Table 4.: The effect some glucagon receptor antagonists.

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]

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