| Identification | Back Directory | [Name]
PF-3274167 | [CAS]
900510-03-4 | [Synonyms]
CS-1465
PF-3274167
Cligosiban
PF-03274167
PF 3274167;PF3274167
PF-3274167(cligosiban)
PF3274167; PF 3274167; PF-03274167; PF 03274167
5-[3-[3-(2-chloro-4-fluorophenoxy)azetidin-1-yl]-5-(methoxymethyl)-1,2,4-triazol-4-yl]-2-methoxypyridine
5-[3-[3-(2-Chloro-4-fluorophenoxy)-1-azetidinyl]-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl]-2-methoxypyridine
5-(3-(3-(2-Chloro-4-fluorophenoxy)azetidin-1-yl)-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl)-2-methoxypyridine
Pyridine, 5-[3-[3-(2-chloro-4-fluorophenoxy)-1-azetidinyl]-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl]-2-methoxy- | [Molecular Formula]
C19H19ClFN5O3 | [MDL Number]
MFCD25976681 | [MOL File]
900510-03-4.mol | [Molecular Weight]
419.84 |
| Hazard Information | Back Directory | [Description]
PF-3274167 is an oxytocin receptor antagonist (Ki = 9.5 nM). It is selective for the oxytocin receptor over the vasopressin receptors V1A and V2 (Kis = 1,120 and 10,000 nM, respectively). | [Uses]
PF-3274167 functions as s triazole oxytocin antagonists. It also functions as a PET radiotracer of oxytocin receptors. | [in vivo]
Cligosiban (0.9 mg/kg; 3 to 5 minutes after injection of Apomorphine (HY-12723); i.v.) shows CNS permeability and inhibits Apomorphine-induced ejaculation in an anesthetized rat CNS neuronal discharge model by modulating oxytocin (OT)-mediated responses in the nucleus tractus solitarius (NTS)[1].
Cligosiban (1 mg/kg; i.v. or p.o.) produces 4 metabolites in rat plasma, with demethylation and glucuronidation being the major metabolic pathways, and the pharmacokinetic profile is favorable[2]. | Animal Model: | Male Sprague Dawley rats (280-350 g), Anesthetized Rat CNS Neuronal Firing Model (Pre injection of Apomorphine (200 mg/kg, intravenous injection) into rats to regulate neuronal firing)[1]. | | Dosage: | 0.9 mg/kg | | Administration: | Intravenous injection (i.v.); 3 to 5 minutes after injection of Apomorphine | | Result: | Reversed the reduced firing of nucleus tractus solitaries (NTS) neurons induced by Apomorphine and reduced the bulbospongiosum burst pattern and contraction amplitude associated with ejaculation. |
| Animal Model: | Male Sprague-Dawley rats with body weight of 200-220?g[2]. | | Dosage: | 1 mg/kg | | Administration: | Intravenous injection (i.v.) or oral gavage (p.o.) | | Result: | Was rapidly absorbed into the plasma after oral administration and reached its maximum blood concentration 1.41 hours after administration, and was quickly eliminated from the plasma after absorption. |
| [References]
[1] ALAN BROWN. Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent[J]. Bioorganic & Medicinal Chemistry Letters, 2010, 20 2: Pages 516-520. DOI: 10.1016/j.bmcl.2009.11.097 |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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