iodopravadoline (AM 630)

an aminoalkylindole; a competitive cannabinoid receptor antagonist; structure given in first source

Also Known As:

AM 630; AM630; 1-(2-(morpholin-4-yl)ethyl)-2-methyl-3-(4-methoxybenzoyl)-6-iodoindole; 2-methyl-3-(4-methoxybenzoyl)-6-iodo-1-(2-morpholinoethyl)-1H-indole; 6-iodopravadoline; AM-630; methanone, (6-iodo-2-methyl-1-(2-(4-morpholinyl)ethyl)-1H-indol-3-yl)(4-methoxyphenyl)-

Networked: 93 relevant articles (6 outcomes, 3 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Indoles: 200
      - iodopravadoline: 93

Experts

1.	Lehmann, Christian: 4 articles (01/2021 - 12/2012)
2.	Zhou, Juan: 3 articles (01/2021 - 12/2012)
3.	Hohmann, Andrea G: 3 articles (07/2015 - 09/2010)
4.	Cao, Qingjun: 2 articles (08/2021 - 12/2018)
5.	Wang, Hua: 2 articles (08/2021 - 12/2018)
6.	Yang, Fenghua: 2 articles (08/2021 - 12/2018)
7.	Burkovskiy, Ian: 2 articles (01/2021 - 01/2016)
8.	Piomelli, Daniele: 2 articles (01/2021 - 05/2010)
9.	Wang, Guonian: 2 articles (01/2021 - 04/2016)
10.	Zhang, Mingyue: 2 articles (01/2021 - 04/2016)

Related Diseases

1.	Pain (Aches) 03/01/2007 - "Pretreatment with the CB(1) receptor subtype-selective antagonist AM 251 completely abolished the antinociceptive effect of WIN 55,212-2 whereas pretreatment with the CB(2) receptor subtype-selective antagonist AM 630 did not alter the antinociceptive effect of WIN 55,212-2. These data indicate that a CB(1)-selective agonist may be novel therapeutic treatment for clinical SCI pain." 12/01/2017 - "The CB2 receptor inverse agonist, AM630, reduced the pain relief of bufalin treatment in the mouse bone cancer model. " 09/01/2019 - "Additionally, AM251 and AM630 (CB1 and CB2 receptor antagonist, respectively, 1 mg/kg, i.p.) were used to evaluate the possible involvement of CB1 and CB2 receptors during the protective effects of WIN 55,212-2. We found that NTG (10 mg/kg, i.p.) in both acute and chronic models increased sensitivity to pain. " 01/01/2018 - "Our results indicated that the classical cannabinoid agonist WIN 55,212-2 produced supraspinal analgesia in preclinical pain models, which was selectively antagonized by the CB1 antagonist/inverse agonist AM251, but not by the CB2 antagonist AM630. " 12/01/2015 - "The influence of 5-HT1B/1D serotonin receptor (GR 127935) and CB1 (AM251) and CB2 cannabinoid receptor (AM630) antagonists on the antinociceptive effect of ESL was tested in the model of trigeminal pain. "
2.	Infarction (Infarctions) 01/01/2013 - "Pretreatment with AM630 but not AM251 abolished the infarct size-limiting effect of AEA. " 05/01/2006 - "On the contrary, the specific CB2 receptor antagonist AM-630 (0.3 microM) did not alter infarct size (31.6 +/- 6.3%, P > 0.05 vs. PC alone). " 05/01/2011 - "Cerebral ischemic injury was evaluated by neurobehavioral scores and infarction volume percentages 72 h after reperfusion in the presence or absence of AM251, a selective CB1 receptor antagonist, and AM630, a selective CB2 receptor antagonist. " 03/01/2014 - "Administration of CB2 receptor agonist JWH133 before ischemia significantly improved the recovery of cardiac ventricular function during reperfusion, increased coronary flow, reduced infarct size, prevented the loss of ΔΨ(m) and MPTP opening, reduced the release of cytochrome c from mitochondria, and increased levels of p-ERK1/2. These effects of JWH133 were abolished by pretreatment with CB2 receptor antagonist AM630, or ERK1/2 inhibitor PD98059. "
3.	Ischemia 03/01/2014 - "Administration of CB2 receptor agonist JWH133 before ischemia significantly improved the recovery of cardiac ventricular function during reperfusion, increased coronary flow, reduced infarct size, prevented the loss of ΔΨ(m) and MPTP opening, reduced the release of cytochrome c from mitochondria, and increased levels of p-ERK1/2. These effects of JWH133 were abolished by pretreatment with CB2 receptor antagonist AM630, or ERK1/2 inhibitor PD98059. " 01/01/2017 - "We observed that chick retinal treatment with a combination of WIN 55212-2 and cannabinoid receptor antagonists (either AM251/O-2050 or AM630) decreased the release of lactate dehydrogenase (LDH) induced by retinal ischemia in an oxygen and glucose deprivation (OGD) model. "
4.	Brain Injuries (Brain Injury) 01/01/2021 - "Late CB2R inhibition with AM630 also improved the peripheral leukocyte response to endotoxin and did not exacerbate the extent of brain injury. " 09/01/2011 - "To test this hypothesis, the effects of estradiol, the cannabinoid CB1 antagonist/inverse agonist AM251, and the cannabinoid CB2 antagonist/inverse agonist AM630 were assessed in the cerebral cortex of male rats after a stab wound brain injury. "
5.	Hyperlipidemias (Hyperlipidemia) 01/01/2021 - "Interestingly, treatment with AM630, a CB2R antagonist was observed to abrogate the protective effects of BCP on the biochemical and molecular parameters except hyperlipidemia and ionic homeostasis in ISO-induced MI in rats. "

Related Drugs and Biologics

1.	AM 251 (AM251)
2.	CB2 Cannabinoid Receptor
3.	1,1-dimethylbutyl-1-deoxy-Delta(9)-THC
4.	(3R)- ((2,3- dihydro- 5- methyl- 3- ((4- morpholinyl)methyl)pyrrolo- (1,2,3- de)- 1,4- benzoxazin- 6- yl)(1- naphthalenyl))methanone (WIN 55,212)
5.	Inflammasomes
6.	1- Methyl- 4- phenyl- 1,2,3,6- tetrahydropyridine (MPTP)
7.	Microtubule-Associated Proteins (Microtubule-Associated Protein 2)
8.	Endotoxins
9.	Autophagy-Related Proteins
10.	2- (2- amino- 3- methoxyphenyl)- 4H- 1- benzopyran- 4- one

Related Therapies and Procedures

1.	Ligation
2.	Intraperitoneal Injections
3.	Analgesia
4.	Spinal Injections
5.	Anesthesia