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Desipramine

Name: Desipramine
Description: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors. (PubChem) Pharmacology: Desipramine, a tertiary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. Desipramine is used to treat depression, pain of neuropathic origin, attentiondeficit hyperactivity disorder, functional enuresis in children, panic and phobic disorder, and to manage some eating disorders. Desipramine inhibits the re-uptake of noradrenaline at the noradrenergic nerve endings and the re-uptake of serotonin (5-hydroxy tryptamine) at the serotoninergic nerve endings in the central nervous system. These two effects are considered to be the likely base of the antidepressant effect of Desipramine. The drug also has a strong anticholinergic effect and serves as an antagonist on a1 and H1 receptors. Mechanism of action: Desipramine is a tricyclic antidepressant that selectively blocks reuptake of norepinephrine (noradrenaline) from the neural synapse. It also appears to impair serotonin transport. Desipramine also possesses minor anticholinergic activity, through its affinity to muscarinic receptors. Evidence also suggests that Desiprmaine binds to and down regulates histamine and beta adrenergic receptors. Tricyclic drugs are believed to act by restoring normal levels of neurotransmitters by blocking the re-uptake of these substances from the synapse in the central nervous system. Drug type: Approved. Small Molecule. Drug category: Adrenergic Uptake Inhibitors. Antidepressants. Antidepressive Agents, Tricyclic. Enzyme Inhibitors. Norepinephrine-Reuptake Inhibitors
Synonym(s): DMI, Demethylimipramine, Desimipramine, Desimpramine, Desipramin, Desipramine Hcl, Desmethylimipramine, Dezipramine, Dimethylimipramine, Methylaminopropyliminodibenzyl, Monodemethylimipramine, Norimipramine, Norpramine, Pentofran, Pertofran, Pertrofane, Sertofran
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB01151
*Id: CHEBI:47781
Related to: Cholinergic system, Muscarinic acetylcholine receptor M1, Beta-1 adrenergic receptor, Histamine H1 receptor, Sodium-dependent noradrenaline transporter, Muscarinic acetylcholine receptor M2, Beta-2 adrenergic receptor, Sodium-dependent serotonin transporter, Sphingomyelin phosphodiesterase
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Facts about DesipramineRDF feed
Commenttaken from DrugBank
CurationStatusuncurated  +
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB01151  +
DefinitionA tricyclic dibenzazepine compound that po A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors. (PubChem) Pharmacology: Desipramine, a tertiary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. Desipramine is used to treat depression, pain of neuropathic origin, attentiondeficit hyperactivity disorder, functional enuresis in children, panic and phobic disorder, and to manage some eating disorders. Desipramine inhibits the re-uptake of noradrenaline at the noradrenergic nerve endings and the re-uptake of serotonin (5-hydroxy tryptamine) at the serotoninergic nerve endings in the central nervous system. These two effects are considered to be the likely base of the antidepressant effect of Desipramine. The drug also has a strong anticholinergic effect and serves as an antagonist on a1 and H1 receptors. Mechanism of action: Desipramine is a tricyclic antidepressant that selectively blocks reuptake of norepinephrine (noradrenaline) from the neural synapse. It also appears to impair serotonin transport. Desipramine also possesses minor anticholinergic activity, through its affinity to muscarinic receptors. Evidence also suggests that Desiprmaine binds to and down regulates histamine and beta adrenergic receptors. Tricyclic drugs are believed to act by restoring normal levels of neurotransmitters by blocking the re-uptake of these substances from the synapse in the central nervous system. Drug type: Approved. Small Molecule. Drug category: Adrenergic Uptake Inhibitors. Antidepressants. Antidepressive Agents, Tricyclic. Enzyme Inhibitors. Norepinephrine-Reuptake Inhibitors bitors. Norepinephrine-Reuptake Inhibitors
Has roleDrug  +
IdCHEBI:47781  +
LabelDesipramine  +
ModifiedDate31 July 2014  +
RelatedToCholinergic system  +, Muscarinic acetylcholine receptor M1  +, Beta-1 adrenergic receptor  +, Histamine H1 receptor  +, Sodium-dependent noradrenaline transporter  +, Muscarinic acetylcholine receptor M2  +, Beta-2 adrenergic receptor  +, Sodium-dependent serotonin transporter  +, and Sphingomyelin phosphodiesterase  +
SuperCategoryMolecular entity  +
SynonymDMI  +, Demethylimipramine  +, Desimipramine  +, Desimpramine  +, Desipramin  +, Desipramine Hcl  +, Desmethylimipramine  +, Dezipramine  +, Dimethylimipramine  +, Methylaminopropyliminodibenzyl  +, Monodemethylimipramine  +, Norimipramine  +, Norpramine  +, Pentofran  +, Pertofran  +, Pertrofane  +, and Sertofran  +