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A Simple and Rapid Evaluation of Methemoglobin Toxicity of 8-aminoquinolines and Related Compounds

A Simple and Rapid Evaluation of Methemoglobin Toxicity of 8-aminoquinolines and Related Compounds

P Srivastava, S Singh, G K Jain, S K Puri, V C Pandey

Ecotoxicol Environ Saf. 2000 Mar;45(3):236-9.

PMID: 10702341

Abstract:

Methemoglobin, a toxic ferric form of hemoglobin, is continuously formed in normal erythrocytes, but during abnormal situations in situ, the level is enhanced. 8-Amino-quinolines and related compounds are causative agents for methemoglobin formation. Employing oxyhemoglobin, methemoglobin toxicity was about six times higher with primaquine compared to CDRI Compound 80/53 at 10(-9) M concentration. Methemoglobin reductase activity was also completely inhibited by primaquine, whereas 24% inhibition was noted in the case of 80/53 at the same concentrations. Mastomys, a rodent animal model, was found to be equally good for comparative evaluation of methemoglobin toxicity. Further, with the use of primaquine transdermal tape on the Mastomys model, a rise in methemoglobin occurred with increase in time. In conclusion, the study presents simple, economical, less time-consuming methods for the evaluation of methemoglobin toxicity, in vitro and in vivo, without employing the conventional Beagle dog model.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP525611	Primaquine Related Compound A		525-61-1	Price

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