Receptor altering

Spironolactone is an antiandrogen which blocks androgen-receptors, alters steroidogenesis by adrenals and gonads and inhibits 5-a reductase. In doses of 100-200 mg daily it reduces sebum production and improves inflammatory acne in women. During treatment, birth control measures are required due to the risk of male fetus feminization. 

Unterwald E.M., Kreek M.J., Cuntapay M. The frequency of cocaine administration impacts cocaine-induced receptor alterations. Brain Res. 900 103, 2001. 

Mash D.C., Staley J.K. D3 dopamine and kappa opioid receptor alterations in human brain of cocaine-overdose victims. Ann. N.Y. Acad. Sci. 877 507, 1999. 

P3-adrenergic receptor Altered leptin and insulin concentrations after agonist treatment [66]... 

Schwab BW, Costa LG, Murphy SD. 1983. Muscarinic receptor alterations as a mechanism ot anticholinesterase (EC 3.1.1.7) tolerance. Toxicol Appl Pharmacol 71 14-23. 

Binding of the signaling substance to a 7-helix receptor alters the receptor conformation in such a way that the corresponding G protein can attach on the inside of the cell. This causes the a-subunit of the G protein to exchange bound GDP for GTP (1). The G protein then separates from the receptor and dissociates into an a-subunit and a Py-unit. Both of these components bind to other membrane proteins and alter their activity ion channels are opened or closed, and enzymes are activated or inactivated. 

Cholinergic receptor alterations at the reticular nucleus prevent stable "gating" of information to and from the cortex. 

The cellular consequences of neurotransmission can be both short term (acute) and long term (chronic). Acutely, stimulation of neurotransmitter receptors alters levels of intracellular signaling molecules, which may induce the neuron to fire or alter the responsiveness of the neuron to further stimulation. Over time, the persistent activation of receptors that occurs with... 

Javitch, J. A., Fu, D., Liapakis, G., and Chen, J. (1997). Constitutive activation of the beta2 adrenergic receptor alters the orientation of its sixth membrane-spanning segment./. Biol. Chem. 272, 18546-18549. 

Berg KA, Cropper JD, Niswender CM, Sanders-Bush E, Emeson RB, Clarke WP. RNA-editing of the 5-HT(2C) receptor alters agonist-receptor-effector coupling specificity. Br J Pharmacol 2001 134 386-392. 

Price RD, Weiner DM, Chang MS, Sanders-Bush E. RNA editing of the human serotonin 5-HT2C receptor alters receptor-mediated activation of G13 protein. J Biol Chem 2001 276 44,663-44,668. 

Niswender CM, Herrick-Davis K, Dilley GE, et al. RNA editing of the human serotonin 5-HT2C receptor. Alterations in suicide and implications for serotonergic pharmacotherapy. Neuropsychopharmacology 2001 24 478-491. 

Porter JE, Perez DM. Characteristics for a salt-bridge switch mutation of the alpha(lb) adrenergic receptor. Altered pharmacology and rescue of constitutive activity. J Biol Chem 1999 274 34,535-34,538. 

Malmberg A, Strange PG. Site-directed mutations in the third intracellular loop of the serotonin 5-HT1A receptor alter G protein coupling from Gj to Gs in a ligand-dependent manner. J Neurochem 2000 75 1283-1293. 

Parkinsonian effects The inhibitory effects of dopaminergic neurons are normally balanced by the excitatory actions of cholinergic neurons. Blocking dopamine receptors alters this balance, causing a relative excess of cholinergic influence and resulting in extrapyramidal motor effects. 

Wamsley, J., Byerley, W., McCabe, R., McConnell, E., Dawson, T., 8c Grosser, B. (1987). Receptor alterations associated with serotonergic agents An autographic analysis. Journal of Clinical Psychiatry, 48, 19-85. 

K9. Klocker, H., Neuschmid-Kaspar, F., Culig, Z., Cato, A. C., Hobisch, A, etal., Androgen receptor alterations in patients with disturbances in male sexual development and in prostatic carcinoma. Urol. Int. 54, 2-5 (1995). 

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