Table 4.
Studies on regulation of β3‐adrenoceptor protein and mRNA by agonist exposure
| Intervention | Protein | mRNA | Reference |
|---|---|---|---|
| In vivo treatments of animals | |||
| Rat brown adipose tissue | |||
| Ro 16‐8741, 0.87 mg·kg−1 orally, every 24 hr | Decrease | Decrease | Revelli, Muzzin, & Giacobino, 1992 |
| Noradrenaline 2 × 250 μg injection, 8 hr | n.r. | Decrease | Granneman & Lahners, 1992 |
| Isoprenaline 2 × 200 μg injection, 8 hr | n.r. | Decrease | |
| BRL 26,830, 2 × 2 mg injection, 8 hr | n.r. | Decrease | |
| Mouse brown adipose tissue | |||
| CL 316,243, 1 mg·kg−1 injection, 1–24 hr | n.r. | Decreasea | Hutchinson et al., 2000 |
| Rat white adipose tissue | |||
| Noradrenaline 2 × 250 μg injection, 8 hr | n.r. | Decrease | Granneman & Lahners, 1992 |
| Isoprenaline 2 × 200 μg injection, 8 hr | n.r. | Decrease | |
| BRL 26,830, 2 × 2 mg injection, 8 hr | n.r. | Decrease | |
| BRL 26,830, 10 mg·kg−1 injection, 4 hr | n.r. | Decrease | Granneman & Lahners, 1995 |
| FR 149,175, 0.1–3.2 mg·kg−1 twice daily p.o., 2 weeks | n.r. | No change | Hatakeyama et al., 2004 |
| Mouse white adipose tissue | |||
| CL 316,243, 1 mg·kg−1 injection, 1–24 hr | n.r. | Decrease | Hutchinson et al., 2000 |
| Mouse ileum | |||
| CL 316,243, 1 mg·kg−1 injection, 1–24 hr | No change (63–77) | No change | Hutchinson et al., 2000 |
| In vitro treatments of tissues and cells natively expressing β3‐adrenoceptor | |||
| Neonatal rat cardiomyocytes | |||
| Noradrenaline 100 μM, 24 hr | Increase | Increase | Germack & Dickenson, 2006 |
| Noradrenaline 100 mM, 72 hr | n.r. | Increase | Watts et al., 2013 |
| Hamster brown adipocytes | |||
| Isoprenaline 1 μM, 2–8 hr | n.r. | Decrease | Klaus et al., 1995 |
| Noradrenaline 1 μM, 2–8 hr | n.r. | Decrease | |
| D7114, 1 μM, 2–8 hr | n.r. | Decrease | |
| Mouse brown adipocytes | |||
| Noradrenaline 100 nM, 24 hr | n.r. | Decrease | Bengtsson, Redegren, Strosberg, Nedergaard, & Cannon, 1996 |
| 3T3‐F442 mouse adipocytes | |||
| Isoprenaline 100 μM, 4–30 hr | Increase (39) | Increase | Thomas, Holt, Schwinn, & Liggett, 1992 |
| Isoprenaline 100 μM, 2–8 hr | n.r. | Decrease | Granneman & Lahners, 1994 |
| Isoprenaline 100 μM, 4 hr | n.r. | Decrease | Granneman & Lahners, 1995 |
| Human myometrial strips | |||
| Salbutamol or SR 59,119, 10 μM, 15 hr | n.r. | No change | Rouget et al., 2004 |
| SK‐N‐MC human neuroblastoma cells | |||
| Isoprenaline 100 μM, 2–6 hr | n.r. | No change | Granneman & Lahners, 1994 |
| Isoprenaline 1–100 nM, 1–24 hr | No change (189) | n.r. | Curran & Fishman, 1996 |
| In vitro treatments of cells transfected with β3‐adrenoceptor | |||
| CHW cells | |||
| Isoprenaline 100 μM, 6–24 hr | No change (5,900) | n.r. | Liggett et al., 1993 |
| Isoprenaline 10 μM, 1–24 hr | No change (281) | No change | Nantel, Marullo, Krief, Strosberg, & Bouvier, 1994 |
| Isoprenaline 10 μM, 2–24 hr | No change (200–350) | n.r. | Nantel et al., 1995 |
| CHO cells | |||
| Isoprenaline 100 μM, 0–24 hr | No change (3,000) | n.r. | Chambers et al., 1994 |
| HEK 293 cells | |||
| Isoprenaline 100 μM, 1 hr | No change (750) | n.r. | Chaudhry & Granneman, 1994 |
| Isoprenaline 10 μM, 24 hr | No change (306) | n.r. | Michel‐Reher & Michel, 2013 |
| L cells | |||
| Isoprenaline 10 μM, 1–24 hr | Decrease (122) | Decrease | Nantel et al., 1994 |
| Isoprenaline 10 μM, 3–24 hr | Decrease (200–350) | n.r. | Nantel et al., 1995 |
| M1 cells | |||
| Mirabegron 10 nM, 6–24 hr | Decrease | n.r. | Milano et al., 2018 |
Note: Where available, baseline β3‐adrenoceptor density (fmol·mg−1·protein) is shown in parentheses. Note that some of the mRNA expression changes were transient, that is, not found at all time points investigated. Studies in transfected cells refer to the human receptor. For details, see Sections 4 and 5. n.r.: not reported.
a
Decrease observed for β3a‐ but not β3b‐adrenoceptor.