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Metabolism of AM404 From Acetaminophen at Human Therapeutic Dosages in the Rat Brain

, : Metabolism of AM404 From Acetaminophen at Human Therapeutic Dosages in the Rat Brain. Anesthesiology and Pain Medicine 6(1): E32873-E32873

Acetaminophen, an analgesic and antipyretic drug, has been used clinically for more than a century. Previous studies showed that acetaminophen undergoes metabolic transformations to form an analgesic compound, N-(4-hydroxyphenyl) arachidonamide (AM404), in the rodent brain. However, these studies were performed with higher concentrations of acetaminophen than are used in humans. The aim of the present study was to examine the metabolism of AM404 from acetaminophen in the rat brain at a concentration of 20 mg/kg, which is used in therapeutic practice in humans, and to compare the pharmacokinetics between them. We used rat brains to investigate the metabolism of AM404 from acetaminophen at concentrations (20 mg/kg) used in humans. In addition, we determined the mean pharmacokinetic parameters for acetaminophen and its metabolites, including AM404. The maximum plasma concentrations of acetaminophen and AM404 in the rat brain were 15.8 µg/g and 150 pg/g, respectively, with corresponding AUC0-2h values of 8.96 μg hour/g and 117 pg hour/g. The tmax for both acetaminophen and AM404 was 0.25 hour. These data suggest that AM404's concentration-time profile in the brain is similar to those of acetaminophen and its other metabolites. Measurement of blood acetaminophen concentration seems to reflect the concentration of the prospective bioactive substance, AM404.


PMID: 27110534

DOI: 10.5812/aapm.32873

Other references

Anonymous, 1988: Prospects for the rural environment in an industrial region. The example of Saarland. Published following the Spring conference of the Agricultural Sociology Society, 9-11 June 1988 in Homburg, within the framework of the European campaign for the rural environment 1987-88. The publication offers a number of brief papers which were presented at the Agricultural Sociology Society conference (ASG) in Hamburg, GFR, in June 1988. The conference was attended by representatives from various regional government departments,...

Phair George; Levine Harry, 1953: Notes on the differential leaching of uranium, radium, and lead from pitchblende in H (sub 2) SO (sub 4) solutions. Economic Geology and the Bulletin of the Society of Economic Geologists 48(5): 358-369

Michel, H.; Kammerer, H., 1958: Professor Hugo Kämmerer on his 80th birthday. Allergie und Asthma 4(4-5): 187-188

Kaur, K.; Santosh., 1966: Comparative study of the two races of silkworm (Bombyx mori) Ver Jaune 45 and Bughdad White. Proceedings of the Indian Science Congress, 53: 359-360

Stiefenhofer Johann; Farrow Darrel J., 2004: Geology of the Mwadui Kimberlite, Shinyanga District, Tanzania. The Mwadui pipe represents the largest diamondiferous kimberlite ever mined and is an almost perfectly preserved example of a kimberlitic crater in-fill, albeit without the tuff ring.The geology of Mwadui can be subdivided into five geological uni...

Tian, C-Xia.; Li, Y.; Wang, M.; Xia, Z-En.; Li, X-Yan.; Huang, C-Xin., 2009: Association between inflammatory cytokine CD40 gene polymorphism and risk of acute coronary syndrome. To investigate the expression levels of CD40, sCD40L, hs-CRP, WBC in acute coronary syndrome (ACS) patients and the association between CD40-1C/T single nucleotide polymorphism and risk of ACS in Han Chinese, moreover, the regulatory effects of IF...

Poulsen, P.R.; Jensen, G.K.; Neimann-Sorensen, A.; Nielsen, E., 1970: Spontaneous oxidized flavour in milk: influence of genetic relations. Investigations covering 1102 cows sired by 60 bulls of the Danish Red, Danish Black Pied, and Jersey breeds demonstrated considerable differences between the breeds in their tendency to oxidized flavour.

Figueras, A.; Laporte, J-Ramon., 2002: Regulatory decisions in a globalised world: the domino effect of phenylpropanolamine withdrawal in Latin America. Rapid drug regulatory decisions regarding phenylpropanolamine (PPA)-containing common cold remedies and diet pills were taken in some Latin American countries following a US Food and Drug Administration (FDA) decision in the US. This situation is...

Minamimoto, R.; Hancock, S.; Schneider, B.; Chin, F.T.; Jamali, M.; Loening, A.; Vasanawala, S.; Gambhir, S.Sam.; Iagaru, A., 2016: Pilot Comparison of ⁶⁸Ga-RM2 PET and ⁶⁸Ga-PSMA-11 PET in Patients with Biochemically Recurrent Prostate Cancer. Glu-NH-CO-NH-Lys-(Ahx)-[(68)Ga(HBED-CC)] ((68)Ga-PSMA-11) is a PET tracer that can detect prostate cancer relapses and metastases by binding to the extracellular domain of PSMA. (68)Ga-labeled DOTA-4-amino-1-carboxymethyl-piperidine-D-Phe-Gln-Trp-...

Chelvan, P.; Hamilton-Miller, J.M.; Brumfitt, W., 1979: Biliary excretion of erythromycin after parenteral administration. 1 The biliary excretion of erythromycin has been studied following parenteral administration in 23 patients. 2 Mean bile levels of the drug were approximately ten times higher than corresponding serum concentrations 1 h after i.v. (erythromycin la...