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Primary Target

Plasmodium falciparum (isolate K1 / Thailand)

8

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

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Development Status

US Approved OTC

6

Other

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Possibly Marketed Outside US

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Approved

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Approval Year

1949

6

2015

1

Unknown

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Condition

Allergic rhinitis

6

Leishmaniasis

1

Malaria

1

Staphylococcus aureus infection

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Tuberculosis

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Treatment Modality

Primary

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Curative

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CNS Active

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Originator

Shering

6

Esterfield, T.H.|McDowell, J.C.

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Chemical

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CAS

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FDA UNII

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PUBCHEM

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EPA CompTox

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DRUG BANK

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ANTIHISTAMINES FOR SYSTEMIC USE

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ANTIHISTAMINES FOR SYSTEMIC USE

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ATC Level 4

Substituted alkylamines

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Salts, Hydrates, Esters, etc.

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Showing 1 - 8 of 8 results

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CHLORPHENIRAMINE

3U6IO1965U

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Status:

US Approved OTC

First approved in 1949

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Plasmodium falciparum (isolate K1 / Thailand)

Histamine H1 receptor

Sodium-dependent serotonin transporter

Sodium-dependent dopamine transporter

Conditions:

Allergic rhinitis

Chlorpheniramine is an antihistamine. Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Chlorpheniramine...

is used for relieving symptoms of sinus congestion, sinus pressure, runny nose, watery eyes, itching of the nose and throat, and sneezing due to upper respiratory infections (eg, colds), allergies, and hay fever. In addition to being a histamine H1 receptor (HRH1) antagonist, chlorphenamine has been shown to work as a serotonin-norepinephrine reuptake inhibitor or SNRI.

OLIVACINE

5WSL5LL2C3

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Plasmodium falciparum 3D7

Plasmodium falciparum (isolate K1 / Thailand)

TOTAROL

67NH2854WW

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Status:

Possibly Marketed Outside US

First approved in 2015

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Plasmodium falciparum (isolate K1 / Thailand)

Mycobacterium tuberculosis H37Rv

Cell division protein FtsZ

Leishmania donovani

Staphylococcus aureus

Conditions:

Staphylococcus aureus infection

Totarol is a meroterpene, and more precisely a terpenophenolic, a chemical compound that is part terpene and part natural phenol. It is a naturally produced diterpene that is bioactive as (+)-totarol. It was first isolated by McDowell and Esterfield ...

from the heartwood of Podocarpus totara, a yew tree found in New Zealand. Totarol showed good activity against Mycobacterium tuberculosis H(37)Rv (MIC of 73.7 uM). It was also most active against the isoniazid-, streptomycin-, and moxifloxacin-resistant variants (MIC of 38.4, 83.4 and 60 uM, respectively). Totarol demonstrated nematicidal and antifouling activities against Caenorhabditis elegans and Artemia salina, it inhibited Leishmania donovani promastigotes, showed good antimicrobial activity against effluxing strains of Staphylococcus aureus. Totarol inhibits bacterial proliferation by targeting FtsZ and it may be useful as a lead compound to develop an effective antitubercular drug.

CHLORPHENIRAMINE TANNATE

72JT935YTT

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Status:

US Approved OTC

First approved in 1949

Class (Stereo):

CHEMICAL (EPIMERIC)

Targets:

Plasmodium falciparum (isolate K1 / Thailand)

Histamine H1 receptor

Sodium-dependent serotonin transporter

Sodium-dependent dopamine transporter

Conditions:

Allergic rhinitis

Chlorpheniramine is an antihistamine. Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Chlorpheniramine...

is used for relieving symptoms of sinus congestion, sinus pressure, runny nose, watery eyes, itching of the nose and throat, and sneezing due to upper respiratory infections (eg, colds), allergies, and hay fever. In addition to being a histamine H1 receptor (HRH1) antagonist, chlorphenamine has been shown to work as a serotonin-norepinephrine reuptake inhibitor or SNRI.

CHLORPHENIRAMINE GLUCONATE

79YPK3BAIT

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Status:

US Approved OTC

First approved in 1949

Class (Stereo):

CHEMICAL (EPIMERIC)

Targets:

Plasmodium falciparum (isolate K1 / Thailand)

Histamine H1 receptor

Sodium-dependent serotonin transporter

Sodium-dependent dopamine transporter

Conditions:

Allergic rhinitis

Chlorpheniramine is an antihistamine. Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Chlorpheniramine...

is used for relieving symptoms of sinus congestion, sinus pressure, runny nose, watery eyes, itching of the nose and throat, and sneezing due to upper respiratory infections (eg, colds), allergies, and hay fever. In addition to being a histamine H1 receptor (HRH1) antagonist, chlorphenamine has been shown to work as a serotonin-norepinephrine reuptake inhibitor or SNRI.

CHLORPHENIRAMINE HYDROCHLORIDE

5S6VUP419V

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Status:

US Approved OTC

First approved in 1949

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Plasmodium falciparum (isolate K1 / Thailand)

Histamine H1 receptor

Sodium-dependent serotonin transporter

Sodium-dependent dopamine transporter

Conditions:

Allergic rhinitis

Chlorpheniramine is an antihistamine. Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Chlorpheniramine...

is used for relieving symptoms of sinus congestion, sinus pressure, runny nose, watery eyes, itching of the nose and throat, and sneezing due to upper respiratory infections (eg, colds), allergies, and hay fever. In addition to being a histamine H1 receptor (HRH1) antagonist, chlorphenamine has been shown to work as a serotonin-norepinephrine reuptake inhibitor or SNRI.

CHLORPHENIRAMINE MALEATE

V1Q0O9OJ9Z

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Status:

US Approved OTC

First approved in 1949

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Plasmodium falciparum (isolate K1 / Thailand)

Histamine H1 receptor

Sodium-dependent serotonin transporter

Sodium-dependent dopamine transporter

Conditions:

Allergic rhinitis

Chlorpheniramine is an antihistamine. Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Chlorpheniramine...

is used for relieving symptoms of sinus congestion, sinus pressure, runny nose, watery eyes, itching of the nose and throat, and sneezing due to upper respiratory infections (eg, colds), allergies, and hay fever. In addition to being a histamine H1 receptor (HRH1) antagonist, chlorphenamine has been shown to work as a serotonin-norepinephrine reuptake inhibitor or SNRI.

CHLORPHENIRAMINE STEARATE

5J341Q2P1E

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Status:

US Approved OTC

First approved in 1949

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Plasmodium falciparum (isolate K1 / Thailand)

Histamine H1 receptor

Sodium-dependent serotonin transporter

Sodium-dependent dopamine transporter

Conditions:

Allergic rhinitis

Chlorpheniramine is an antihistamine. Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Chlorpheniramine...

is used for relieving symptoms of sinus congestion, sinus pressure, runny nose, watery eyes, itching of the nose and throat, and sneezing due to upper respiratory infections (eg, colds), allergies, and hay fever. In addition to being a histamine H1 receptor (HRH1) antagonist, chlorphenamine has been shown to work as a serotonin-norepinephrine reuptake inhibitor or SNRI.

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