Page last updated: 2024-10-22

am 251 and Inflammation

am 251 has been researched along with Inflammation in 20 studies

AM 251: an analog of SR141716A; structure given in first source
AM-251 : A carbohydrazide obtained by formal condensation of the carboxy group of 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid with the amino group of 1-aminopiperidine. An antagonist at the CB1 cannabinoid receptor.

Inflammation: A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.

Research Excerpts

ExcerptRelevanceReference
"Spinal glial activation has been implicated in sustained morphine-mediated paradoxical pain sensitization."7.78Repeated morphine treatment-mediated hyperalgesia, allodynia and spinal glial activation are blocked by co-administration of a selective cannabinoid receptor type-2 agonist. ( Keresztes, A; Largent-Milnes, TM; Ren, J; Roeske, WR; Tumati, S; Vanderah, TW; Varga, EV, 2012)
"The pharmacological inhibition of anandamide (AEA) hydrolysis by fatty acid amide hydrolase (FAAH) attenuates pain in animal models of osteoarthritis (OA) but has failed in clinical trials."3.81A multi-target approach for pain treatment: dual inhibition of fatty acid amide hydrolase and TRPV1 in a rat model of osteoarthritis. ( Binkowski, M; Czaja, M; Di Marzo, V; Kolosowska, N; Makuch, W; Malek, N; Morera, E; Mrugala, M; Przewlocka, B; Starowicz, K, 2015)
"Spinal glial activation has been implicated in sustained morphine-mediated paradoxical pain sensitization."3.78Repeated morphine treatment-mediated hyperalgesia, allodynia and spinal glial activation are blocked by co-administration of a selective cannabinoid receptor type-2 agonist. ( Keresztes, A; Largent-Milnes, TM; Ren, J; Roeske, WR; Tumati, S; Vanderah, TW; Varga, EV, 2012)
"In this study we analyzed the mechanisms underlying celecoxib-induced analgesia in a model of inflammatory pain in rats, using the intracerebroventricular (i."3.78Endogenous opioid and cannabinoid mechanisms are involved in the analgesic effects of celecoxib in the central nervous system. ( Bakhle, YS; Camêlo, VM; Dos Reis, WG; Faraco, A; Francischi, JN; Paiva-Lima, P; Rezende, RM, 2012)
"Cannabinoids, such as anandamide, are involved in pain transmission."3.74AM404 decreases Fos-immunoreactivity in the spinal cord in a model of inflammatory pain. ( Bianchi, R; Borsani, E; Labanca, M; Rodella, LF, 2007)
"Obesity is characterized by chronic low-grade inflammation that contributes to development of cardiometabolic disorders."1.51Cannabinoid Receptor 1 Blockade Attenuates Obesity and Adipose Tissue Type 1 Inflammation Through miR-30e-5p Regulation of Delta-Like-4 in Macrophages and Consequently Downregulation of Th1 Cells. ( Mehrpouya-Bahrami, P; Miranda, K; Nagarkatti, M; Nagarkatti, PS, 2019)
"The results showed that JZL lowered brain infarction, neurological disorders, TNF-α and MMP9 more effectively than JZL plus AM251."1.48JZL184, as a monoacylglycerol lipase inhibitor, down-regulates inflammation in a cannabinoid pathway dependent manner. ( Allahtavakoli, M; Bazmandegan, G; Moghadam-Ahmadi, A; Rahmani, MR; Shamsizadeh, A, 2018)

Research

Studies (20)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (25.00)29.6817
2010's13 (65.00)24.3611
2020's2 (10.00)2.80

Authors

AuthorsStudies
Rodrigues, FF1
Morais, MI1
Melo, ISF1
Augusto, PSA1
Dutra, MMGB1
Costa, SOAM1
Costa, FC1
Goulart, FA1
Braga, AV1
Coelho, MM1
Machado, RR1
Zhang, D1
Liu, X1
Dong, X1
Zhu, R1
Jiang, J1
Ye, Y1
Jiang, Y1
Rahmani, MR1
Shamsizadeh, A1
Moghadam-Ahmadi, A1
Bazmandegan, G1
Allahtavakoli, M1
Miranda, K1
Mehrpouya-Bahrami, P1
Nagarkatti, PS1
Nagarkatti, M1
Prestifilippo, JP1
Medina, VA1
Mohn, CE1
Rodriguez, PA1
Elverdin, JC1
Fernandez-Solari, J1
Petrenko, AB1
Yamazaki, M1
Sakimura, K1
Kano, M1
Baba, H1
Krustev, E1
Reid, A1
McDougall, JJ1
Malek, N1
Mrugala, M1
Makuch, W1
Kolosowska, N1
Przewlocka, B1
Binkowski, M1
Czaja, M1
Morera, E1
Di Marzo, V1
Starowicz, K1
Carey, LM1
Slivicki, RA1
Leishman, E1
Cornett, B1
Mackie, K1
Bradshaw, H1
Hohmann, AG1
Sagar, DR1
Kendall, DA1
Chapman, V1
Potenzieri, C1
Brink, TS1
Pacharinsak, C1
Simone, DA1
Lin, XH1
Yuece, B1
Li, YY1
Feng, YJ1
Feng, JY1
Yu, LY1
Li, K1
Li, YN1
Storr, M1
Alhamoruni, A1
Wright, KL1
Larvin, M1
O'Sullivan, SE1
Ebrahimzadeh, M1
Haghparast, A1
Tumati, S1
Largent-Milnes, TM1
Keresztes, A1
Ren, J1
Roeske, WR1
Vanderah, TW1
Varga, EV1
Escobar, W1
Ramirez, K1
Avila, C1
Limongi, R1
Vanegas, H1
Vazquez, E1
Rezende, RM1
Paiva-Lima, P1
Dos Reis, WG1
Camêlo, VM1
Faraco, A1
Bakhle, YS1
Francischi, JN1
Guindon, J1
De Léan, A1
Beaulieu, P1
Borsani, E1
Labanca, M1
Bianchi, R1
Rodella, LF1
Mitchell, VA1
Greenwood, R1
Jayamanne, A1
Vaughan, CW1

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Osteoarthritis of the Knee Pain Study Using CBD and THC in Rapidly Dissolvable Sublingual Tablet[NCT04195269]Phase 230 participants (Anticipated)Interventional2020-04-20Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Other Studies

20 other studies available for am 251 and Inflammation

ArticleYear
Clindamycin inhibits nociceptive response by reducing tumor necrosis factor-α and CXCL-1 production and activating opioidergic mechanisms.
    Inflammopharmacology, 2020, Volume: 28, Issue:2

    Topics: Analgesics; Animals; Anti-Bacterial Agents; Anti-Inflammatory Agents; Behavior, Animal; Carrageenan;

2020
Cannabinoid 1 Receptor Antagonists Play a Neuroprotective Role in Chronic Alcoholic Hippocampal Injury Related to Pyroptosis Pathway.
    Alcoholism, clinical and experimental research, 2020, Volume: 44, Issue:8

    Topics: Alcohol-Induced Disorders, Nervous System; Animals; Cannabinoid Receptor Agonists; Cannabinoid Recep

2020
JZL184, as a monoacylglycerol lipase inhibitor, down-regulates inflammation in a cannabinoid pathway dependent manner.
    Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 2018, Volume: 103

    Topics: Animals; Benzodioxoles; Brain Edema; Brain Infarction; Cannabinoids; Down-Regulation; Enzyme Inhibit

2018
Cannabinoid Receptor 1 Blockade Attenuates Obesity and Adipose Tissue Type 1 Inflammation Through miR-30e-5p Regulation of Delta-Like-4 in Macrophages and Consequently Downregulation of Th1 Cells.
    Frontiers in immunology, 2019, Volume: 10

    Topics: Adaptor Proteins, Signal Transducing; Adipose Tissue; Animals; Calcium-Binding Proteins; Diet, High-

2019
Endocannabinoids mediate hyposalivation induced by inflammogens in the submandibular glands and hypothalamus.
    Archives of oral biology, 2013, Volume: 58, Issue:9

    Topics: Analysis of Variance; Animals; Cannabinoid Receptor Agonists; Dinoprostone; Endocannabinoids; Hypoth

2013
Augmented tonic pain-related behavior in knockout mice lacking monoacylglycerol lipase, a major degrading enzyme for the endocannabinoid 2-arachidonoylglycerol.
    Behavioural brain research, 2014, Sep-01, Volume: 271

    Topics: Animals; Arachidonic Acids; Benzodioxoles; Cannabinoid Receptor Modulators; Endocannabinoids; Glycer

2014
Tapping into the endocannabinoid system to ameliorate acute inflammatory flares and associated pain in mouse knee joints.
    Arthritis research & therapy, 2014, Sep-27, Volume: 16, Issue:5

    Topics: Acute Disease; Amidohydrolases; Animals; Arthralgia; Benzamides; Carbamates; Carrageenan; Endocannab

2014
A multi-target approach for pain treatment: dual inhibition of fatty acid amide hydrolase and TRPV1 in a rat model of osteoarthritis.
    Pain, 2015, Volume: 156, Issue:5

    Topics: Activating Transcription Factor 3; Amidohydrolases; Anilides; Animals; Arachidonic Acids; Benzamides

2015
A pro-nociceptive phenotype unmasked in mice lacking fatty-acid amide hydrolase.
    Molecular pain, 2016, Volume: 12

    Topics: Acrylamides; Amidohydrolases; Analgesia; Animals; Arachidonic Acid; Bridged Bicyclo Compounds, Heter

2016
Inhibition of fatty acid amide hydrolase produces PPAR-alpha-mediated analgesia in a rat model of inflammatory pain.
    British journal of pharmacology, 2008, Volume: 155, Issue:8

    Topics: Amidohydrolases; Analgesia; Animals; Benzamides; Carbamates; Carrageenan; Disease Models, Animal; In

2008
Cannabinoid modulation of cutaneous Adelta nociceptors during inflammation.
    Journal of neurophysiology, 2008, Volume: 100, Issue:5

    Topics: Action Potentials; Analysis of Variance; Animals; Arachidonic Acids; Cannabinoids; Dose-Response Rel

2008
A novel CB receptor GPR55 and its ligands are involved in regulation of gut movement in rodents.
    Neurogastroenterology and motility, 2011, Volume: 23, Issue:9

    Topics: Animals; Cannabidiol; Electromyography; Gastrointestinal Motility; Gastrointestinal Transit; Indoles

2011
Cannabinoids mediate opposing effects on inflammation-induced intestinal permeability.
    British journal of pharmacology, 2012, Volume: 165, Issue:8

    Topics: Amidohydrolases; Benzamides; Benzodioxoles; Caco-2 Cells; Cannabinoids; Carbamates; Cell Survival; E

2012
Analgesic effects of cannabinoid receptor agonist WIN55,212-2 in the nucleus cuneiformis in animal models of acute and inflammatory pain in rats.
    Brain research, 2011, Oct-28, Volume: 1420

    Topics: Analgesics; Analysis of Variance; Animals; Area Under Curve; Benzoxazines; Cannabinoid Receptor Agon

2011
Repeated morphine treatment-mediated hyperalgesia, allodynia and spinal glial activation are blocked by co-administration of a selective cannabinoid receptor type-2 agonist.
    Journal of neuroimmunology, 2012, Volume: 244, Issue:1-2

    Topics: Analgesics; Analgesics, Opioid; Animals; Cannabinoids; Hyperalgesia; Indoles; Inflammation; Interleu

2012
Metamizol, a non-opioid analgesic, acts via endocannabinoids in the PAG-RVM axis during inflammation in rats.
    European journal of pain (London, England), 2012, Volume: 16, Issue:5

    Topics: Action Potentials; Animals; Anti-Inflammatory Agents, Non-Steroidal; Cannabinoid Receptor Modulators

2012
Endogenous opioid and cannabinoid mechanisms are involved in the analgesic effects of celecoxib in the central nervous system.
    Pharmacology, 2012, Volume: 89, Issue:3-4

    Topics: Analgesics; Animals; Carrageenan; Celecoxib; Central Nervous System; Cyclooxygenase 2; Cyclooxygenas

2012
Local interactions between anandamide, an endocannabinoid, and ibuprofen, a nonsteroidal anti-inflammatory drug, in acute and inflammatory pain.
    Pain, 2006, Volume: 121, Issue:1-2

    Topics: Acute Disease; Analysis of Variance; Animals; Anti-Inflammatory Agents, Non-Steroidal; Arachidonic A

2006
AM404 decreases Fos-immunoreactivity in the spinal cord in a model of inflammatory pain.
    Brain research, 2007, Jun-04, Volume: 1152

    Topics: Animals; Arachidonic Acids; Capsaicin; Endocannabinoids; Immunohistochemistry; Indoles; Inflammation

2007
Actions of the endocannabinoid transport inhibitor AM404 in neuropathic and inflammatory pain models.
    Clinical and experimental pharmacology & physiology, 2007, Volume: 34, Issue:11

    Topics: Analgesics; Animals; Arachidonic Acids; Cannabinoid Receptor Modulators; Carrier Proteins; Disease M

2007