Impact of up- and downregulation on relevant pharmacological parameters for agonists
| Target change | Cause | Baseline R0 | Complex RLss | Potency EC50 (numerical value = nv) | Efficacy parameter Emax | Comment |
|---|---|---|---|---|---|---|
| Upregulation (increased concentration of target R or complex RL) | ksyn ↑ | ↑ | ↑ | ↔ | ↑ | Baseline and complex and efficacy increase since target synthesis rate impacts all (eq. 3). Potency remains unchanged (eq. 2). |
| kdeg ↓ | ↑ | ↔ | ↑ (nv=↓) | ↔ | Baseline and potency increase (lower numerical value, eq. 2) whereas complex and efficacy remain unchanged. | |
| ke(RL) ↓ | ↔ | ↑ | ↓ (nv=↑) | ↑ | Baseline unchanged, complex and efficacy increase, but potency drops (increased numerical value (eqs. 2 and 3) | |
| Downregulation (decreased concentration of target R or complex RL) | ksyn ↓ | ↓ | ↓ | ↔ | ↓ | Baseline, complex, and efficacy decrease since target synthesis rate impacts all (eq. 3). Potency remains unchanged (eq. 2). |
| kdeg ↑ | ↓ | ↔ | ↓ (nv=↑) | ↔ | Baseline and potency decrease (higher numerical value, eq. 2) whereas complex and efficacy remain unchanged. | |
| ke(RL) ↑ | ↔ | ↓ | ↑ (nv=↓) | ↓ | Baseline unchanged, complex and efficacy decrease, but increased potency (decreased numerical value (eqs. 2 and 3) |