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Jouveinal Laboratories

10

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Eli Lilly

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Calcium-activated potassium channel subunit alpha-1

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Opioid receptors; mu/kappa/delta

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Synthetic anticholinergics, esters with tertiary amino group

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Showing 1 - 10 of 10 results

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FEDOTOZINE

F45VW2087W

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Kappa-type opioid receptor

Conditions:

Irritable bowel syndrome

Fedotozine [(1R)-1-phenyl-1-[(3,4,5-trimethoxy) benzyloxymethyl]-N,N- dimethyl-n-propylamine, (2S,3S-tartrate], derived from the arylacetamide series, is an opioid drug which acts as a selective agonist for kappa(1a)-opioid receptor. Pharmacological ...

studies have shown that fedotozine exerts a peripheral antinociceptive action, comparable with that of other kappa-agonists. Results of Phase III trials of fedotozine against irritable bowel syndrome and dyspepsia have ultimately been disappointing and was lack of efficacy in subsequent studies.

TRIMEBUTINE

QZ1OJ92E5R

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Vascular cell adhesion protein 1

Voltage-gated L-type calcium channel

Opioid receptors; mu/kappa/delta

Calcium-activated potassium channel subunit alpha-1

Conditions:

Irritable bowel syndrome

Spinal cord injury

Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta o...

piate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.

FEDOTOZINE TARTRATE

3YJ57F78WM

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Kappa-type opioid receptor

Conditions:

Irritable bowel syndrome

Fedotozine [(1R)-1-phenyl-1-[(3,4,5-trimethoxy) benzyloxymethyl]-N,N- dimethyl-n-propylamine, (2S,3S-tartrate], derived from the arylacetamide series, is an opioid drug which acts as a selective agonist for kappa(1a)-opioid receptor. Pharmacological ...

studies have shown that fedotozine exerts a peripheral antinociceptive action, comparable with that of other kappa-agonists. Results of Phase III trials of fedotozine against irritable bowel syndrome and dyspepsia have ultimately been disappointing and was lack of efficacy in subsequent studies.

TRIMEBUTINE MALEATE, (+)-

DKM38HXX5A

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (UNKNOWN)

Targets:

Vascular cell adhesion protein 1

Voltage-gated L-type calcium channel

Opioid receptors; mu/kappa/delta

Calcium-activated potassium channel subunit alpha-1

Conditions:

Irritable bowel syndrome

Spinal cord injury

Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta o...

piate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.

TRIMEBUTINE TOSYLATE

M62HUT52HM

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Vascular cell adhesion protein 1

Voltage-gated L-type calcium channel

Opioid receptors; mu/kappa/delta

Calcium-activated potassium channel subunit alpha-1

Conditions:

Irritable bowel syndrome

Spinal cord injury

Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta o...

piate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.

TRIMEBUTINE 3-THIOCARBAMOYLBENZENESULFONATE

5O1CF9IS48

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Vascular cell adhesion protein 1

Voltage-gated L-type calcium channel

Opioid receptors; mu/kappa/delta

Calcium-activated potassium channel subunit alpha-1

Conditions:

Irritable bowel syndrome

Spinal cord injury

Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta o...

piate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.

TRIMEBUTINE MALEATE, (-)-

H4XZJ9GX7T

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (UNKNOWN)

Targets:

Vascular cell adhesion protein 1

Voltage-gated L-type calcium channel

Opioid receptors; mu/kappa/delta

Calcium-activated potassium channel subunit alpha-1

Conditions:

Irritable bowel syndrome

Spinal cord injury

Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta o...

piate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.

TRIMEBUTINE, (-)-

U4UUZ24TRB

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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (UNKNOWN)

Targets:

Vascular cell adhesion protein 1

Voltage-gated L-type calcium channel

Opioid receptors; mu/kappa/delta

Calcium-activated potassium channel subunit alpha-1

Conditions:

Irritable bowel syndrome

Spinal cord injury

Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta o...

piate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.

TRIMEBUTINE, (+)-

9RKX7S7WFY

Export Data
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Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (UNKNOWN)

Targets:

Vascular cell adhesion protein 1

Voltage-gated L-type calcium channel

Opioid receptors; mu/kappa/delta

Calcium-activated potassium channel subunit alpha-1

Conditions:

Irritable bowel syndrome

Spinal cord injury

Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta o...

piate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.

TRIMEBUTINE MALEATE

2A051GM4YM

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Search for Structure

Status:

Possibly Marketed Outside US

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Vascular cell adhesion protein 1

Voltage-gated L-type calcium channel

Opioid receptors; mu/kappa/delta

Calcium-activated potassium channel subunit alpha-1

Conditions:

Irritable bowel syndrome

Spinal cord injury

Trimebutine [3,4,5-trimethoxybenzoic acid 2-(dimethylamino)-2-phenylbutylester] is a noncompetitive spasmolytic agent. The actions of trimebutine on the gastrointestinal tract are mediated via (i) an agonist effect on peripheral mu, kappa and delta o...

piate receptors and (ii) release of gastrointestinal peptides such as motilin and modulation of the release of other peptides, including vasoactive intestinal peptide, gastrin and glucagon. Trimebutine attenuated colonic motility mainly through the inhibition of L-type Ca(2+) channels at higher concentrations, whereas, at lower concentrations, it depolarized membrane potentials by reducing BK(ca) currents, resulting in the enhancement of the muscle contractions.Trimebutine accelerates gastric emptying, induces premature phase III of the migrating motor complex in the intestine and modulates the contractile activity of the colon. It is indicated for the treatment and relief of symptoms associated with the irritable bowel syndrome (spastic colon); and in postoperative paralytic ileus in order to accelerate the resumption of the intestinal transit following abdominal surgery.

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