Receptor classification

Barnard EA, Skolnick P, Olsen RW et al (1998) International Union of Pharmacology. XV. Subtypes of y-aminobutyric acidA receptors classification on the basis of subunit structure and receptor function. Pharmacol Rev 50 291-313... 

Colquhoun, D., Affinity, efficacy and receptor classification is the classical theory still useful , in Perspectives on Receptor Classification, Black, J. W., Jenkinson, D. H., and Gerskowitch, V.R, Eds., Liss, New York, 1987, chap. 11. 

Measurement of dissociation equilibrium constants, which is of particular value in receptor classification and in the study of structure/activity relationships, where the effects of changes in chemical structure on affinity (and efficacy) are explored. 

Thus, cholinergic receptor classification can be considered in terms of three stages of development. Initially, Dale [2] distinguished nicotinic and muscarinic receptor subtypes with crude alkaloids. Then, chemical synthesis and structure-activity relationships clearly revealed that nicotinic and muscarinic receptors were heterogeneous, but chemical selectivity could not come close to uncovering the true diversity of receptor subtypes. Lastly, analysis of subtypes came from molecular cloning, making possible the classification of receptors on the basis of primary structure (Fig. 11-2). 

Kebabian JW, Neumeyer JL. (1994). The RBI Handbook of Receptor Classification. Natick, MA Research Biochemicals International. 

Hoyer D, Martin G (1997) 5-HT receptor classification and nomenclatm-e towards a harmonization with the himian genome. Neuropharmacology 36 419-428 Hynes M, Ye W, Wang K, Stone D, Murone M, Sauvage F, Rosenthal A (2000) The seven-transmembrane receptor smoothened cell-autonomously induces multiple ventral cell types. Nat Neurosci 3 41-46... 

D. Satchell (1984). Purine receptors classification and properties. Trends Pharmacol. Sci. 5 340-343. 

Regrettably, the receptor classification system is much more complex than this. For example, the chemokine class of cytokine receptors is further subdivided into at least 16-20 different receptor subtypes, including CCRl, CCR2. .. CCRll, CXCRl, CXCR2. .. CXCR5. These receptors interact with more than 25-30 different types of chemokines. 

FIGURE 18-2 Receptor classifications and subclassifications for acetylcholine (ACh] and norepinephrine [NE], the two primary neurotransmitters used in the autonomic nervous system. 

Respiratory smooth-muscle cells contain the beta-2 subtype of adrenergic receptors.76 (See Chapter 18 for a discussion of adrenergic receptor classifications.) Stimulation of these beta-2 receptors results in relaxation of bronchiole smooth muscle. Lienee, drugs that stimulate these beta-2 adrenergic receptors (i.e., beta-adrenergic agonists) produce bronchodilation and can be used to prevent or inhibit airway obstruction in bronchospastic diseases.22,99... 

Table 1 Tissues in which neurotransmitter release is increased (f) or decreased (J.) by presynaptic dopamine receptor activation. Receptor classification (except with superscript11) as by the authors cited. Designation as D -like or D2-like where no differentiation between D and D5, or between D2, D3 and D4, was made...

Table summarizes studies in which release was determined either as overflow or by means of the postsynaptic response. References to reviews 1, Starke et al. 1989 2, Gothert and Schiicker 1997 3, Cassel and Jeltsch 1995 4, Fuder and Muscholl 1995. a Retrospective receptor classification by T.J.F. 

Barnard, E. A., Skolnick, P, Olsen, R. W., Mohler, H., Sieghart, W., Biggio, G., Braestrup, C., Bateson, A. N., and Langer, S. Z. (1998). International Union of Pharmacology. XV. Subtypes of gamma-aminobutyric acidA receptors Classification on the basis of subunit structure and receptor function. Pharmacol. Rev. 50, 291-313. 

---