Nonpeptidic agonists/antagonists

Sawada Y, Kayakiri H, Abe Y, et al. A new class of nonpeptide bradykinin B2 receptor ligands, incorporating a 4-aminoquinoline framework. Identification of a key pharmacophore to determine species difference and agonist/antagonist profile. 7 Med Chem 2004 47 2667-77. 

Both peptide and nonpeptide 5-opioid antagonists have been developed. The nonpeptide 6-antagonist naltrindole and its analogues are described in Chapter 9 of this volume. In the present chapter, the development of opioid peptide-derived 6-antagonists, inverse 6-agonists, and mixed p-agonist/6-antagonists is reviewed. 

There is enormous activity worldwide seeking to identify nonpeptide agonists or antagonists for both the peptide receptors and the orphans, since it is expected that this will be a fruitful area for drug discovery - witness the success of the nonpeptide angiotensin II receptor antagonists (collectively known as the sartans ) approved several years ago for the treatment of hypertension. 

Fig. 4. Structures of several nonpeptide opioid agonists, (a) morphine, (c) BW373U86, (e) U50488 and antagonists, (b) naloxone, (d) naltrindole, and (f)...

SR 48692 Nonpeptide antagonist at NTS1 agonist at NTS2 Inhibition of tumor growth drug addiction treatment... 

Nonpeptide Antagonists May Bind Rather Differently from the Agonist.103... 

Compound 686 (PNU-97018) is an orally active nonpeptide angiotensin II receptor antagonist without any agonistic activity that has an insurmountably high antihypertensive effect <2002CPB1022, 1995JEP1042, 1995MI880>. 

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