O-823(O-823) - 药物靶点：CB_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CB

作用机制

CB激动剂(大麻素受体激动剂)

治疗领域

免疫系统疾病

在研适应症-

非在研适应症

器官移植排斥

原研机构

Organix, Inc.

在研机构-

非在研机构

Organix, Inc.

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C23H27NO2

InChIKeyMZMMIGOIGWVGEH-RTBURBONSA-N

CAS号184433-64-5

关联

100 项与 O-823 相关的临床结果

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100 项与 O-823 相关的转化医学

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100 项与 O-823 相关的专利（医药）

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1

项与 O-823 相关的文献（医药）

1996-11-01·European Journal of Pharmacology

Agonist-antagonist characterization of 6′-cyanohex-2′-yne-Δ8-tetrahydrocannabinol in two isolated tissue preparations

Article

作者: Griffin, Graeme ; Ryan, William ; Razdan, Raj K. ; Pertwee, Roger G. ; Fernando, Susanthi R. ; Compton, David R. ; Martin, Billy R.

This investigation was directed at characterizing some of the pharmacological properties of 6'-cyanohex-2'-yne-delta 8-tetrahydrocannabinol (O-823), a compound with high affinity for cannabinoid binding sites (Ki = 0.77 nM). In mouse vasa deferentia, O-823 behaved as a potent partial cannabinoid CB1 receptor agonist (EC50 = 0.015 nM). In the guinea-pig myenteric plexus preparation, it antagonized WIN 55.212-2 [(R)-(+)-[2,3-dihydro-5-methyl-3-[(4-morpholino)methyl]pyrrolo-[1,2,3-de ]-1, 4-benzoxazin-6-yl](1-naphthyl)methanone] and CP 55.940 [(-)-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-4-(3-hydroxypropyl ) cyclohexan-1-ol] with Kd values of 0.65 and 0.27 nM, respectively. After in vivo delta 9-tetrahydrocannabinol pretreatment. the sensitivity of vasa deferentia to O-823-induced inhibition of electrically evoked contractions was reduced by 127-fold. 3.162 nM O-823 was inhibitory in unpretreated vasa deferentia but antagonized CP 55,940 in pretreated tissues (Kd = 0.26 nM). O-823 is probably an antagonist in the myenteric plexus preparation and delta 9-tetrahydro-cannabinol pretreated vasa deferentia but a partial agonist in unpretreated vasa deferentia because the first two of these preparations contain fewer receptors than the third.

100 项与 O-823 相关的药物交易

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