dibenzepin hydrochloride
Clinical trial activity
0 trials · 0 clinical orgs · 0 marketing orgs
Mechanism of action
- Histamine H1 receptorANTAGONIST
HRH1 antagonist
Dibenzepin is a tricyclic antidepressant (TCA). It acts as a selective norepinephrine reuptake inhibitor (NRI). It is also a potent antihistamine (H1 receptor). The drug has weak or negligible effects on serotonin and dopamine reuptake. Unlike many other TCAs, dibenzepin has no antiadrenergic (¿1, ¿2), antiserotonergic (5-HT1A, 5-HT2A), or antidopaminergic effects and has few or no anticholinergic (mACh) effects.
Inhibitory effect on the uptake of noradrenaline (59 nM) by the perfused rabbit heart: 44.8 mM (ID50) Ki = 23 nM for H1 receptors.
- Norepinephrine transporterINHIBITOR
SLC6A2 inhibitor
Dibenzepin is a tricyclic antidepressant (TCA). It acts as a selective norepinephrine reuptake inhibitor (NRI). It is also a potent antihistamine (H1 receptor). The drug has weak or negligible effects on serotonin and dopamine reuptake. Unlike many other TCAs, dibenzepin has no antiadrenergic (¿1, ¿2), antiserotonergic (5-HT1A, 5-HT2A), or antidopaminergic effects and has few or no anticholinergic (mACh) effects.
Inhibitory effect on the uptake of noradrenaline (59 nM) by the perfused rabbit heart: 44.8 mM (ID50) Ki = 23 nM for H1 receptors.
Chemistry & pharmacology
SMILES
CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21- Mol. weight
- 295.39 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL1442422 ↗
- ChEMBLCHEMBL99486 ↗
- ChEMBLCHEMBL2104287 ↗
Also known as
- 11h-dibenzo(b,e)(1,4)diazepin-11-one, 10-(2-(dimethylamino)ethyl)-5,10-dihydro-5-methyl-
- dibenzepin
- dibenzepin
- dibenzepin
- dibenzepin
- dibenzepin
- dibenzepin
- dibenzepine
- dibenzepine hcl
- dibenzepine hydrochloride
- dibenzepin hcl
- dibenzepin hcl
- dibenzepin hcl
- dibenzepin hydrochloride
- dibenzepin hydrochloride
- dibenzepin hydrochloride
- dibenzepin hydrochloride
- dibenzepin hydrochloride
- hf-1927
- hf-1927
- noveril
- noveril
- noveril