The pharmacokinetics of thyrotropin-releasing hormone (TRH) and deamido-TRH in the rat.

Abstract:

:The pharmacokinetics of TRH and its metabolite deamido-TRH (TRH-OH) were evaluated and compared. After a 60- to 90-min infusion of the appropriate peptide into rats, the MCR, half-life of disappearance (t 1/2), and volume of distribution were calculated. The MCR of TRH averaged 4 ml/min, whereas that of TRH-OH was 6.5 ml/min. The serum concentrations of both TRH and TRH-OH decreased in a biexponential manner after stopping the corresponding peptide infusions. The t 1/2 values were 2.4 and 3.9 min for the initial phase of disappearance and 14.1 and 20.6 min for the later phase of disappearance for TRH and TRH-OH, respectively. The volume of distribution of TRH-OH was twice that of TRH. The fractional conversion rate of TRH to TRH-OH, based on serum TRH-OH concentrations measured during TRH infusions, was 0.7-1.4%. Less than 1 ng TRH-OH was excreted in the urine during the last 30 min of TRH infusion. The rapid clearance of TRH-OH and low fractional conversion of TRH to TRH-OH, as measured in serum, suggest that little TRH secretion will be reflected in serum TRH-OH concentrations.

journal_name

Endocrinology

journal_title

Endocrinology

authors

Safran M,Wu CF,Matys R,Alex S,Emerson CH

doi

10.1210/endo-115-3-1031

subject

Has Abstract

pub_date

1984-09-01 00:00:00

pages

1031-7

issue

3

eissn

0013-7227

issn

1945-7170

journal_volume

115

pub_type

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