Smoothened agonist (SAG), a chlorobenzothiophene-containing Hh pathway agonist, was shown to be able to bind directly to Smo and activate Shh-dependent pathway. SAG and similar compounds represent attractive molecules to be developed for treatment of disorders where stimulation of the generation and survival of new neural cells would be beneficial. Thus, it was demonstrated that small-molecule agonist of Smo has potential as a neuroprotective agent in neonates at risk for glucocorticoid-induced neonatal cerebellar injury. Moreover, hedgehog agonist therapy corrects structural and cognitive deficits in a Down syndrome mouse model.

6-amino-2-(butylamino)-9-((6-(2-(dimethylamino)ethoxy)pyridin-3-yl)methyl)-7,9-dihydro-8H-purin-8-one (DSR-6434) is a small molecule toll-like receptor (TLR)-7 agonist, which didn’t have direct antitumor activity, but enhanced efficacy of ionizing radiation therapy in a model of colorectal carcinoma.

77-LH-28-1 Oxalate is a salt of 77-LH-28-1. This drug is a potent, selective, bioavailable and brain-penetrant agonist of muscarinic acetylcholine receptor subtype 1. 77-LH-28-1 can increase network oscillations relevant to cognitive processing that would support the potential use of this mechanism in the treatment of cognitive impairment. 77-LH-28-1 exhibited U-shaped dose-effect functions in attenuating cocaine discrimination. 77-LH-28-1, can significantly enhance donepezil-induced gamma oscillations. These data support the notion that it should be possible to find a more efficacious AChE inhibitor or an adjunctive approach, to provide a better therapeutic intervention in Alzheimer's disease.

BMS-470539 2 HCL (BMS-470539) is a potent, specific MC1R ligand. The affinity of this molecule, as determined by [125I]NDP-MSH competition binding experiments, was in the nanomolar range (IC50 120 nM). BMS-470539 is a potent, full agonist of recombinant human MC-1R, stably expressed in CHO cells, with an EC50 of 16.8 nM and an intrinsic activity of 88% in a cAMP accumulation assay. BMS-470539 exhibits anti-inflammatory properties following ischemia-reperfusion in the vasculature. BMS-470539 inhibits leukocyte trafficking. In mice, BMS-470539 inhibits lipopolysaccharide (LPS)-induced systemic tumour necrosis factor (TNF) release and LPS-induced leucocyte migration into the lung.

TC OT 39 was developed as potent non-peptide oxytocin receptor partial agonist and V2 vasopressin receptor agonist. Also was a V1a vasopressin receptor antagonist.