Variable | Affinitya | ||
---|---|---|---|
BB1 | BB2 | BB3 | |
nM | |||
Naturally occurring agonist | |||
GRP | 440 | 18 | >10,000 |
NMB | 4 | 248 | >10,000 |
Bombesin | 34 | 4 | >10,000 |
Litorin | 7 | 6 | >10,000 |
Ranatensin | 13 | 2 | >10,000 |
Alytesin | 460 | 62 | >10,000 |
Phyllolitorin | 47 | 240 | >10,000 |
Neuromedin C (GRP18–27) | 140 | 20 | >10,000 |
[Phe13]bombesin | 350 | 0.77 | >10,000 |
Synthetic agonists | |||
[d-Phe6,β-Ala11,Phe13,Nle14]Bn6–14 | 0.36 | 0.99 | 4.2 |
[d-Tyr6,(R)-Apa11,Phe13,Nle14]Bn6–14b | 7200 | >1900 | 8.2 |
[d-Tyr6,Apa-4Cl11,Phe13,Nle14]Bn6–14b | 2400 | 151 | 2.8 |
Ac-Phe,Trp,Ala,His (tBzl),Nip,Gly,Arg-NH2b | 3800 | 5000 | 259 |
[d-Phe6]Bn6–14 | 14 | 2 | >10,000 |
[d-Phe6,d-Ala11,Leu14]Bn6–14 | 7600 | 13 | >10,000 |
Antagonists | |||
[d-Phe6]Bn6–13 methyl ester | 7500 | 1.1 | >10,000 |
N-Propionyl-[d-Ala11]GRP20–26 methyl ester | 13,660 | 3.4 | >10,000 |
Pd 168368 | 39 | 1300 | 1010 |
d-Nal,Cys,Tyr,d-Trp,Lys,Val,Cys, Nal-NH2 | 59 | 2780 | >10,000 |
[Tyr4,d-Phe12]Bn6–14 | 1900 | >10,000 | >10,000 |
[Leu13,ψ13–14,Leu14]Bn6–14 | >10,000 | 430 | >10,000 |
[d-Phe6,Leu13,Cpa14,ψ13–14]Bn6–14 | 2700 | 42 | 6800 |
BW2258U89 | >10,000 | 0.74 | >10,000 |
[d-Arg1,d-Trp7,9,Leu11]substance P | 4,100 | 11,300 | >10,000 |
JMV594 | >10,000 | 2.2 | >10,000 |
JMV641 | 1500 | 0.46 | >10,000 |
↵a All data are for rat BB1, mouse BB2, and human BB3 except for data indicated in footnote b. Data are from Coy et al. (1992b), Mantey et al. (1997), Pradhan et al. (1998), Ryan et al. (1998b, 1999), Katsuno et al. (1999), and Tokita et al. (2001b)
↵ b Data are from human BB1, BB2, and BB3 (Mantey et al., 2001, 2004, 2006)