. Author manuscript; available in PMC: 2015 Feb 18.

Published in final edited form as: ChemMedChem. 2012 Feb 28;7(5):903–909. doi: 10.1002/cmdc.201100574

Table 2.

Galanin peptide analogs synthesized with various modifications.

Analog	Sequence	hGAL₁ (nM)	hGAL₂ (nM)	R2/R1
Gal-B2	(Sar)WTLNSAGYLLGPKKK_PK	3.5 ± 1.0	51.5 ± 34.4	14.71
Gal-B9	(Sar)WTLNSAGYLLGPK_DK_DK_PK_D	0.9 ± 0.2	15.0 ± 8.5	16.67
Gal-B11	(Sar)WTLNSAGYLLGKKK_PK	25.5 ± 4.9	75.0 ± 10.6	2.94
Gal-B12	(Sar)WTLNSAGYLLKKK_PK	306.5 ± 12.0	1,323.5 ± 27.6	4.32
[des-LLGP]Gal-B2	(Sar)WTLNSAGYKKK_PK	≥ 30,000	27,395 ± 6,229	–
D-[des-LLGP]Gal-B2	(Sar)WTLNSAGYK_DK_DK_PK_D	≥ 30,000	n.d.	n.d.
L-Gal(6-Ahx)-B2	(Sar)WTLNSAGY(6-Ahx)KKK_PK	1166 ± 300	n.d.	n.d.
D-Gal(6-Ahx)-B2	(Sar)WTLNSAGY(6-Ahx)K_DK_DK_PK_D	n.d.	n.d.	n.d.
L-Gal(7-Ahp)-B2	(Sar)WTLNSAGY(7-Ahp)KKK_PK	n.d.	n.d.	n.d.

K_D is the D-amino acid of lysine, K_P is palmitoylation of N^ε-L-lysine, 6-Ahx is 6-aminohexanoic acid, 7-Ahp is 7-aminoheptanoic acid. Competitive receptor binding assays were performed on human galanin receptor membrane preparations.