The behaviorally active peptide ACTH 4-10: measurement in plasma and pharmacokinetics in man.
A specific radioimmunoassay for the quantitative measurement of ACTH 4-10 and a procedure for its extraction from plasma have been developed. Its pharmacokinetics was studied in eight healthy male volunteers given ACTH 4-10 125 micrograms/kg body weight as a bolus i.v. injection, by infusion and intranasally. Following the i.v. bolus, plasma levels rapidly declined biexponentially, with half-lives of 0.39 +/- 0.05 min for the alpha-phase and 3.84 +/- 1.5 min for the beta-phase (mean +/- SD). The constant rate i.v. infusion yielded steady-state levels between 0.74 and 5.06 ng/ml plasma. Administered as intranasal spray, absorption of intact ACTH 4-10 was low and variable (maximal bioavailability 7.6%). The results are discussed in relation to the dose-dependent effects of ACTH 4-10 on the auditory evoked potential.
Bickel
U
U
Institut für Klinische Pharmakologie, Freie Universität Berlin, Federal Republic of Germany.
Born
J
J
Fehm
H L
HL
Distler
M
M
Voigt
K H
KH
D000281:Administration, Intranasal; D000324:Adrenocorticotropic Hormone / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics; D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D006207:Half-Life; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007262:Infusions, Intravenous; D007275:Injections, Intravenous; D008297:Male; D010446:Peptide Fragments / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics; D011863:Radioimmunoassay
D010446:Peptide Fragments; D000324:Adrenocorticotropic Hormone; C011394:ACTH (4-10)