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US Approved Rx

5

US Approved OTC

4

Other

1

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Primary Target

Serotonin 1b (5-HT1b) receptor

5

Serotonin 1d (5-HT1d) receptor

5

Adenosine A1 receptor

4

Adenosine A2a receptor

4

Adenosine A2b receptor

4

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Highest Phase

Approved

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Approval Year

1921

4

2001

3

1998

2

Unknown

1

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Condition

Migraine

6

Apnea of prematurity

4

Atopic dermatitis

4

Drowsiness

4

Migraine with aura

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Treatment Modality

Primary

9

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CNS Activity

CNS Active

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Originator

SmithKline Beecham

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GlaxoSmithKline

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PUBCHEM

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EPA CompTox

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ANALGESICS

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DIAGNOSTIC AGENTS

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PSYCHOANALEPTICS

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ATC Level 3

ANTIMIGRAINE PREPARATIONS

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OTHER DIAGNOSTIC AGENTS

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PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS

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ATC Level 4

Selective serotonin (5HT1) agonists

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Tests for gastric secretion

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Xanthine derivatives

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Salts, Hydrates, Esters, etc.

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Frovatriptan

H82Q2D5WA7

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Status:

US Approved Rx (2018)

First approved in 2001

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Serotonin 1a (5-HT1a) receptor

Serotonin 1b (5-HT1b) receptor

Serotonin 1d (5-HT1d) receptor

Serotonin 1b (5-HT1b) receptor

Serotonin 1d (5-HT1d) receptor

Conditions:

Migraine without aura

Migraine with aura

Frovatriptan succinate (trade name Frova) is a selective 5-hydroxytryptamine1 (5-HT1B/1D) receptor subtype agonist, and is used for the treatment of migraine attacks with or without aura in adults. Frovatriptan has no significant effects on GABAA me...

diated channel activity and has no significant affinity for benzodiazepine binding sites. Frovatriptan is believed to act on extracerebral, intracranial arteries and to inhibit excessive dilation of these vessels in migraine. Serious but rare cardiac events have been reported in patients with risk factors predictive of coronary artery disease (CAD). These include coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia and ventricular fibrillation.

NARATRIPTAN

QX3KXL1ZA2

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Status:

US Approved Rx (2012)

First approved in 1998

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Serotonin 1b (5-HT1b) receptor

Serotonin 1d (5-HT1d) receptor

Conditions:

Naratriptan (trade names include Amerge and Naramig) is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches.Naratriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptor...

s. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonist. Naratriptan has only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Naratriptan also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Naratriptan in humans.Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.

CAFFEINE

3G6A5W338E

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Status:

US Approved OTC

First marketed in 1921

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Adenosine A2a receptor

Adenosine A2b receptor

Phosphodiesterase 1

Adenosine A1 receptor

Conditions:

Atopic dermatitis

Apnea of prematurity

Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic a...

nd anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.

ZOLMITRIPTAN, (R)-

F3YOE57701

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Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

FROVATRIPTAN SUCCINATE ANHYDROUS

36K05YF32G

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Status:

US Approved Rx (2018)

First approved in 2001

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Serotonin 1a (5-HT1a) receptor

Serotonin 1b (5-HT1b) receptor

Serotonin 1d (5-HT1d) receptor

Serotonin 1b (5-HT1b) receptor

Serotonin 1d (5-HT1d) receptor

Conditions:

Migraine without aura

Migraine with aura

Frovatriptan succinate (trade name Frova) is a selective 5-hydroxytryptamine1 (5-HT1B/1D) receptor subtype agonist, and is used for the treatment of migraine attacks with or without aura in adults. Frovatriptan has no significant effects on GABAA me...

diated channel activity and has no significant affinity for benzodiazepine binding sites. Frovatriptan is believed to act on extracerebral, intracranial arteries and to inhibit excessive dilation of these vessels in migraine. Serious but rare cardiac events have been reported in patients with risk factors predictive of coronary artery disease (CAD). These include coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia and ventricular fibrillation.

Frovatriptan Succinate

D28J6W18HY

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Status:

US Approved Rx (2018)

First approved in 2001

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Serotonin 1a (5-HT1a) receptor

Serotonin 1b (5-HT1b) receptor

Serotonin 1d (5-HT1d) receptor

Serotonin 1b (5-HT1b) receptor

Serotonin 1d (5-HT1d) receptor

Conditions:

Migraine without aura

Migraine with aura

Frovatriptan succinate (trade name Frova) is a selective 5-hydroxytryptamine1 (5-HT1B/1D) receptor subtype agonist, and is used for the treatment of migraine attacks with or without aura in adults. Frovatriptan has no significant effects on GABAA me...

diated channel activity and has no significant affinity for benzodiazepine binding sites. Frovatriptan is believed to act on extracerebral, intracranial arteries and to inhibit excessive dilation of these vessels in migraine. Serious but rare cardiac events have been reported in patients with risk factors predictive of coronary artery disease (CAD). These include coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia and ventricular fibrillation.

NARATRIPTAN HYDROCHLORIDE

10X8X4P12Z

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Status:

US Approved Rx (2012)

First approved in 1998

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Serotonin 1b (5-HT1b) receptor

Serotonin 1d (5-HT1d) receptor

Conditions:

Naratriptan (trade names include Amerge and Naramig) is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches.Naratriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptor...

s. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonist. Naratriptan has only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Naratriptan also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Naratriptan in humans.Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.

caffeine sodium iodide

7DU9VK8U6A

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Status:

US Approved OTC

First marketed in 1921

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Adenosine A2a receptor

Adenosine A2b receptor

Phosphodiesterase 1

Adenosine A1 receptor

Conditions:

Atopic dermatitis

Apnea of prematurity

Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic a...

nd anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.

CAFFEINE MONOHYDRATE

9T65I06326

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Status:

US Approved OTC

First marketed in 1921

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Adenosine A2a receptor

Adenosine A2b receptor

Phosphodiesterase 1

Adenosine A1 receptor

Conditions:

Atopic dermatitis

Apnea of prematurity

Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic a...

nd anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.

CAFFEINE CITRATE

U26EO4675Q

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Status:

US Approved OTC

First marketed in 1921

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Adenosine A2a receptor

Adenosine A2b receptor

Phosphodiesterase 1

Adenosine A1 receptor

Conditions:

Atopic dermatitis

Apnea of prematurity

Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic a...

nd anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.

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