Fasciola hepatica: effects of diamfenetide free amine on in vitro physiology, biochemistry, and morphology.
Short-term (1-3 hr) incubations in vitro of immature and adult Fasciola hepatica with 10(-4) to 10(-5) M free amine of diamfenetide (DPT-FA) demonstrated a time/dose-dependent, irreversible paralysis that involved an increase in muscular tension and decrease in contraction amplitude. The following events occurred preceding or concomitant with the paralysis: influx of Na+, decrease in surface membrane potential, increase in wet weight, swellings on the ventral surface, and inhibition of 3-O-methyl glucose transport. These events were all consistent with a disturbance in surface membrane functions. The effects of DPT-FA were more severe in immature flukes (3-5 weeks postinfection) than adults which agrees with observed in vivo efficacy.
D019325:3-O-Methylglucose; D000083:Acetanilides / Q000494:pharmacology*; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D003957:Diamfenetide / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005210:Fasciola hepatica / Q000187:drug effects* / Q000502:physiology / Q000648:ultrastructure; D008564:Membrane Potentials / Q000187:drug effects; D008757:Methylglucosides / Q000378:metabolism; D009119:Muscle Contraction / Q000187:drug effects; D011188:Potassium / Q000378:metabolism; D012701:Serotonin / Q000494:pharmacology; D012964:Sodium / Q000378:metabolism; D013997:Time Factors
D000083:Acetanilides; D008757:Methylglucosides; D019325:3-O-Methylglucose; D012701:Serotonin; D012964:Sodium; D011188:Potassium; D003957:Diamfenetide