Neuroreceptor

Nutt DJ, Linnoila M Neuroreceptor science a clarification of terms. J Clin Psycho-pharmacol 8 387-389, 1988... 

Liechti, M.E. and Vollenweider, F.X., Which neuroreceptors mediate the subjective effects of MDMA in humans A summary of mechanistic studies, Hum. Psychopharmacol. 16(8), 589-598, 2001. 

Determining the underlying rationale for studying a neuroreceptor system, e.g. the dopamine hypothesis for cocaine abuse and schizophrenia ... 

Understanding the mechanism of action of various drugs, especially those that act on neuroreceptors systems ... 

To calculate these measures in PET/SPECT, typically two- or three-compartment models are employed. Such models have been the basis for extension into neuroreceptor imaging of the methods described below. 

Wong, D. F. and Pomper, M. G. Predicting the success of a radiopharmaceutical for in vivo imaging of central nervous system neuroreceptor systems. Mol. Imaging Biol. 5 350-362, 2003. 

Gjedde, A. and Wong, D. F. Quantification of neuroreceptors in living human brain, v. Endogenous neurotransmitter inhibition of haloperidol binding in psychosis. /. Cereb. Blood Flow Metab. 21 982-994,2001. 

Gephyrin was initially found in the central nervous system, where it is essential for the clustering of inhibitory neuroreceptors in the postsynaptic membrane. 

Nordberg A. (1992). Neuroreceptor changes in Alzheimer disease. Cerebrovasc Brain Metab Rev. 

Ichise M, Meyer JH, Yonekura Y. 2001. An introduction to PET and SPECT neuroreceptor quantification models. JNuclMed 42 755-763. 

To be ready for the next odor stimulus, jS-adrenoceptor kinase (Bark) 2 inactivates a receptor only a tenth of a second after the first stimulation occurred. This kinase phosphorylates the activated receptor, which allows another protein, B-arrestin, to bind to the receptor and inactivate it. This is a specific example of a group of enzymes that deactivate hormone or neuroreceptors (Dawson et al., 1993). 

Brett PM, Curtis D, Robertson MM, Curling HM (1995) Exclusion of the 5-HTlA serotonin neuroreceptor and tryptophan oxygenase genes in a large British kindred multiply affected with Tourette s syndrome, chronic motor tics, and obsessive-compulsive behavior. Am J Psychiatry 152 437-440... 

Bunce K, Tyers M, Beranek P Clinical evaluation of S-HTj receptor antagonists as anti-emetics. Trends Pharmacol Sci 12 46-48, 1991 Bunney WE Neuronal receptor function in psychiatry strategy and theory, in Neuroreceptors Basic and Clinical Aspects. Edited by Usdin E, Bunney WE Jr, Davis JM. New York, Wiley, 1981... 

Venlafaxine, a phenylethylamine, sequentially inhibits first the neuronal uptake pump for serotonin and then NE ( 137). In contrast to tertiary amine TCAs, which can also inhibit serotonin and NE uptake pumps, venlafaxine has low binding for most other neuroreceptors and does not inhibit Na ion fast channels, making it relatively safe in overdoses compared with TCAs. 

Because of its sequential, concentration-dependent effects on 5-HT and NE uptake pumps, venlafaxine may offer a wider spectrum of efficacy than SSRIs. Because of its absence of effects on other neuroreceptors and fast Na channels, venlafaxine has a better safety and tolerability profile than do TCAs. 

Venlafaxine is the only marketed antidepressant that inhibits both the uptake pumps for serotonin and NE without affecting numerous neuroreceptors in contrast to tertiary amine TCAs. However, several have been or are under development, including duoloxetine and milnicipram ( 446). 

Beaudet, A. Dournaud, P. Boudin, H. Complementarity of radioautographic and immunohistochemical techniques for localizing neuroreceptors at the light and electron microscopy level. Braz. J. Med. Biol. Res. 1998, 37(2), 215-223. 

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