Tarazepide

Modify Date: 2024-01-09 20:50:33

Tarazepide Structure
Tarazepide structure
Common Name Tarazepide
CAS Number 141374-81-4 Molecular Weight 448.516
Density 1.3±0.1 g/cm3 Boiling Point 788.0±60.0 °C at 760 mmHg
Molecular Formula C28H24N4O2 Melting Point N/A
MSDS N/A Flash Point 430.4±32.9 °C

 Use of Tarazepide


Tarazepide is a potent and specific CCK-A receptor antagonist.

 Names

Name Tarazepide
Synonym More Synonyms

 Tarazepide Biological Activity

Description Tarazepide is a potent and specific CCK-A receptor antagonist.
Related Catalog
Target

CCK-A receptor[1]

In Vivo Tarazepide decreases duodenal electric activity, reduces interdigestive pancreatic secretion, especially protein; reduces cephalic and early postprandial (milk) induced secretion of bicarbonate and protein.Pancreatic protein secretion to intravenous CCK-8 was little affected by atropine, but was significantly reduced by Tarazepide±Atropine; in contrast, protein secretion to intraduodenal CCK-8 was abolished by Tarazepide or atropine[1]. Leptin is administered to the animals at doses of 0.1, 1.0 or 10.0 μg/kg i.d. Tarazepide (2.5 mg/kg, i.d.), a CCK(1) receptor antagonist, is given to the rats prior to the application of leptin. CCK plasma level is measured by radioimmunoassay (RIA) following administration of leptin to the rats. Intraduodenal administration of leptin (1.0 or 10.0 microg/kg) to the fasted rats significantly and dose-dependently increases pancreatic protein and amylase outputs. Pancreatic secretory responses to leptin were totally abolished by prior capsaicin deactivation of sensory nerves or by pretreatment of the rats with Tarazepide[2].
Animal Admin Calve[1] The 5 to 7-day-old Friesian male calves (42.0±1.5 kg body weight) are used. The study is made on four calves. After recording 2 to 3 preprandial (interdigestive) MMC/PPS cycles, Tarazepide suspension (0.05, 0.5 and 5.0 mg/kg body weight), or vehicle alone (1% methylcellulose) is infused intraduodenally (i.d.).
References

[1]. Zabielski R, et al. Effects of intraduodenal administration of tarazepide on pancreatic secretion and duodenal EMG in neonatal calves. Regul Pept. 1998 Nov 30;78(1-3):113-23.

[2]. Nawrot-Porabka K, et al. Leptin is able to stimulate pancreatic enzyme secretion via activation of duodeno-pancreatic reflex and CCK release. J Physiol Pharmacol. 2004 Jul;55 Suppl 2:47-57.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 788.0±60.0 °C at 760 mmHg
Molecular Formula C28H24N4O2
Molecular Weight 448.516
Flash Point 430.4±32.9 °C
Exact Mass 448.189911
LogP 3.64
Vapour Pressure 0.0±2.7 mmHg at 25°C
Index of Refraction 1.713
Storage condition 2-8℃

 Synonyms

(-)-N-[(S)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinoline-2-carboxamide
RK2972YZ2U
tarazepide
4H-Pyrrolo[3,2,1-ij]quinoline-2-carboxamide, N-[(3S)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-5,6-dihydro-
(-)-N-((S)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)-5,6-dihydro-4H-pyrrolo(3,2,1-ij)quinoline-2-carboxamide
N-[(3S)-1-Methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinoline-2-carboxamide