Subtype selection

Kaumann, A. J., and Marano, M. (1982). On equilibrium dissociation constants for complexes of drag receptor subtypes Selective and nonselective interactions of partial agonists with two P-adrenoceptor subtypes mediating positive chronotropic effects of (-) isoprenaline in kitten atria. Nannyn Schmiedebeberg s Arch. Pharmacol. 219 216—221. 

These findings demonstrate that subtype-selective diugs are likely to be of benefit, e.g., as anxiolytics... 

Dipeptidylpeptidase IV (also known as CD26) cleaves neuropeptide Y, and peptide YY to generate their subtype-selective fragments NPY3 36 and PYY3 36. 

Currently, more group-selective and subtype selective compounds remain to be discovered. The recent demonstration of a possible action of new subtype selective... 

The hormone peptide YY (PYY) is a 36 amino acid peptide, which is closely related to neuropeptide Y and pancreatic polypeptide. PYY is predominantly synthesised and released by intestinal endocrine cells, and can also coexist with glucagon in pancreatic acini and enteroglucagon in endocrine cells of the lower bowel. It acts on the same receptors as neuropeptide Y. The endogenous long C-terminal PYY fragment PYY3 36 is a biologically active and subtype-selective metabolite. 

Future generations of such receptor subtype-selective retinoids or also retinobenzoic acids [3] may provide clinicians with more specific and less toxic diugs for dermatologic therapy. 

Bremner,. B., Coban, B., Griffith, R Groenewoud, K. M., Yates, B. F. Ligand design for alpha] adrenoceptor subtype selective antagonists. Bioorg. Med. Chem. 2000, 8, 201-214. 

Receptor subtype selective CB2 agonists are seen as potential candidates for the treatment of a variety of diseases, including pain-related indications. The promise of useful therapeutic effects without unwanted CNS side effects makes the development of CB2 selective compounds a particularly attractive... 

Birdsall NJ, Farries T, Gharagozloo P, Kobayashi S, Lazareno S, Sugimoto M. Subtype-selective positive cooperative interactions between brucine analogs and acetylcholine at muscarinic receptors functional studies. Mol Pharmacol 1999 55 778-786. 

Jakubik J, Bacakova L, El-Fakahany EE, Tucek S. Subtype selectivity of the positive allosteric action of alcuronium at cloned M M5 muscarinic acetylcholine receptors. J Pharmacol Exp Ther 1995 274 1077-1083. 

Rivkees SA, Lasbury ME, Barbahalya H. Identification of domains of the human Ai adenosine receptor that are important for binding receptor subtype selective ligands using chimeric Ai/A2 adenosine receptors. J Biol Chem 1995 270 20485-20490. 

Recognition and quantification of receptor subtypes, which may be possible if subtype-selective ligands are available. 

More recently, the action of subtype-selective 5-HT2 receptor antagonists on sleep variables was assessed in the rat. Systemic administration of the 5-HT2a... 

Kantor, S., Jakus, R., Balogh, B., Benko, A. Bagdy, G. (2004). Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505. Br. J. Pharmacol. 142, 1332-42. 

Nishi M., Takeshima H., Fukada K., Kato S., Mori K. cDNA cloning and pharmacological characterization of an opioid receptor with high affinities for kappa-subtype selective ligands. FEBS Lett. 330 77, 1993. 

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