PF-3274167
PF-3274167 Basic information
- Product Name:
- PF-3274167
- Synonyms:
-
- PF-3274167
- PF-03274167
- 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)-1,2,4-triazol-4-yl]-2-methoxypyridine
- Cligosiban
- PF 3274167;PF3274167
- PF-3274167(cligosiban)
- 5-(3-(3-(2-Chloro-4-fluorophenoxy)azetidin-1-yl)-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl)-2-methoxypyridine
- CAS:
- 900510-03-4
- MF:
- C19H19ClFN5O3
- MW:
- 419.84
- Mol File:
- 900510-03-4.mol
PF-3274167 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO: 18 mg/mL
- form
- A crystalline solid
- color
- Off-white to pink
PF-3274167 Usage And Synthesis
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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