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Primary Target

GABA transporter 1

11

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

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Development Status

Other

8

US Approved Rx

3

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Highest Phase

Approved

3

Phase I

2

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Approval Year

Unknown

8

1997

3

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Condition

Anxiety

3

Cocaine-related disorders

3

Partial seizures

3

Epilepsy

2

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Treatment Modality

Primary

5

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CNS Activity

CNS Active

5

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Originator

Braestrup, C.|Nielsen, E.B.|Wolffbrandt, K.H.|Andersen, K.E.|Knutsen, L.J. S.|Sonnewald, U.

3

Warner-Lambert

2

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Substance Class

Chemical

11

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Code System

CAS

11

FDA UNII

11

PUBCHEM

11

EPA CompTox

8

WIKIPEDIA

5

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ATC Level 1

NERVOUS SYSTEM

1

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ATC Level 2

ANTIEPILEPTICS

1

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ATC Level 3

ANTIEPILEPTICS

1

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ATC Level 4

Fatty acid derivatives

1

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Substance Form

Salts, Hydrates, Esters, etc.

6

Principal Form

5

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Showing 1 - 10 of 11 results

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TIAGABINE

Z80I64HMNP

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Status:

US Approved Rx (2021)

First approved in 1997

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Betaine transporter

GABA transporter 3

GABA transporter 1

Conditions:

Partial seizures

Cocaine-related disorders

Tiagabine (trade name Gabitril) is an anticonvulsant medication used in the treatment of Partial Seizures. The precise mechanism by which Tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to enha...

nce the activity of gamma-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Tiagabine binds to recognition sites associated with the GABA uptake carrier. It is thought that, by this action, Tiagabine blocks GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells. Tiagabine is approved by U.S. Food and Drug Administration (FDA) as an adjunctive treatment for partial seizures in individuals of age 12 and up. It may also be prescribed off-label by physicians to treat anxiety disorders and panic disorder as well as neuropathic pain (including fibromyalgia). For anxiety and neuropathic pain, tiagabine is used primarily to augment other treatments. Tiagabine may be used alongside selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, or benzodiazepines for anxiety, or antidepressants, gabapentin, other anticonvulsants, or opioids for neuropathic pain. The most common side effect of tiagabine is dizziness. Other side effects that have been observed with a rate of statistical significance relative to placebo include asthenia, somnolence, nervousness, memory impairment, tremor, headache, diarrhea, and depression.

1-(4,4-Diphenylbut-3-en-1-yl)piperidine-3-carboxylic acid

HKU93AZP6B

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Status:

Other

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

GABA transporter 1

NIPECOTIC ACID

1U1QTN40SY

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Status:

Other

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

GABA transporter 3

GABA transporter 1

GABA transporter 2

GUVACINE

41538P325K

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

GABA transporter 2

GABA transporter 1

GABA transporter 3

Betaine transporter

CI-966

MGZ24EM59L

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

GABA transporter 1

Conditions:

CI-966 is a GABA reuptake inhibitor, acting as an indirect and nonselective GABA agonist by blocking GABA transporter protein GAT-1. CI-966 was investigated in phase I clinical study for treatment of epilepsy, but its development was discontinued due...

to physical and mental disturbances at high doses.

TIAGABINE HYDROCHLORIDE MONOHYDRATE

OXB00SKC7R

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Status:

US Approved Rx (2021)

First approved in 1997

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Betaine transporter

GABA transporter 3

GABA transporter 1

Conditions:

Partial seizures

Cocaine-related disorders

Tiagabine (trade name Gabitril) is an anticonvulsant medication used in the treatment of Partial Seizures. The precise mechanism by which Tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to enha...

nce the activity of gamma-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Tiagabine binds to recognition sites associated with the GABA uptake carrier. It is thought that, by this action, Tiagabine blocks GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells. Tiagabine is approved by U.S. Food and Drug Administration (FDA) as an adjunctive treatment for partial seizures in individuals of age 12 and up. It may also be prescribed off-label by physicians to treat anxiety disorders and panic disorder as well as neuropathic pain (including fibromyalgia). For anxiety and neuropathic pain, tiagabine is used primarily to augment other treatments. Tiagabine may be used alongside selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, or benzodiazepines for anxiety, or antidepressants, gabapentin, other anticonvulsants, or opioids for neuropathic pain. The most common side effect of tiagabine is dizziness. Other side effects that have been observed with a rate of statistical significance relative to placebo include asthenia, somnolence, nervousness, memory impairment, tremor, headache, diarrhea, and depression.

TIAGABINE HYDROCHLORIDE

DQH6T6D8OY

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Status:

US Approved Rx (2021)

First approved in 1997

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Betaine transporter

GABA transporter 3

GABA transporter 1

Conditions:

Partial seizures

Cocaine-related disorders

Tiagabine (trade name Gabitril) is an anticonvulsant medication used in the treatment of Partial Seizures. The precise mechanism by which Tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to enha...

nce the activity of gamma-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Tiagabine binds to recognition sites associated with the GABA uptake carrier. It is thought that, by this action, Tiagabine blocks GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells. Tiagabine is approved by U.S. Food and Drug Administration (FDA) as an adjunctive treatment for partial seizures in individuals of age 12 and up. It may also be prescribed off-label by physicians to treat anxiety disorders and panic disorder as well as neuropathic pain (including fibromyalgia). For anxiety and neuropathic pain, tiagabine is used primarily to augment other treatments. Tiagabine may be used alongside selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, or benzodiazepines for anxiety, or antidepressants, gabapentin, other anticonvulsants, or opioids for neuropathic pain. The most common side effect of tiagabine is dizziness. Other side effects that have been observed with a rate of statistical significance relative to placebo include asthenia, somnolence, nervousness, memory impairment, tremor, headache, diarrhea, and depression.

1-(4,4-Diphenylbut-3-en-1-yl)piperidine-3-carboxylic acid hydrochloride

933TH75A2D

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Status:

Other

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

GABA transporter 1

Nipecotinic acid hydrochloride

4A2FH6F5EG

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Status:

Other

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

GABA transporter 3

GABA transporter 1

GABA transporter 2

NIPECOTIC ACID, SODIUM SALT

4FFB4R29DS

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Status:

Other

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

GABA transporter 3

GABA transporter 1

GABA transporter 2

Showing 1 - 10 of 11 results

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