Table 1.

Summary of galanin receptor agonists, their structures, and respective binding affinities. All analogues are C-terminal amides.

				KI in nM
	Entry	Ligand	Strucure	hGalR1	hGalR2	Ref.
hGalR1	1	Galanin	GWTLNSAGYLLGPHAVGNHRSFSDKNGLTS-CONH2	0.03	0.9	14, 15
	2	C7	GWTLNSAGYLLGPrPKPQQwFwLL-CONH2a	0.08	0.6	14, 16
	3	M15	GWTLNSAGYLLGPQQFFGLM-CONH2	0.03	1.1	14, 16
	4	M32	GWTLNSAGYLLGPRHYINLITRQRY-CONH2	0.30	1.4	14, 16
	5	M35	GWTLNSAGYLLGPPPGFSPFR-CONH2	0.01	1.8	14, 15
	6	M40	GWTLNSAGYLLGPPPALALA-CONH2	0.10	1.5	14, 15
	7	GalB2	(Sar)WTLNSAGYLLGPKK(KP)K-CONH2b	3.50	52	5
	8	Galmic		34,200	>100,000c	4
	9	Galnon		11,700	34,100c	4
hGalR2	10	Gal(2-30)	WTLNSAGYLLGPHAVGNHRSFSDKNGLTS-CONH2	51d	9.8d	10
	11	Gal(2-11)	WTLNSAGYLL-CONH2	870d	1.74d	9
	12	[D-Trp2]Gal	GwTLNSAGYLLGPHAVGNHRSFSDKNGLTS-CONH2a	545d	218d	10

^aLower case letters denote D-amino acids;

^bSar = sarcosine (N-methyl glycine), K_p = lysine-palmitoyl;

^cData taken from rat GalR2;

^dDerived from IC₅₀ values using the Cheng-Prusoff equation.¹⁷