Stereochemical Aspects of Psychotropic Drugs

Stereochemical and other geometric factors are significant in determining the type of psychotropic activity obtained. It appears that planar ring systems yield optimal neuroleptic activity. The tricyclic 6-6-6 system (i.e., all three rings contain six atoms) of the phenoth-iazines seems to prove this. However, compounds with total rigid planarity, as in a 6-5-6 system exemplified by carbazole and fluorene derivatives, are invariably inactive. It might be postulated that neuroleptic receptors are planar but have rather strict size requirements for binding.

Dopaminergic synapse Tyrosine

Dopaminergic Synapse

Figure 12-27. Model of central dopaminergic neuron (adapted from Cooper et al., 1991, with permission).

Figure 12-27. Model of central dopaminergic neuron (adapted from Cooper et al., 1991, with permission).

Carbazole derivative chch2ch2n chch2ch2n

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