| Identification | Back Directory | [Name]
1H-1,2,4-Triazole, 5-[4-(1,1-dimethylethyl)phenyl]-1-methyl-3-(1-pyrrolidinylmethyl)-, hydrochloride (1:1) | [CAS]
2573850-59-4 | [Synonyms]
1H-1,2,4-Triazole, 5-[4-(1,1-dimethylethyl)phenyl]-1-methyl-3-(1-pyrrolidinylmethyl)-, hydrochloride (1:1) | [Molecular Formula]
C18H26N4.ClH | [MOL File]
2573850-59-4.mol | [Molecular Weight]
334.89 |
| Hazard Information | Back Directory | [Uses]
PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN)[1]. | [in vivo]
PW507 (20 mg/kg; i.p; twice daily; for 14 days) demonstrates significant efficacy in alleviating mechanical allodynia hyperalgesia[1].
PW507’s Pharmacokinetic Properties in SD rats Studies[1].
1.19 | plasma PK | IV | PO | IP | | dose (mg/kg) | 1 | 25 | 10 | | tmax (h) | N/A | 1.20 | 0.25 | | t1/2 (h) | 0.53 | 0.69 | 0.56 | | Cmax (ng/mL) | 193 | 296 | 671 | | AUC0-inf (h*ng/mL) | 108 | 692 | 552 | | CL (mL/min/kg) | 155 | N/A | N/A | | ratio (brain/plasma, t = 0.25 h) | N/A | N/A | 12 | | F (%) | 100 | 28 | 51 |
| Animal Model: | Male SD rats injected Streptozotocin (HY-13753; STZ; 60 mg/kg)[1] | | Dosage: | 20 mg/kg | | Administration: | i.p; twice daily; for 14 days | | Result: | Demonstrated significant efficacy in alleviating mechanical allodynia hyperalgesia.
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| [References]
[1] Youyi Peng, et al. Preclinical Evaluation of Sigma 1 Receptor Antagonists as a Novel Treatment for Painful Diabetic Neuropathy. ACS Pharmacol. Transl. Sci. July 18, 2024. |
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