-18(19)24)28-13-5-11-25-28)27-22(23(21)31)20-10-12-26-30(20)16-6-3-2-4-7-16/h2-15H,1H3 |
| Stdinchikey: | KVHRYLNQDWXAGI-UHFFFAOYSA-N |
Balipodect (; developmental code name TAK-063) is a selective phosphodiesterase 10A (PDE10A) inhibitor which was under development by Takeda for the treatment of schizophrenia.[1] [2] [3]
It is active in animal models of antipsychotic-like activity, including inhibition of hyperlocomotion induced by the NMDA receptor antagonist dizocilpine (MK-801) or the dopamine releasing agent methamphetamine, inhibition of conditioned avoidance responses, and reversal of prepulse inhibition deficits.[4]
The drug reached phase 2 clinical trials for this indication but its development was discontinued. It was reported to be poorly effective or ineffective for schizophrenia in clinical trials.[5] [6] [7]
See also
Notes and References
- Web site: Balipodect . AdisInsight . 30 January 2018 . 19 October 2024.
- Web site: Delving into the Latest Updates on Balipodect with Synapse . Synapse . 19 September 2024 . 19 October 2024.
- Suzuki K, Kimura H . TAK-063, a novel PDE10A inhibitor with balanced activation of direct and indirect pathways, provides a unique opportunity for the treatment of schizophrenia . CNS Neuroscience & Therapeutics . 24 . 7 . 604–614 . July 2018 . 29318783 . 6489916 . 10.1111/cns.12798 .
- Menniti FS, Chappie TA, Schmidt CJ . PDE10A Inhibitors-Clinical Failure or Window Into Antipsychotic Drug Action? . Frontiers in Neuroscience . 14 . 600178 . 2020 . 33551724 . 7855852 . 10.3389/fnins.2020.600178 . free .
- Bondarev AD, Attwood MM, Jonsson J, Chubarev VN, Tarasov VV, Liu W, Schiöth HB . Recent developments of phosphodiesterase inhibitors: Clinical trials, emerging indications and novel molecules . Frontiers in Pharmacology . 13 . 1057083 . 2022 . 36506513 . 9731127 . 10.3389/fphar.2022.1057083 . free .
- Neef J, Palacios DS . Progress in mechanistically novel treatments for schizophrenia . RSC Medicinal Chemistry . 12 . 9 . 1459–1475 . September 2021 . 34671731 . 8459322 . 10.1039/d1md00096a .
- Krogmann A, Peters L, von Hardenberg L, Bödeker K, Nöhles VB, Correll CU . Keeping up with the therapeutic advances in schizophrenia: a review of novel and emerging pharmacological entities . CNS Spectrums . 24 . S1 . 38–69 . August 2019 . 31482779 . 10.1017/S109285291900124X . free .
