Table 1.

A summary of the most common agonists and antagonists of the CRF family

	Agonist					Antagonist
	Name	Peptide/nonpeptide	Peptide sequence	Binding affinity Ki (nM)	References	Name	Peptide/nonpeptide	Peptide sequence	Binding affinity Ki (nM)	References
CRF-R1	h/r CRF	Peptide	SEEPPISLDLT FHLLREVLEM ARAEQLAQQA HSNRKLMEII	1.0 (0.2–4.6)	109, 131	Alpha-helical CRF fragment 9–41	Peptide	DLT FHLLREMLEM AKAEQEAEQA ALNRLLLEEA	19 (5.5–66)	108, 129, 130
						Astressin	Peptide	fHLLREVLEZ ARAEQLAQEA HKNRKLZEII	0.7 (0.3–1.8)	101, 129
						Antalarmin	Non-peptide	NA	1	110, 132
						CP-154,526	Non-peptide	NA	2.7	110, 132
						CP-316,311	Non-peptide	NA	6.8	110, 111
	h UCN I	Peptide	DNPSLSIDLT FHLLRTLLEL ARTQSQRERA EQNRIIFDSV	0.1 (0.1–0.2)	109, 131	CRA-0450	Non-peptide	NA	40–60	110, 133
						NBI-30775/R121919	Non-peptide	NA	3.5	114 , 134 , 135
						Pexacerfont	Non-peptide	NA	7.2 ± 0.9	113 , 136
						Verucerfont	Non-peptide	NA	6.1	136
CRF-R2	h/r CRF	Peptide	SEEPPISLDLT FHLLREVLEM ARAEQLAQQA HSNRKLMEII	6.2 (2.0–19)	109, 131	Antisauvagine 30	Peptide	fHLLRKMIEI EKQEKEKQQA ANNRLLLDTI	1.4	130
	h UCN I	Peptide	DNPSLSIDLT FHLLRTLLEL ARTQSQRERA EQNRIIFDSV	0.5 (0.3–0.7)	109, 131
	h UCN II	Peptide	IVLSLDV IGLLQILLEQ ARARAAREQA TTNARILARV	0.5 (0.2–1.2)	109, 131	Astressin2-B	Peptide	DLS FHLLRKXIEI EKQEKEKQQA ENNKLLLDLI	1.3	130
	h UCN III	Peptide	FTLSLDV TNIMNLLFNI AKAKNLRAQA AANAHLMAQI	13.5 (9.2–19.7)	109, 131
CRF-BP	CRF	Peptide	SEEPPISLDLT FHLLREVLEM ARAEQLAQQA HSNRKLMEII	0.2	109, 131	h/r CRF6-33	Peptide	ISLDLTFH LLREVLEMAR AEQLAQQAHS	0.2–5	40
	UCN I	Peptide	DNPSLSIDLT FHLLRTLLEL ARTQSQRERA EQNRIIFDSV	2	109, 131	h/r CRF9-33	Peptide	DLTFH LLREVLEMAR AEQLAQQAHS	0.2–5	40

In bold, receptor activation; underlined, ECD1-binding domain; blue letter, CRF-R2 specific; double underlined, CRF-BP sequence; Ki, binding affinity