1520893-08-6
Chemical Structure
TASP0434299
- CAS No.: 1520893-08-6
- Formula:C27H35N5O5
- Molecular Weight:509.61
IUPAC Name: N-(tert-butyl)-2-(2-(3-methoxyphenyl)-6-(3-morpholinopropoxy)-4-oxopyrido[2,3-d]pyrimidin-3(4H)-yl)acetamide
InChIKey: XVASOLQWDBYKQE-UHFFFAOYSA-N
SMILES: O=C1C2=CC(OCCCN3CCOCC3)=CN=C2N=C(C=4C=CC=C(OC)C4)N1CC(=O)NC(C)(C)C
Biological Activity: TASP0434299 (Compound 10) is a labeled ligand for the vasopressin V1b receptor. TASP0434299 exhibits high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and shows potent antagonistic activity against the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 is a substrate for human and rhesus monkey P-glycoprotein, resulting in low brain uptake in rhesus monkeys. TASP0434299 binds to V1B receptors in rat and monkey pituitary tissues in a saturable and specific manner both in vitro and in vivo. When radiolabeled with tritium or 11C, TASP0434299 serves as a prototype V1B receptor radiotracer to visualize V1B receptor in the pituitary gland of anesthetized monkeys via positron emission tomography[1][2][3].
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TASP0434299 | TASP0434299 (Compound 10) is a labeled ligand for the vasopressin V1b receptor. TASP0434299 exhibits high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and shows potent antagonistic activity against the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 is a substrate for human and rhesus monkey P-glycoprotein, resulting in low brain uptake in rhesus monkeys. TASP0434299 binds to V1B receptors in rat and monkey pituitary tissues in a saturable and specific manner both in vitro and in vivo. When radiolabeled with tritium or 11C, TASP0434299 serves as a prototype V1B receptor radiotracer to visualize V1B receptor in the pituitary gland of anesthetized monkeys via positron emission tomography. | |||||||||||||||||||||
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- [1]. Kazumi Koga, et al. Radioactively labeled ligand of v1b receptor. JP2015120644A. 2018-08-22
- [2]. Koga K, et al. TASP0434299: A Novel Pyridopyrimidin-4-One Derivative as a Radioligand for Vasopressin V1B Receptor. J Pharmacol Exp Ther. 2016;357(3):495-508. [Content Brief]
- [3]. Koga K, et al. High-Contrast PET Imaging of Vasopressin V1B Receptors with a Novel Radioligand, 11C-TASP699. J Nucl Med. 2017;58(10):1652-1658. [Content Brief]
Keywords
