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Development Status

US Approved Allergenic Extract

4

Investigational

3

Possibly Marketed Outside US

1

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Primary Target

Histamine H1 receptor

4

Histamine H2 receptor

4

Histamine H3 receptor

4

Histamine H4 receptor

4

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Highest Phase

Approved

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Approval Year

1939

4

Unknown

3

2020

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Condition

Allergenic skin

4

Gastric acid secretory

4

Multiple sclerosis

4

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Treatment Modality

Diagnostic

4

Primary

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CNS Activity

CNS Active

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Originator

Dale, H.H.|Laidlaw, P.P.

4

GlaxoSmithKline

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Substance Class

Chemical

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Code System

CAS

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FDA UNII

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PUBCHEM

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DAILYMED

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DRUG BANK

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ATC Level 1

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

2

VARIOUS

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ATC Level 2

IMMUNOSTIMULANTS

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DIAGNOSTIC AGENTS

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ATC Level 3

IMMUNOSTIMULANTS

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OTHER DIAGNOSTIC AGENTS

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ATC Level 4

Other immunostimulants

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Tests for gastric secretion

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Substance Form

Salts, Hydrates, Esters, etc.

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Principal Form

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Showing 1 - 8 of 8 results

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GSK-364735

SXN0KXT60S

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

GlaxoSmithKline was developing GSK-364735 as a human immunodeficiency virus (HIV) integrase inhibitor. The inhibition of viral DNA integration takes place by interacting at the two-metal binding site within the catalytic center of HIV integrase. GSK-...

364735 was successfully studied at Phase II in HIV-infected patients; however, adverse liver effects of GSK364735 were recently observed in a long-term preclinical safety study in the monkey and preclude further development of the compound.

HISTAMINE

820484N8I3

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Status:

US Approved Allergenic Extract (1995)

First approved in 1939

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Histamine H1 receptor

Histamine H2 receptor

Histamine H3 receptor

Histamine H4 receptor

Conditions:

Multiple sclerosis

Gastric acid secretory

Allergenic skin

Histamine is a depressor amine derived by enzymatic decarboxylation of histidine. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and a centrally acting neurotransmitter. Phosphate salt of jis...

tamine was used as a diagnostic aid for evaluation of gastric acid secretory function. In addition, this compound is used as a positive control in evaluation of allergenic (immediate hypersensitivity or "Type I") skin testing. In addition, histamine is being studied for treatment of multiple sclerosis. It was approved, that histamine physiological functions are mediated by four 7-transmembrane G protein-coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. The receptors display molecular heterogeneity and constitutive activity. H1R antagonists are long known antiallergic and sedating drugs, whereas the H2R led to the development of H2R-antagonists that revolutionized stomach ulcer treatment. The H3R is an auto receptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons. The H4R occurs on immuncompetent cells and the development of anti-inflammatory drugs is anticipated.

2-AMINO-1,3-PROPANEDIOL

IC94L30J8M

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Status:

Possibly Marketed Outside US

First approved in 2020

Class (Stereo):

CHEMICAL (ACHIRAL)

GSK-364735 SODIUM

G8X28PC11Y

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

GlaxoSmithKline was developing GSK-364735 as a human immunodeficiency virus (HIV) integrase inhibitor. The inhibition of viral DNA integration takes place by interacting at the two-metal binding site within the catalytic center of HIV integrase. GSK-...

364735 was successfully studied at Phase II in HIV-infected patients; however, adverse liver effects of GSK364735 were recently observed in a long-term preclinical safety study in the monkey and preclude further development of the compound.

GSK-364735 POTASSIUM

324268A537

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

GlaxoSmithKline was developing GSK-364735 as a human immunodeficiency virus (HIV) integrase inhibitor. The inhibition of viral DNA integration takes place by interacting at the two-metal binding site within the catalytic center of HIV integrase. GSK-...

364735 was successfully studied at Phase II in HIV-infected patients; however, adverse liver effects of GSK364735 were recently observed in a long-term preclinical safety study in the monkey and preclude further development of the compound.

HISTAMINE MONOHYDROCHLORIDE

F9I23AC4PQ

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Status:

US Approved Allergenic Extract (1995)

First approved in 1939

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Histamine H1 receptor

Histamine H2 receptor

Histamine H3 receptor

Histamine H4 receptor

Conditions:

Multiple sclerosis

Gastric acid secretory

Allergenic skin

Histamine is a depressor amine derived by enzymatic decarboxylation of histidine. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and a centrally acting neurotransmitter. Phosphate salt of jis...

tamine was used as a diagnostic aid for evaluation of gastric acid secretory function. In addition, this compound is used as a positive control in evaluation of allergenic (immediate hypersensitivity or "Type I") skin testing. In addition, histamine is being studied for treatment of multiple sclerosis. It was approved, that histamine physiological functions are mediated by four 7-transmembrane G protein-coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. The receptors display molecular heterogeneity and constitutive activity. H1R antagonists are long known antiallergic and sedating drugs, whereas the H2R led to the development of H2R-antagonists that revolutionized stomach ulcer treatment. The H3R is an auto receptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons. The H4R occurs on immuncompetent cells and the development of anti-inflammatory drugs is anticipated.

HISTAMINE DIHYDROCHLORIDE

3POA0Q644U

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Status:

US Approved Allergenic Extract (1995)

First approved in 1939

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Histamine H1 receptor

Histamine H2 receptor

Histamine H3 receptor

Histamine H4 receptor

Conditions:

Multiple sclerosis

Gastric acid secretory

Allergenic skin

Histamine is a depressor amine derived by enzymatic decarboxylation of histidine. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and a centrally acting neurotransmitter. Phosphate salt of jis...

tamine was used as a diagnostic aid for evaluation of gastric acid secretory function. In addition, this compound is used as a positive control in evaluation of allergenic (immediate hypersensitivity or "Type I") skin testing. In addition, histamine is being studied for treatment of multiple sclerosis. It was approved, that histamine physiological functions are mediated by four 7-transmembrane G protein-coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. The receptors display molecular heterogeneity and constitutive activity. H1R antagonists are long known antiallergic and sedating drugs, whereas the H2R led to the development of H2R-antagonists that revolutionized stomach ulcer treatment. The H3R is an auto receptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons. The H4R occurs on immuncompetent cells and the development of anti-inflammatory drugs is anticipated.

HISTAMINE PHOSPHATE

QWB37T4WZZ

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Status:

US Approved Allergenic Extract (1995)

First approved in 1939

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Histamine H1 receptor

Histamine H2 receptor

Histamine H3 receptor

Histamine H4 receptor

Conditions:

Multiple sclerosis

Gastric acid secretory

Allergenic skin

Histamine is a depressor amine derived by enzymatic decarboxylation of histidine. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and a centrally acting neurotransmitter. Phosphate salt of jis...

tamine was used as a diagnostic aid for evaluation of gastric acid secretory function. In addition, this compound is used as a positive control in evaluation of allergenic (immediate hypersensitivity or "Type I") skin testing. In addition, histamine is being studied for treatment of multiple sclerosis. It was approved, that histamine physiological functions are mediated by four 7-transmembrane G protein-coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. The receptors display molecular heterogeneity and constitutive activity. H1R antagonists are long known antiallergic and sedating drugs, whereas the H2R led to the development of H2R-antagonists that revolutionized stomach ulcer treatment. The H3R is an auto receptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons. The H4R occurs on immuncompetent cells and the development of anti-inflammatory drugs is anticipated.

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