91833-49-7

91833-49-7 structure

Name: Rocastine
Chemical Name: 2-[2-(dimethylamino)ethyl]-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepine-5(4H)-thione
CAS Number: 91833-49-7
Molecular Formula: C₁₃H₁₉N₃OS
Molecular Weight: 265.37400
Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
Create Date: 2018-03-13 20:39:26
Modify Date: 2024-01-18 14:21:08
Rocastine is a selective, nonsedating H1 antagonist, acting as an antihistamine.

Name	2-[2-(dimethylamino)ethyl]-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepine-5(4H)-thione
Synonyms	rocastine 2-[2-(dimethylamino)ethyl]-3,4-dihydro-4-methylpyrido[3,2-f]-1,4-oxazepine-5(2H)-thione 8-(2-Dimethylamino-ethyl)-6-methyl-7,8-dihydro-6H-9-oxa-1,6-diaza-benzocycloheptene-5-thione AHR 11325 2-(dimethylamino)ethyl-2,3-dihydro-4-methylpyrido-[3,2-f]-1,4-oxazepine-5(4 H)-thione

Description	Rocastine is a selective, nonsedating H1 antagonist, acting as an antihistamine.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Histamine Receptor Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Others
In Vivo	Rocastine is effective with a 15 min pretreatment time (PD50 = 0.13 mg/kg) as it is with a 1 hr pretreatment time (PD50 = 0.12 mg/kg). Rocastine protects guinea pigs from collapse induced by aerosolized antigen; rocastine is approximately 36x more potent than diphenhydramine and as potent as oxatomide and terfenadine. Rocastine does not alter the EEG of cats at doses in vast excess (150x) of its antihistaminic dose nor does it potentiate yohimbine toxicity in mice[1].
References	[1]. Nolan JC, et al. Rocastine (AHR-11325), a rapid acting, nonsedating antihistamine. Agents Actions. 1989 Aug;28(1-2):53-61.