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Figure 1

A. NT. EISAI-1. NT. EISAI. R. R. V. V. VII. VII. VI. VI. JMV449. B. EISAI-1. Gi. /o. Gq. Gi. /o. Gs. Gs. Gq. InsP. Arachidonic Acid. cAMP. -10. -8. -6. -10. -8. -6. -4. -10. -8. -6. Peptide (log M). Figure 1. g. K. a. L+RG. L+RG. LRG. LRG. K. L+RG. G.

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Figure 1

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  1. A NT EISAI-1 NT EISAI R R V V VII VII VI VI JMV449 B EISAI-1 Gi /o Gq Gi /o Gs Gs Gq InsP Arachidonic Acid cAMP -10 -8 -6 -10 -8 -6 -4 -10 -8 -6 Peptide (log M) Figure 1

  2. g K a L+RG L+RG LRG LRG K L+RG G K G g K L+R LR L+R G LR L+R b k K act a k LR*G L+R*G L+R*G act g : - ability of G to alter b K L+R* LR* the affinity of L for R L+R* G K (« GTP shift »). b a : ability of G to L+R LR - ability of L to alter alter the R/R* ratio the affinity of R for G k a k act act a K a LR* L+R* a : - ability of L to alter a - agonists : >1 the R/R* ratio. a - antagonists : =1 - ratio of the affinities a - inverse agonists : <1 of L for R and R* R*G* G* k G act m : ability of R* to m k Activation G act alter the G/G* ratio (k ) G R*G G act Interaction R* Figure 2 A B

  3. LRG RG 1 1 L+R*G LR*G 1 1 R LR LRG RG LR*G 2 2 1 L+R LR LR* LR*G R*G 2 2 L+R**G LR**G 2 2 Figure 3 A B

  4. A B Pathway 1 Pathway 2 LRG LRG L+R*G LR*G RG RG 1 2 1 1 1 2 R R LR LR L+R LR LR*G LR*G R*G R*G 1 2 1 2 L+R LR R* LR* R* LR* L+R**G LR**G 2 2 Figure 4

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