Norvaline super(2)-TRH: Binding to TRH receptors in rat brain homogenates

Norvaline super(2)-TRH: Binding to TRH receptors in rat brain homogenates

Norvaline super(2)-thyrotropin-releasing hormone ((Nva super(2))TRH) has been described as a thyrotropin-releasing hormone (TRH) analog with no thyrotropin (TSH)-releasing capacity but enhanced analeptic activity compared with TRH, as shown by the reversal of haloperidol-induced catalepsy. The autho...

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Veröffentlicht in:European journal of pharmacology 1990-01, Vol.180 (1), p.1-12
Hauptverfasser: Vonhof, S, Feuerstein, G Z, Cohen, LA, Labroo, V M
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container_title European journal of pharmacology
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creator Vonhof, S
Feuerstein, G Z
Cohen, LA
Labroo, V M
description Norvaline super(2)-thyrotropin-releasing hormone ((Nva super(2))TRH) has been described as a thyrotropin-releasing hormone (TRH) analog with no thyrotropin (TSH)-releasing capacity but enhanced analeptic activity compared with TRH, as shown by the reversal of haloperidol-induced catalepsy. The authors evaluated the receptor-binding properties of (Nva super(2))TRH in homogenates of rat anterior pituitary, hypothalamus, brainstem and cortex tissue, using ( super(3)H)TRH and ( super(3)H)(3-Me-His super(2))TRH as radioligands. Additionally, (Nva super(2))TRH was shown to compete with ( super(3)H)TRH at low affinity TRH-binding sites with similar affinities. It is concluded that the loss of TSH-releasing activity of (Nva super(2))TRH appears to be due to a drastic reduction in binding affinity to the high affinity TRH receptor subtype.
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title Norvaline super(2)-TRH: Binding to TRH receptors in rat brain homogenates
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