A tricyclic antidepressant; binds to SERT and NET (Kds = 68 and 29.5 nM

Doxepin (hydrochloride) – 1 g

Brand:
Cayman
CAS:
1229-29-4
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Doxepin is a tricyclic antidepressant that binds to the serotonin (5-HT) transporter (SERT) and norepinephrine transporter (NET; Kds = 68 and 29.5 nM, respectively).{22877} It is a histamine H1 receptor antagonist (Ki = 1.23 nM).{40358} Doxepin selectively binds to SERT and NET over the dopamine transporter (DAT; Kd = 12,100 nM) and inhibits histamine H1 over H2, H3, and H4 receptors (Kis = 170, 39,810, and 15,135 nM, respectively).{22877,40358} It also binds to the 5-HT2 receptor, as well as to muscarinic acetylcholine and α1-adrenergic receptors (α1-ARs; Kds = 27, 23, and 23.5 nM, respectively).{25803} Doxepin (10 mg/kg, i.p.) decreases allodynia and hyperalgesia in a mouse model of chronic constriction injury-induced neuropathic pain.{48874} It increases the distance traveled in the center of the open field test and reduces immobility time in the forced swim test in a mouse model of depression induced by chronic stress when administered orally at a dose of 15 mg/kg.{48875} Formulations containing doxepin have been used in the treatment of depression and insomnia.  

 

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A tricyclic antidepressant; binds to SERT and NET (Kds = 68 and 29.5 nM, respectively); a histamine H1 receptor antagonist (Ki = 1.23 nM); selectively binds to SERT and NET over DAT (Kd = 12,100 nM) and inhibits histamine H1 over H2, H3, and H4 receptors (Kis = 170, 39,810, and 15,135 nM, respectively); binds to the 5-HT2 receptor, as well as to muscarinic acetylcholine and α1-ARs (Kds = 27, 23, and 23.5 nM, respectively); decreases allodynia and hyperalgesia in a mouse model of chronic constriction injury-induced neuropathic pain at 10 mg/kg, i.p.; increases the distance traveled in the center of the open field test and reduces immobility time in the forced swim test in a mouse model of depression induced by chronic stress at 15 mg/kg

Formal name: 3-(dibenz[b,e]oxepin-11(6H)-ylidene)-N,N-dimethyl-1-propanamine, monohydrochloride

Synonyms: 

Molecular weight: 315.8

CAS: 1229-29-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Pain Research

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