| Candidate ID: | R0405 |
| Source ID: | DB01104 |
| Source Type: | approved |
| Compound Type: |
small molecule
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| Compound Name: |
Sertraline
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| Synonyms: |
(+)-Sertraline; (1S-cis)-1,2,3,4-tetrahydro-4-(3,4-dichlorophenyl)-N-methyl-1-naphthalenamine; (1S,4S)-sertraline; cis-(+)-sertraline; Sertraline
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| Molecular Formula: |
C17H17Cl2N
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| SMILES: |
CN[C@H]1CC[C@@H](C2=CC(Cl)=C(Cl)C=C2)C2=CC=CC=C12
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| Structure: |
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| DrugBank Description: |
Sertraline is a popular antidepressant medication commonly known as a selective serotonin reuptake inhibitor (SSRI), and is similar to drugs such as and . Despite marked structural differences between compounds in this drug class, SSRIs exert similar pharmacological effects.
Several weeks of therapy with sertraline may be required before beneficial effects are noticed. Sertraline displays enhanced safety or tolerability than other classes of antidepressants, which frequently cause high levels of drowsiness, dizziness, blurred vision, and other undesirable effects.
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| CAS Number: |
79617-96-2
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| Molecular Weight: |
306.23
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| DrugBank Indication: |
Sertraline is indicated for the management of major depressive disorder (MDD), post-traumatic stress disorder (PTSD), obsessive-compulsive disorder (OCD), panic disorder (PD), premenstrual dysphoric disorder (PMDD), and social anxiety disorder (SAD). Common off-label uses for sertraline include the prevention of post stroke depression, generalized anxiety disorder (GAD), fibromyalgia, premature ejaculation, migraine prophylaxis, diabetic neuropathy, and neurocardiogenic syncope.
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| DrugBank Pharmacology: |
Sertraline improves or relieves the symptoms of depression, OCD, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, and premenstrual dysphoric disorder via the inhibition of serotonin reuptake. Clinical studies have shown that it improves cognition in depressed patients. It has less sedative, anticholinergic, and cardiovascular effects than the tricyclic antidepressant drugs because it does not exert significant anticholinergic, antihistamine, or adrenergic (alpha1, alpha2, beta) blocking activity. The onset of action and beneficial effects are usually noticed after 4-6 weeks, for reasons that are not fully understood and currently under investigation.
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| DrugBank MoA: |
Sertraline selectively inhibits the reuptake of serotonin (5-HT) at the presynaptic neuronal membrane, thereby increasing serotonergic activity. This results in an increased synaptic concentration of serotonin in the CNS, which leads to numerous functional changes associated with enhanced serotonergic neurotransmission. These changes are believed to be responsible for the antidepressant action and beneficial effects in obsessive-compulsive (and other anxiety related disorders). It has been hypothesized that obsessive-compulsive disorder, like depression, is also caused by the disregulation of serotonin.
In animal studies, chronic administration of sertraline results in down-regulation of brain norepinephrine receptors. Sertraline displays affinity for sigma-1 and 2 receptor binding sites, but binds with stronger affinity to sigma-1 binding sites. In vitro, sertraline shows little to no affinity for GABA, dopaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors. It exerts weak inhibitory actions on the neuronal uptake of norepinephrine and dopamine and exhibits no inhibitory effects on the monoamine oxidase enzyme.
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| Targets: |
Sodium-dependent serotonin transporter inhibitor&binder&downregulator; Sodium-dependent dopamine transporter inhibitor&binder; Sigma receptor inhibitor&binder; Sodium-dependent noradrenaline transporter inhibitor&downregulator; Equilibrative nucleoside transporter 4
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| Inclusion Criteria: |
Indication associated
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