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Originator

Rajsner, M.|Svater, E.|Metysova, J.|Protiva, M.

3

Pfizer

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Eli Lilly

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Dopamine transporter

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Muscarinic acetylcholine receptor M1

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Muscarinic acetylcholine receptor M2

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Muscarinic acetylcholine receptor M3

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Non-selective monoamine reuptake inhibitors

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DOTHIEPIN

W13O82Z7HL

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Muscarinic acetylcholine receptor M2

Norepinephrine transporter

Muscarinic acetylcholine receptor M4

Muscarinic acetylcholine receptor M1

Muscarinic acetylcholine receptor M3

Histamine H1 receptor

Serotonin transporter

Muscarinic acetylcholine receptor M5

Dopamine transporter

Serotonin transporter

Norepinephrine transporter

Conditions:

Major depressive disorder

Neuropathic pain

cis-Dosulepin is a stereoisomer of Dothiepin (trade name Prothiaden, Dothep, Thaden, and Dopress; Dosulepin (INN, BAN) a tricyclic antidepressant that is used in several European and South Asian countries, as well as Australia, South Africa, and New ...

Zealand. Dosulepin is used for the treatment of the major depressive disorder and neuropathic pain. Dosulepin is only Therapeutic Goods Administration and Medicines and Healthcare products Regulatory Agency approved for the treatment of the major depressive disorder. Dothiepin is not used in the United States. The central action of cis-dosulepin was compared with that of its antidepressant stereoisomer trans-dosulepin, cis-dosulepin exerted weaker anti-reserpine, anti-tetrabenazine, and 3H-5-HT (serotonin) uptake inhibiting actions than trans-dosulepin, but cis-dosulepin's inhibition of 3H-dopamine and 3H-norepinephrine uptake was slightly more potent than that of trans-dosulepin. On the other hand, cis-dosulepin exhibited extremely potent anticholinergic action in oxotremorine induced tremor, isolated ileum and the 3H-quinuclidinyl benzilate binding test. It also showed potent apomorphine enhancing the action and shortened the period of immobility in the forced swimming test in animals.

DOTHIEPIN, Z-

CZ377VWX9P

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Search for Structure

Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Muscarinic acetylcholine receptor M2

Norepinephrine transporter

Muscarinic acetylcholine receptor M4

Muscarinic acetylcholine receptor M1

Muscarinic acetylcholine receptor M3

Histamine H1 receptor

Serotonin transporter

Muscarinic acetylcholine receptor M5

Dopamine transporter

Serotonin transporter

Norepinephrine transporter

Conditions:

Major depressive disorder

Neuropathic pain

cis-Dosulepin is a stereoisomer of Dothiepin (trade name Prothiaden, Dothep, Thaden, and Dopress; Dosulepin (INN, BAN) a tricyclic antidepressant that is used in several European and South Asian countries, as well as Australia, South Africa, and New ...

Zealand. Dosulepin is used for the treatment of the major depressive disorder and neuropathic pain. Dosulepin is only Therapeutic Goods Administration and Medicines and Healthcare products Regulatory Agency approved for the treatment of the major depressive disorder. Dothiepin is not used in the United States. The central action of cis-dosulepin was compared with that of its antidepressant stereoisomer trans-dosulepin, cis-dosulepin exerted weaker anti-reserpine, anti-tetrabenazine, and 3H-5-HT (serotonin) uptake inhibiting actions than trans-dosulepin, but cis-dosulepin's inhibition of 3H-dopamine and 3H-norepinephrine uptake was slightly more potent than that of trans-dosulepin. On the other hand, cis-dosulepin exhibited extremely potent anticholinergic action in oxotremorine induced tremor, isolated ileum and the 3H-quinuclidinyl benzilate binding test. It also showed potent apomorphine enhancing the action and shortened the period of immobility in the forced swimming test in animals.

DOTHIEPIN HYDROCHLORIDE

3H0042311V

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Search for Structure

Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Muscarinic acetylcholine receptor M2

Norepinephrine transporter

Muscarinic acetylcholine receptor M4

Muscarinic acetylcholine receptor M1

Muscarinic acetylcholine receptor M3

Histamine H1 receptor

Serotonin transporter

Muscarinic acetylcholine receptor M5

Dopamine transporter

Serotonin transporter

Norepinephrine transporter

Conditions:

Major depressive disorder

Neuropathic pain

cis-Dosulepin is a stereoisomer of Dothiepin (trade name Prothiaden, Dothep, Thaden, and Dopress; Dosulepin (INN, BAN) a tricyclic antidepressant that is used in several European and South Asian countries, as well as Australia, South Africa, and New ...

Zealand. Dosulepin is used for the treatment of the major depressive disorder and neuropathic pain. Dosulepin is only Therapeutic Goods Administration and Medicines and Healthcare products Regulatory Agency approved for the treatment of the major depressive disorder. Dothiepin is not used in the United States. The central action of cis-dosulepin was compared with that of its antidepressant stereoisomer trans-dosulepin, cis-dosulepin exerted weaker anti-reserpine, anti-tetrabenazine, and 3H-5-HT (serotonin) uptake inhibiting actions than trans-dosulepin, but cis-dosulepin's inhibition of 3H-dopamine and 3H-norepinephrine uptake was slightly more potent than that of trans-dosulepin. On the other hand, cis-dosulepin exhibited extremely potent anticholinergic action in oxotremorine induced tremor, isolated ileum and the 3H-quinuclidinyl benzilate binding test. It also showed potent apomorphine enhancing the action and shortened the period of immobility in the forced swimming test in animals.

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