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US Approved Rx

10

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Primary Target

Muscarinic acetylcholine receptor M3

7

Muscarinic acetylcholine receptor M2

5

Phosphodiesterase 5A

3

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Highest Phase

Approved

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Approval Year

1998

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2004

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Overactive bladder

7

Erectile dysfunction

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Pulmonary arterial hypertension

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Treatment Modality

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Curative

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Palliative

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CNS Penetrant

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CNS Active

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Pfizer

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PUBCHEM

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CHEBI

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GENITO URINARY SYSTEM AND SEX HORMONES

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UROLOGICALS

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ATC Level 3

OTHER UROLOGICALS, INCL. ANTISPASMODICS

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ATC Level 4

Urinary antispasmodics

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Drugs used in erectile dysfunction

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Showing 1 - 10 of 10 results

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DARIFENACIN

APG9819VLM

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Status:

US Approved Rx (2016)

First approved in 2004

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Muscarinic acetylcholine receptor M3

Conditions:

Overactive bladder

Darifenacin is a selective muscarinic receptor M3 antagonist which was approved by FDA for the treatment of overactive bladder.

SILDENAFIL

3M7OB98Y7H

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Status:

US Approved Rx (2014)

First approved in 1998

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Phosphodiesterase 5A

Conditions:

Erectile dysfunction

Pulmonary arterial hypertension

Sildenafil (Viagra, Revatio) is a PDE5 inhibitor which was approved by FDA for the treatment of erectile disfunction and adults with pulmonary arterial hypertension. Upon administration sildenafil inhibits PDE5 and results in elevated level of cyclic...

guanosine monophosphate and smooth muscle relaxation.

TOLTERODINE

WHE7A56U7K

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Status:

US Approved Rx (2021)

First approved in 1998

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Muscarinic acetylcholine receptor M3

Muscarinic acetylcholine receptor M2

Conditions:

Overactive bladder

Tolterodine is competitive muscarinic receptors M3 and M2 antagonist. It was sold under trade names detrol for the treatment of overactive bladder with symptoms of urge urinary incontinence. Both urinary bladder contraction and salivation are mediate...

d via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity and affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine at 1 and 5 hours were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure. These findings are consistent with an antimuscarinic action on the lower urinary tract.

DARIFENACIN HYDROBROMIDE

CR02EYQ8GV

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Status:

US Approved Rx (2016)

First approved in 2004

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Muscarinic acetylcholine receptor M3

Conditions:

Overactive bladder

Darifenacin is a selective muscarinic receptor M3 antagonist which was approved by FDA for the treatment of overactive bladder.

(S)-TOLTERODINE

UWD7V7S6JT

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Status:

US Approved Rx (2021)

First approved in 1998

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Muscarinic acetylcholine receptor M3

Muscarinic acetylcholine receptor M2

Conditions:

Overactive bladder

Tolterodine is competitive muscarinic receptors M3 and M2 antagonist. It was sold under trade names detrol for the treatment of overactive bladder with symptoms of urge urinary incontinence. Both urinary bladder contraction and salivation are mediate...

d via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity and affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine at 1 and 5 hours were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure. These findings are consistent with an antimuscarinic action on the lower urinary tract.

TOLTERODINE FUMARATE

HH7RXJ4PW1

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Status:

US Approved Rx (2021)

First approved in 1998

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Muscarinic acetylcholine receptor M3

Muscarinic acetylcholine receptor M2

Conditions:

Overactive bladder

Tolterodine is competitive muscarinic receptors M3 and M2 antagonist. It was sold under trade names detrol for the treatment of overactive bladder with symptoms of urge urinary incontinence. Both urinary bladder contraction and salivation are mediate...

d via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity and affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine at 1 and 5 hours were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure. These findings are consistent with an antimuscarinic action on the lower urinary tract.

TOLTERODINE HYDROCHLORIDE

75I47Y48S7

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Status:

US Approved Rx (2021)

First approved in 1998

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Muscarinic acetylcholine receptor M3

Muscarinic acetylcholine receptor M2

Conditions:

Overactive bladder

Tolterodine is competitive muscarinic receptors M3 and M2 antagonist. It was sold under trade names detrol for the treatment of overactive bladder with symptoms of urge urinary incontinence. Both urinary bladder contraction and salivation are mediate...

d via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity and affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine at 1 and 5 hours were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure. These findings are consistent with an antimuscarinic action on the lower urinary tract.

SILDENAFIL NITRATE

8B699ZY1CH

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Status:

US Approved Rx (2014)

First approved in 1998

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Phosphodiesterase 5A

Conditions:

Erectile dysfunction

Pulmonary arterial hypertension

Sildenafil (Viagra, Revatio) is a PDE5 inhibitor which was approved by FDA for the treatment of erectile disfunction and adults with pulmonary arterial hypertension. Upon administration sildenafil inhibits PDE5 and results in elevated level of cyclic...

guanosine monophosphate and smooth muscle relaxation.

SILDENAFIL CITRATE

BW9B0ZE037

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Status:

US Approved Rx (2014)

First approved in 1998

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Phosphodiesterase 5A

Conditions:

Erectile dysfunction

Pulmonary arterial hypertension

Sildenafil (Viagra, Revatio) is a PDE5 inhibitor which was approved by FDA for the treatment of erectile disfunction and adults with pulmonary arterial hypertension. Upon administration sildenafil inhibits PDE5 and results in elevated level of cyclic...

guanosine monophosphate and smooth muscle relaxation.

TOLTERODINE TARTRATE

5T619TQR3R

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Status:

US Approved Rx (2021)

First approved in 1998

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Muscarinic acetylcholine receptor M3

Muscarinic acetylcholine receptor M2

Conditions:

Overactive bladder

Tolterodine is competitive muscarinic receptors M3 and M2 antagonist. It was sold under trade names detrol for the treatment of overactive bladder with symptoms of urge urinary incontinence. Both urinary bladder contraction and salivation are mediate...

d via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity and affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine at 1 and 5 hours were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure. These findings are consistent with an antimuscarinic action on the lower urinary tract.

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