| Drug | Compound | Efficacy | Dosage | Adverse effect | Clinical phase | Ref |
|---|---|---|---|---|---|---|
| Spiro-urea | Compound 15 | (a)Reduced glucose excursion after glucagon challenge ; (b) blocks glucagon effect | 10 and 30 mg/kg (i.m.) | thirst, dry mouth, nausea, polyuria | Pre-clinical | [53, 67] |
| Benzimidazole | Compound 36 | Reduced glucose levels in diabetes; suppressed glucagon-induced glucose increase in animals | 10 and 3 mg/kg in rhesus monkeys |
Reduced human liver microsome stability | Pre-clinical | [56, 68] |
| Skyrin | Fungal bisanthro-quinone | Antagonized functional glucagon (uncouples glucagon receptor from adenylate cyclase in hepatocyte plasmalemma | 30 micromol/l inhibited glucagon-stimulated cAMP production and glucose output | Suppressed Na+, K+-activated ATPase; Inhibits microsomal activity in rat brain | Not in clinical trial | [51, 69] |