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AM 251 (AM251)

an analog of SR141716A; structure given in first source

Also Known As:

AM251; AM-251; N-(piperidin-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxamide; N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide

Networked: 126 relevant articles (6 outcomes, 13 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 60
- 1-Ring Heterocyclic Compounds
  - Azoles: 413
    - Pyrazoles: 26
      - AM 251: 126
  - Piperidines: 12
    - AM 251: 126

Experts

1.	Dehpour, Ahmad Reza: 5 articles (08/2013 - 09/2004)
2.	Shafaroodi, Hamed: 5 articles (08/2013 - 09/2004)
3.	Rivera, Patricia: 4 articles (01/2015 - 01/2011)
4.	Suárez, Juan: 4 articles (01/2015 - 01/2011)
5.	Serrano, Antonia: 4 articles (01/2015 - 01/2011)
6.	Ayyildiz, Mustafa: 4 articles (12/2014 - 07/2009)
7.	Agar, Erdal: 4 articles (12/2014 - 07/2009)
8.	Ghasemi, Mehdi: 4 articles (04/2009 - 11/2007)
9.	Sharkey, Keith A: 4 articles (01/2008 - 10/2004)
10.	Naderi, Nima: 3 articles (11/2015 - 11/2008)

Related Diseases

1.	Seizures (Seizure) 11/01/2007 - "However, regarding the seizure modulating properties of both classes of receptors this study investigated whether ultra-low dose cannabinoid antagonist AM251 influences cannabinoid anticonvulsant effects. " 11/01/2015 - "Pretreatment with different dosages of AM251 had contrary effects so that at lower doses they increased the seizure in animals but at higher doses led to the attenuation of seizure. " 08/15/2013 - "Injection of the selective cannabinoid CB₁ agonist ACEA (2 mg/kg) significantly (P<0.01) increased the seizure threshold which was prevented by pretreatment with the selective CB1 antagonist AM251 (1 mg/kg, i.p.). " 04/01/2009 - "Injection of the selective cannabinoid CB(1) agonist ACEA (2mg/kg, i.p.) significantly (P<0.01) increased the seizure threshold which was prevented (P<0.001) by pretreatment with the selective CB(1) antagonist AM251 (1mg/kg, i.p.). " 11/01/2007 - "A similar potentiation by AM251 (100 pg/kg and 1 ng/kg) of anticonvulsant effects of non-effective dose of ACEA (0.5 and 1 mg/kg) was also observed in the generalized tonic-clonic model of seizure. "
2.	Weight Gain 04/01/2015 - "The administration of AM 251 at 1, 2, or 5 mg/kg led to a significant reduction in food intake, along with a significant decrease in the digestive utilization of protein in the groups injected with 1 and 2 mg/kg. There was a dose-related slowdown in weight gain, especially at the doses of 2 and 5 mg/kg, during the initial days of the trial. " 04/01/2009 - "AM251 suppressed food intake and weight gain in fasted and non-fasted animals. " 10/15/2004 - "Reductions in food intake brought about by AM 251 were accompanied by reductions in weight gain for 6 days (P<.05). " 01/01/2009 - "Effects of acute low-dose combined treatment with naloxone and AM 251 on food intake, feeding behaviour and weight gain in rats." 11/01/2007 - "rimonabant, AM 251) on food intake and weight gain in rodents, surprisingly little is known about the behavioural selectivity of such effects. "
3.	Pain (Aches) 04/01/2012 - "administration of low doses of AM251 per se significantly decreased both pain related behavior and spinal IL1-β expression in formalin test. " 10/01/2010 - "WIN55,212-2 and AM251 did not affect IA conditioning, while AM404 enhanced it, probably due to a drug-induced increase in pain sensitivity. " 09/30/2008 - "Here we show that in thermal, mechanical and chemical pain tests, AM-251, a specific CB(1) receptor antagonist, abolished the analgesic action of acetaminophen, which was also lost in CB(1) receptor knockout mice. " 12/01/2014 - "Although many studies have documented the utility of CB1R agonists, this study indicates that endogenous cannabinoids may have an unexpected pronociceptive effect during development of burn pain, explaining why CB1R antagonist, AM251, improves nociceptive behaviors. " 12/01/2014 - "This study tested the hypothesis that burn injury activates glial cells, and cannabinoid receptor 1 (CB1R) antagonist, AM251, will decrease burn pain. "
4.	Status Epilepticus (Complex Partial Status Epilepticus) 02/01/2011 - "ACEA, at a dose of 7.5 μg, also decreased the frequency of epileptiform activity, whereas AM-251, at a dose of 0.25 μg increased the frequency by causing status epilepticus-like activity. " 07/01/2009 - "AM-251, at a dose of 0.25 μg (i.c.v.), was the most effective in changing the frequency of penicillin-induced epileptiform activity, and it also caused status epilepticus-like activity. " 12/01/2014 - "The administration of a 0.25 µg dose of AM-251 increased the frequency of penicillin-induced epileptiform activity by producing status epilepticus-like activity. " 04/01/2013 - "The administration of AM-251, at a dose of 0.25 μg, increased the frequency of penicillin-induced epileptiform activity by producing status epilepticus-like activity, whereas AM-251, at a dose of 0.125 μg, was not effective when applied alone. " 03/08/2007 - "In addition, the anti-status epilepticus effects of methanandamide and 2-AG were mediated by activation of the cannabinoid CB(1) receptor since they were blocked by the cannabinoid CB(1) receptor antagonist AM251. "
5.	Substance-Related Disorders (Drug Abuse) 01/01/2010 - "The reduction of ethanol intake induced by AM251 was associated with blockade or significant reduction of the changes produced by ethanol in the expression of these genes in key regions related to drug dependence. "

Related Drugs and Biologics

1.	rimonabant
2.	Cannabinoid Receptors (Cannabinoid Receptor)
3.	iodopravadoline (AM 630)
4.	Win 55212-2 (WIN 55,212)
5.	Penicillins (Penicillin)
6.	Ethanol (Ethyl Alcohol)
7.	CB1 Cannabinoid Receptor (CB1 Receptor)
8.	AM 251 (AM251)
9.	pyrazole
10.	Endocannabinoids (Endocannabinoid)

Related Therapies and Procedures

1.	Fat-Restricted Diet (Diet, Fat Restricted)
2.	Injections
3.	Intraperitoneal Injections
4.	Induced Hypothermia
5.	Analgesia