Disease relevance of CR-605

• Controlled study of the effects of tiropramide on biliary dyskinesia [1].
• The toxicity of the chiralic forms of tiropramide does not differ significantly from that of the racemic substance [2].

Psychiatry related information on CR-605

• These results confirm the antispastic synchronizing effect of tiropramide on the motor activity of the gall bladder and the sphincter of Oddi and indicate that it should be the drug of choice for treatment of motor disorders of the biliary tract [1].

High impact information on CR-605

• A simple sample preparation with HPLC-UV method for estimation of tiropramide from plasma: Application to bioequivalence study [3].
• An improved chromatographic condition to resolve racemic tiropramide on the CSP was examined by changing the flow rate, composition, and kind of mobile phases [4].
• When tiropramide was added during the sustained phase of the K+ (60 mM)-contracture, IC50 values of tiropramide for the contraction and the increased fluorescence were 1.9 x 10(-5) M and 16.4 x 10(-5) M, respectively [5].
• Mechanism of smooth muscle relaxation by tiropramide [6].
• Tiropramide inhibited phosphodiesterase activity in rabbit colon homogenates in a range of doses about ten times that producing relaxation, cAMP content enhancement and increase Ca2+ binding to sarcoplasmic reticulum [6].

Chemical compound and disease context of CR-605

• A controlled trial was carried out in patients with biliary dyskinesia to compare the effects of the new calmodulin-independent and antispastic drug tiropramide with those of imecromone [1].

Biological context of CR-605

• Tiropramide inhibited the Ca2+ (3 mM)-induced contractions of the isolated urinary bladder depolarized in a Ca(2+)-free medium, and the IC50 value was 3.3 x 10(-6) M [5].
• Pharmacokinetics of tiropramide after single doses in man [7].
• The absolute bioavailability of total radioactivity calculated on the ratio between the p.o. and i.v. AUC was 0.67, that of tiropramide was 0.23 [8].
• It appears that after p.o. administration the biotransformation of tiropramide is more intense than after i.v. administration [8].
• The difference between the absolute bioavailability of total radioactivity and that of tiropramide is probably due to a first-pass effect and a more intense biotransformation of the substance after p.o. administration [8].

Anatomical context of CR-605

• Tiropramide had small effects on vascular smooth muscles and showed very small calcium channel blocking activity [9].

Associations of CR-605 with other chemical compounds

• (+/-) Tiropramide hydrochloride, its D and L optical isomers and some of its metabolites were characterized in a number of in vitro pharmacological tests [9].
• In subjects with delayed filling of the gall bladder during cholecystography, tiropramide but not imecromone was able to normalize the condition [1].

Gene context of CR-605

• The analytical method of antispasmodic agent tiropramide ((+/-)alpha-(benzoylamino)-4-[2-(diethylamino)ethoxy]-N,N-dipropylbenzenepropanamide hydrochloride) was developed by gas chromatography/nitrogen-phosphorus detector (GC/NPD) in human plasma [10].
• Two formulations of tiropramide ((+/-)alpha-(benzoylamino)-4-[2-(diethylamino) ethoxy]-N,N-dipropyl-benzenepropanamide hydrochloride, CAS 55837-29-1), an antispasmodic agent, were orally administered to 16 healthy volunteers by the Latin cross-over design with the purpose of evaluating bioequivalence and pharmacokinetics of tiropramide [11].

Analytical, diagnostic and therapeutic context of CR-605

• A sensitive, selective and simple gas chromatography coupled to mass spectrometry (GC/MS) was developed for quantification of tiropramide in human plasma using internal standard (ISD, (+/-) alpha-benzoylamino-4-[2-(dimethylamino) ethoxy]-N,N-dipropylbenzenepropanamide) [12].
• Enantioseparation of tiropramide by HPLC [4].
• A rapid and sensitive column-switching semi-micro high-performance liquid chromatography method was developed for the direct analysis of tiropramide in human plasma [13].
• Plasma samples obtained from human volunteers were analyzed for the determination of tiropramide concentration by using this method [10].
• Two kinds of tiropramide tablets were orally administered to volunteers by Latin square crossover design, and blood was withdrawn as designed schedule [10].

References