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Details

Stereochemistry ACHIRAL
Molecular Formula C11H16N4O.ClH
Molecular Weight 256.732
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LIDAMIDINE HYDROCHLORIDE

SMILES

Cl.CNC(=N)NC(=O)NC1=C(C)C=CC=C1C

InChI

InChIKey=INMBONSHXVMDSX-UHFFFAOYSA-N
InChI=1S/C11H16N4O.ClH/c1-7-5-4-6-8(2)9(7)14-11(16)15-10(12)13-3;/h4-6H,1-3H3,(H4,12,13,14,15,16);1H

HIDE SMILES / InChI

Description

Lidamidine, also known as WHR-1142A and Lidaral, is an alpha2-adrenergic receptor agonist that inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle contraction. Lidamidine hydrochloride is used to treat diarrhoea and other gastrointestinal disorders. Lidamidine’s intestinal antisecretory effects are mediated through the activation of peripheral alpha-2 adrenoceptors. Lidamidine crosses the blood brain barrier poorly and is therefore devoid of the centrally mediated alpha-2 effects that have limited the use of other alpha-2 adrenoceptor agonists in the intestinal tract.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Lidarral

Doses

OverviewOther

Other InhibitorOther SubstrateOther Inducer







Drug as perpetrator​

Drug as victim

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
Lidamidine HCL (4 mg) or placebo was taken orally t.i.d. with food. Lidamidine decreased the augmented mechanical response to food, reduced rectal sensitivity, and relieved symptoms of patients with irritable bowel syndrome.
Route of Administration: Oral
In Vitro Use Guide
The effects of clonidine and lidamidine on ion transport in the intestine of the rabbit were determined. In the ileum both clonidine (10(-6) M) and lidamidine (10(-3) M) (a) decreased the short circuit current (-1.9 +/- 0.3 and -2.0 +/- 0.4 muEq/h . cm2, respectively) and potential difference; (b) increased net sodium absorption (2.0 +/- 0.6 and 1.8 +/- 0.4 muEq/h . cm2) and chloride absorption (3.4 +/- 0.5 and 3.4 +/- 0.6 muEq/h . cm2); and (c) increased tissue conductance (8.7 +/- 1.7 and 10.0 +/- 1.6 mmho/cm2).