CID 657299

DescriptionClomipramine is a tricyclic antidepressant, the 3-chlorinated derivative of imipramine . Like imipramine, clomipramine potently inhibits serotonin and norepinephrine reuptake (Kis = 7.4 and 96 nM, respectively). It also is an antagonist at histamine, muscarinic acetylcholine, α1-adrenergic, and dopamine receptors (Kds = 31, 37, 38, and 190 nM for H1, M1, α1, and D2, respectively).

UsesPotent, selective 5-HT uptake blocker

UsesSerotonin reuptake inhibitor. Antidepressant; antiobsessional agent

Usesanti-depressant, serotonin uptake inhibitor

General DescriptionClomipramine (Anafranil) is up to 50 times as potentas imipramine in some bioassays. This does not implyclinical superiority, but it might be informative about tricyclicand, possibly, other reuptake inhibitors. The chloro replacingthe H-substituent could increase potency by increasingdistribution to the CNS, but it is unlikely that this wouldgive the potency magnitude seen. It might be conjecturedthat an H-bond between the protonated amino group (as invivo) and the unshared electrons of the chloro substituent might stabilize a β-arylamine–like shape and give moreefficient competition for the transporter. The drug is anantidepressant. It is used in obsessive–compulsive disorder,an anxiety disorder that may have an element of depression.