An in vitro method for screening compounds for the effect on the rate of sickling of erythrocytes.
Since no practical animal model is available for the evaluation of compounds in vivo, we have developed an in vitro model for determining the effect of compounds on the rate of sickling of erythrocytes in whole blood taken from patients with sickle cell anaemia. RMI 6792 (a phenethanol-diamine derivative), procaine, and L-glutamine were tested in this in vitro system. RMI 6792 was tested at various concentrations in whole blood. The data indicate that RMI 6792 decreased the rate of sickling at and above 60 microgram/ml. Procaine slightly decreased sickling rate at 100 microgram/ml. L-glutamine at 555 had no inhibitory effect. RMI 6792 and procaine had no effect on the oxygen dissociation curve. RMI 6792 affected the calcium flux of the erythrocytes and the calcium concentration in the erythrocytes.
D015078:2-Hydroxyphenethylamine / Q000031:analogs & derivatives; D000755:Anemia, Sickle Cell / Q000097:blood / Q000503:physiopathology; D000814:Aniline Compounds / Q000494:pharmacology*; D000986:Antisickling Agents / Q000494:pharmacology*; D002118:Calcium / Q000097:blood; D004910:Erythrocyte Membrane / Q000187:drug effects*; D004912:Erythrocytes / Q000032:analysis / Q000187:drug effects*; D004983:Ethanolamines / Q000494:pharmacology*; D005973:Glutamine / Q000494:pharmacology*; D006801:Humans; D008722:Methods; D010100:Oxygen / Q000097:blood; D011343:Procaine / Q000494:pharmacology*
D000814:Aniline Compounds; D000986:Antisickling Agents; D004983:Ethanolamines; D005973:Glutamine; C000956:N-(2-diethylaminoethyl)-N-(2-hydroxy-2-phenylethyl)-2,5-dichloroaniline; D011343:Procaine; D015078:2-Hydroxyphenethylamine; D010100:Oxygen; D002118:Calcium