Thyrotropin-releasing hormone receptors

Overview

Thyrotropin-releasing hormone (TRH) receptors are activated by the endogenous tripeptide TRH (pGlu-His-ProNH2). TRH and TRH analogues fail to distinguish TRH₁ and TRH₂ receptors [1]. [³H]TRH (human, mouse, rat) is... [read more] able to label both TRH₁ and TRH₂ receptors with K_d values of 13 and 9 nM respectively. Synthesis and biology of ring-modified L-Histidine containing TRH analogues has been reported [2].

References

Sun Y, Lu X, Gershengorn MC. Thyrotropin-releasing hormone receptors -- similarities and differences. J Mol Endocrinol 2003;30:87-97.
Meena CL, Thakur A, Nandekar PP, et al. Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues. Eur J Med Chem 2016;111:72-83.

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Human	TRHR thyrotropin releasing hormone receptor
Mouse	Trhr thyrotropin releasing hormone receptor

Human

TRHR

thyrotropin releasing hormone receptor

Mouse

Trhr

thyrotropin releasing hormone receptor

Species	Receptor	Family	Assays
Human	TRHR thyrotropin releasing hormone receptor	Thyrotropin-releasing hormone receptors	Available Assay modes: Agonist ⋅ Inverse agonist ⋅ Antagonist ⋅ PAM ⋅ NAM Panels: Human non-orphan GPCRs ⋅ Endocrinology/Metabolism ⋅ Musculoskeletal ⋅ à la carte	Reference agonist: TRH EC50: 160 pM
Mouse	Trhr thyrotropin releasing hormone receptor	Thyrotropin-releasing hormone receptors	Available Assay modes: Agonist ⋅ Inverse agonist ⋅ Antagonist ⋅ PAM ⋅ NAM Panels: Mouse non-orphan GPCRs ⋅ à la carte	Reference agonist: TRH EC50: 400 pM

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