[11C]OMAR([11C]OMAR) - 药物靶点：CB1R_在研适应症：阿片相关性障碍_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CB1R

作用机制

CB1拮抗剂(大麻素受体CB1拮抗剂)

治疗领域

其他疾病

在研适应症

阿片相关性障碍

非在研适应症

酗酒大麻戒断大麻滥用+ [3]

原研机构

The Johns Hopkins University School of Medicine

在研机构

National Institute on Drug Abuse

非在研机构

The Johns Hopkins University School of Medicine

Yale University

最高研发阶段临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C23H21Cl2N5O2

InChIKeyMCNQUWLLXZZZAC-BJUDXGSMSA-N

CAS号942063-86-7

关联

5

项与 [11C]OMAR 相关的临床试验

NCT05683184 / Recruiting临床1期IIT

Characterization of CB1 Receptors Using [11-C]OMAR in Opioid Use Disorder

The goal of this research study is to examine the endocannabinoid (eCB) function in vivo in individuals with opioid use disorder (OUD) by measuring cannabinoid receptor 1 (CB1R) availability.

开始日期2023-03-10

申办/合作机构

Yale University

[+1]

NCT03539575 / Active, not recruitingN/AIIT

CB1R Availability in Synthetic Psychoactive Cannabinoid Users

The purpose of this research study is to determine whether the CB1R availability is lower in synthetic psychoactive cannabinoid subjects using the most widely available synthetic psychoactive cannabinoids at the time the study is initiated.

开始日期2018-05-01

申办/合作机构

Yale University

[+2]

NCT03204305 / Completed早期临床1期IIT

Brain Imaging of Cannabinoid Receptors in Women

All participants will be healthy volunteers and all procedures will be completed for research purposes only. Two groups will be recruited, females who use cannabis (marijuana, MJ), and female who do not use cannabis (controls). Female MJ users will be enrolled in a protocol that includes an outpatient drug administration session and a 4-day/3-night inpatient stay on the Johns Hopkins Bayview Clinical Research Unit (CRU). During outpatient visits, MJ users will have an MRI, and complete MJ self-administration and cognitive performance sessions. MJ users will then reside on the CRU,and complete MJ abstinence, and self-report instruments for withdrawal discomfort. A positron emission tomography (PET) scan of brain cannabinoid type 1 receptors will also be completed. Non-users will complete MRI, PET imaging and cognitive testing under an outpatient protocol (no MJ administration).

开始日期2017-09-14

申办/合作机构

The Johns Hopkins University

[+1]

100 项与 [11C]OMAR 相关的临床结果

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100 项与 [11C]OMAR 相关的转化医学

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100 项与 [11C]OMAR 相关的专利（医药）

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2

项与 [11C]OMAR 相关的文献（医药）

2011-11-01·Molecular Imaging

Positron Emission Tomographic Imaging of the Cannabinoid Type 1 Receptor System with [¹¹C]OMAR ([¹¹C]JHU75528): Improvements in Image Quantification Using Wild-Type and Knockout Mice

Article

作者: Martín-García, Elena ; Abad, Sergio ; Pareto, Deborah ; Jiménez, Xavier ; Gispert, Juan Domingo ; Burokas, Aurelijus ; Millán, Olga ; Serra, Miquel Àngel ; Herance, Raúl ; Rojas, Santiago ; Maldonado, Rafael

In this study, we assessed the feasibility of using positron emission tomography (PET) and the tracer [¹¹C]OMAR ([¹¹C]JHU75528), an analogue of rimonabant, to study the brain cannabinoid type 1 (CB1) receptor system. Wild-type (WT) and CB1 knockout (KO) animals were imaged at baseline and after pretreatment with blocking doses of rimonabant. Brain uptake in WT animals was higher (50%) than in KO animals in baseline conditions. After pretreatment with rimonabant, WT uptake lowered to the level of KO animals. The results of this study support the feasibility of using PET with the radiotracer [¹¹C]JHU75528 to image the brain CB1 receptor system in mice. In addition, this methodology can be used to assess the effect of new drugs in preclinical studies using genetically manipulated animals.

2006-10-01·Journal of nuclear medicine : official publication, Society of Nuclear Medicine

11C-JHU75528: a radiotracer for PET imaging of CB1 cannabinoid receptors.

Article

作者: Fan, Hong ; Kuwabara, Hiroto ; Rahmim, Arman ; Horti, Andrew G ; Kumar, Anil ; Ravert, Hayden T ; Wong, Dean F ; Dannals, Robert F ; Scheffel, Ursula ; Hilton, John ; Alexander, Mohab ; Holt, Daniel P

The development of the radioligands for PET imaging of the cerebral cannabinoid receptor (CB1) is of great importance for studying its role in neuropsychiatric disorders, obesity, and drug dependence. None of the currently available radioligands for CB1 are suitable for quantitative PET, primarily because of their insufficient binding potential (BP) in brain or low penetration through the blood-brain barrier (BBB). The goal of this study was to evaluate 11C-JHU75528, an analog of the selective CB1 antagonist rimonabant, in vivo as a potential CB1 radioligand for PET.METHODSThe brain regional distribution and pharmacology of 11C-JHU75528 have been evaluated in vivo in mice (dissection) and baboons (PET).RESULTS11C-JHU75528 readily entered the mouse and baboon brain and specifically and selectively labeled cerebral CB1 receptors. The ratio of striatum to brain stem in mice and the binding potential (BP) in the baboon putamen were 3.4 and 1.3-1.5, respectively. The specific binding of 11C-JHU75528 in vivo was blocked by preinjection of nonlabeled JHU75528. Administration of rimonabant (1 mg/kg, intravenously) also blocked the specific binding of 11C-JHU75528 in the mouse and baboon brain, whereas various central noncannabinoid drugs did not significantly reduce the 11C-JHU75528 binding in the mouse brain. 11C-JHU75528 formed several hydrophilic metabolites, but only a minute fraction of metabolic radioactivity penetrated the BBB.CONCLUSION11C-JHU75528 holds promise as a radiotracer with suitable imaging properties for quantification of CB1 receptors in the human brain.

100 项与 [11C]OMAR 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14902

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
阿片相关性障碍	临床1期	美国	National Institute on Drug Abuse	2023-03-10
大麻戒断	药物发现	美国	National Institute on Drug Abuse	2017-09-14
大麻滥用	药物发现	美国	National Institute on Drug Abuse	2017-09-14
酗酒	药物发现	美国	Yale University	2009-06-01
肥胖	药物发现	美国	Yale University	2009-06-01
心理压力	药物发现	美国	Yale University	2009-06-01
精神分裂症	药物发现	-	The Johns Hopkins University School of Medicine	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


SNMMI2017	N/A	肥胖	-	11 C-OMAR (Obese mice)	觸願鬱憲膚醖築膚鹽鹽(夢壓簾襯遞餘憲糧衊齋) = 醖範築顧願繭鏇醖壓顧淵膚憲鏇憲鏇範繭簾夢 (繭顧膚憲衊鏇窪鏇願廠, 68.1 ~ 75.9) 更多	-	2017-05-24
				11 C-OMAR (Normal weight mice)	觸願鬱憲膚醖築膚鹽鹽(夢壓簾襯遞餘憲糧衊齋) = 獵構簾願顧齋鏇遞築網淵膚憲鏇憲鏇範繭簾夢 (繭顧膚憲衊鏇窪鏇願廠, 50.5 ~ 57.8) 更多