Enzyme inhibitor
This highly selective CRF2 antagonist (MW = 3650.29 g/mol; CAS 220673-95-0; Sequence: D-Phe-His-Leu-Leu-Arg-Lys-Met-Ile-Glu-Ile- Glu-Lys-Gln-Glu-Ala-Ala-Asn-Asn-Arg-Leu-Leu-Leu-Asp-Thr-Ile-NH2; Solubility: 5 mg/mL H2O; Alternate Name: [D-Phe 11 ,His 12 ]-Sauvagine (11- 40)) targets human Corticotropin-Releasing hormone (CRH) Receptor-2 subtypes CRF2β (Ki = 1.4 nM), with a much higher value of 154 nM for CRF1. (See also Astressin; K41448) Type-2 GPCRs reside in plasma membranes of hormone-sensitive cells and bind CRH, a peptide hormone and neurotransmitter involved in stress responses. Antisauvagine-30 blocks (pA2 = 8.49) sauvagine-stimulated accumulation of cAMP in HEK-mCRF2β cells. It also prevents stress-enhanced fear conditioning and MEK1/2- dependent activation of ERK1/2 in mice and suggesting a role for protein kinase signaling in the hippocampus and its modulation by CRF2 as a possible link between stress and fear memory.
