Tryptoline
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Tryptoline is an organic amine and the prototype for a group of compounds known collectively as tryptolines. All these compounds are competitive selective inhibitors of monoamine oxidase type A (MAO-A), 5-hydroxytryptamine being type A substrate. 5-hydroxytryptoline and 5-methoxytryptoline are the most active monoamine oxidase inhibitors with IC50 of 0.5 μM and 1.5 μM respectively, using 5-hydroxytryptamine as substrate. Tetrahydro-β-carbolines are also potent reuptake inhibitors of 5-hydroxytryptamine and epinephrine; a significantly greater uptake inhibitory selectivity being shown for 5-hydroxytryptamine than epinephrine. The comparison of the inhibition kinetics of tetrahydro-β-carbolines for 5-hydroxytryptamine and epinephrine uptake (with that of the platelet aggregation response to these amines) have shown that 5-hydroxymethtryptoline, methtryptoline, and tryptoline are poor inhibitors of uptake. In all respects 5-hydroxytryptoline and 5-methoxytryptoline showed greater pharmacological activity than the tryptoline and methtryptoline.
![Tryptoline; Noreleagnine; Tetrahydronorharman; 2,3,4,9-Tetrahydro-1H-β-carboline;1,2,3,4-Tetrahydro-β-carboline;1,2,3,4-Tetrahydro-9H-pyrido[3,4-b]indole;2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indole; (structural formula)](../../../upload/d/d6/Tryptoline.png)
Although the in vivo formation of tryptolines has been a matter of controversy, they have profound pharmacological activity. This is reflected in their actions described above.
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