Receptor up-regulation

Fc receptor up-regulation on macrophages (enhancing activity of immune complex clearance)... 

Unterwald E., Ho A., Rubenfeld J., Kreek M. Time course of the development of behavioral sensitization and dopamine receptor up-regulation during binge cocaine administration. J. Pharmacol. Exp. Ther. 270 1387, 1994. 

Figure 6.21. Role of phospholipase D in receptor up-regulation. Neutrophils were incubated in the presence or absence of fMet-Leu-Phe and butanol for 15 min prior to analysis of expression of CDllb by FACS analysis. In (a), neutrophils were not stimulated and suspensions did not contain butanol. In (b), suspensions did not contain butanol, but were stimulated with fMet-Leu-Phe. The hatched lines show the receptor expression of suspensions incubated with 10, 20 and 30 mM butanol for 5 min prior to stimulation by fMet-Leu-Phe. Source Experiment of Fiona Watson.

Nicotinic receptors are widely distributed in the brain and are involved in a number of physiological processes. The prefrontal cortex is a major site for the cognitive effects of nicotine (Vidal 1996). Some of the cognitive benefits of nicotine may occur after chronic treatment, resulting in part from nicotinic receptor up-regulation in frontal, entorhinal, and dorsal hippocampal regions (Abdulla et al. 1996). Chronic nicotine treatment also increases the sensitivity of muscarinic receptors (Wang et al. 1996). 

Inflammatory cytokine activity — the lL-1 receptor and TNF receptor up-regulated. 

Receptor down-regulation is a phenomenon whereby an agonist, after binding to a receptor, acmally induces a decrease in the number of those receptors available for binding. Receptor up-regulation is the opposite and involves an agonist-induced increase in the number of receptors. 

Chronic use of beta blockers (e.g in angina, HTN) leads to receptor up-regulation. 

Bauer, B., Hartz, A. M., Fricker, G., and Miller, D. S. (2004) Pregnane X receptor up-regulation of P-glycoprotein expression and transport function at the blood-brain-barrier. 

Another way to compensate for the cell decline in PD is the D2 receptor up-regulation seen in untreated patients, whereas the L-DOPA substitution, depending on the dose, provokes either normalization or down-regulation (Rinne et al., 1981 Guttman and Seeman, 1986 Riederer et al., 1989b Montastruc, 1991 Playford and Brooks, 1992). 

Abrupt discontinuation of the drug may precipitate angina or vasospastic infarct. These effects appear to be due to cardiac receptor up-regulation, caused by chronic therapy with (5-blockers. 

Sodhi A. The Kaposi s sarcoma-associated herpes virus G protein-coupled receptor up-regulates vascular endothelial growth factor expression and secretion through mitogen-activated protein kinase and p38 pathways acting on hypoxia-inducible factor lalpha. Cancer Res 2000 60(l7) 4873-80. 

Epidermal growth factor receptor up-regulation is suggested to stimulate the respective DNA repair pathways leading thus to radioresistance. 

Li YH, Yang P, Kong WJ et al (2009) Berberine analogues as a novel class of the low-density-lipoprotein receptor up-regulators synthesis, structure-activity relationships, and cholesterol-lowering efficacy. J Med Chem 52(2) 492-501... 

BR-2llb (bupleuran 2llb) pectin (with galactan and 36,000 arabinogalactan) anti-complementary activity Fc receptor up-regulation activity Bupleurum falcatum L., 1989 [36, 92, 93]... 

Joseph JA, Bartus RT, Clody DE, Morgan D, Finch C, Beer B, Sesack S. Psycomotor performance in the senescent rodent reduction of deficits via striatal dopamine receptor up-regulation. Neurobiol Aging 1983 4 313 319. 

---