Гидрохлорид Кломипрамин

Описание

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

Химические свойства

Off-White Solid

Использование

Serotonin reuptake inhibitor. Antidepressant; antiobsessional agent

Определение

ChEBI: A hydrochloride resulting from the reaction of equimolar amounts of clomipramine and hydrogen chloride. One of the more sedating tricyclic antidepressants, it is used for the treatment of depression as well as obsessive-compulsive disorder and phobias.

Общее описание

Clomipramine (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.

Биологическая активность

Potent, selective 5-HT uptake blocker. Antidepressant. Binds to the human 5-HT transporter with a K i of 0.05 nmol/l. Also available as part of the Serotonin Uptake Inhibitor Tocriset™ .