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TC OT 39

Names

[ CAS No. ]:
479232-57-0

[ Name ]:
TC OT 39

[Synonym ]:
(2S)-2-[(4-Methyl-1,4-diazepan-1-yl)carbonothioyl]-N-{2-methyl-4-[(1-methyl-4,10-dihydropyrazolo[3,4-b][1,5]benzodiazepin-5(1H)-yl)carbonyl]benzyl}-1-pyrrolidinecarboxamide
(2S)-2-[(4-methyl-1,4-diazepan-1-yl)carbothioyl]-N-{2-methyl-4-[(1-methyl-4,10-dihydropyrazolo[3,4-b][1,5]benzodiazepin-5(1H)-yl)carbonyl]benzyl}pyrrolidine-1-carboxamide
1-Pyrrolidinecarboxamide, N-[[4-[(4,10-dihydro-1-methylpyrazolo[3,4-b][1,5]benzodiazepin-5(1H)-yl)carbonyl]-2-methylphenyl]methyl]-2-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)thioxomethyl]-, (2S)-
MFCD28133368
TC OT 39

Biological Activity

[Description]:

TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Vasopressin Receptor
Signaling Pathways >> GPCR/G Protein >> Oxytocin Receptor
Research Areas >> Neurological Disease

[Target]

Avprla vasopressin receptor:300 nM (Ki)

Oxytocin Receptor:180 nM (EC50)


[In Vivo]

TC OT 39 (50 mg/kg、75 mg/kg；腹腔注射；在 8-9 天内注射 4 次)，在 50 mg/kg 的剂量下，显著减少 C57BL/6J 小鼠的大理石掩埋行为，并在 75 mg/kg 的剂量下显示出明显的镇静作用[1]。 大理石掩埋是基于啮齿动物掩埋物体的自然本能，常用于临床前研究以评估啮齿动物的焦虑样行为[1]。

[References]

[1]. Moy SS, et al. Prosocial effects of an oxytocin metabolite, but not synthetic oxytocin receptor agonists, in a mouse model of autism. Neuropharmacology. 2019 Jan;144:301-311.  

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C32H40N8O2S

[ Molecular Weight ]:
600.777

[ Exact Mass ]:
600.299500

[ LogP ]:
2.00

[ Index of Refraction ]:
1.702

Related Compounds