Prodipine hydrochloride

Modify Date: 2024-01-10 14:17:22

Prodipine hydrochloride Structure
Prodipine hydrochloride structure
Common Name Prodipine hydrochloride
CAS Number 31314-39-3 Molecular Weight 315.88000
Density N/A Boiling Point N/A
Molecular Formula C20H26ClN Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Prodipine hydrochloride


Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.

 Names

Name 4,4-diphenyl-1-propan-2-ylpiperidine,hydrochloride
Synonym More Synonyms

 Prodipine hydrochloride Biological Activity

Description Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.
Related Catalog
Target

IC50: 4.5 μM (purified DPP IV), 30 μM (plasma DPP IV)[1]

In Vitro Prodipine, a diphenyl-phosphonate derivative selected from a group of slow-binding irreversible inhibitors of this enzyme. The IC50 values of Prodipine for purified and plasma DPP IV from the rabbit are 4.5 μM and 30 μM, respectively[1].
In Vivo Male rabbits weighing 3-4 kg receive a single intravenous injection with 10 mg Prodipine or saline. After 1 hr, plasma DPP IV activity has decreased to less than 20% of the preinjection value and remaines unchanged during a 24 hr observation period. A profound and long-lasting inhibition of plasma DPP IV activity is observed in the treated animals (1, 5 or 10 mg). It takes 5 to 8 days to reach half of the pretreatment DPP IV activity and generally more than 20 days for a complete recovery[1].
Kinase Assay Dipeptidyl peptidase IV activity is determined using the fluorogenic substrate Gly-Pro-4-methoxy-2-naphthylamide. Hydrolysis of L-Ala-4-methoxy-2-naphthylamide in 60 mM phosphate buffer pH 7.4 is chosen for the determination of aminopeptidase M activity. The intramolecularly quenched fluorogenic substrate Lys (2,4 dinitrophenyl)-Pro-Pro-NH-CH2-CH,-NH,-aminobenzoyl-2HCl is used to assay aminopeptidase P activity. Prolyl oligopeptidase (PO) is measured with N-benzyloxycarbonyl-Gly-Pro-7-amino-4-methylcoumarin. One unit of enzymatic activity is defined as the amount of enzyme catalyzing the formation of 1 μmol of assay product per minute under the conditions used[1].
Animal Admin Rabbits[1] Male New Zealand white rabbits (3-4 kg) are used. EXPERIMENT 1 The rabbits (n=1 for each condition) receive a single iv. injection of 10 mg Prodipine or saline. Blood samples are taken 5 min before injection and 30 min, 1 hr, 2 hr, and 24 hr after the treatment. EXPERIMENT 2 The rabbits (n=1 for each condition) receive a single i.v. bolus injection of saline or are treated with 1, 5, or 10 mg Prodipine (also in a single i.v. bolus) at time 0. The animals are kept under observation for 40 days. At several time points (-5 min, 4 hr, and at days 1, 2, 3, 6, 12, 21, and 40), blood samples are taken and body weight determined. Rabbits are killed with pentobarbital after termination of the observation period.
References

[1]. De Meester I, et al. In vivo inhibition of dipeptidyl peptidase IV activity by pro-pro-diphenyl-phosphonate (Prodipine). Biochem Pharmacol. 1997 Jul 1;54(1):173-9.

 Chemical & Physical Properties

Molecular Formula C20H26ClN
Molecular Weight 315.88000
Exact Mass 315.17500
PSA 3.24000
LogP 5.21680

 Synonyms

Prodipine hydrochloride
Piperidine,4,4-diphenyl-1-isopropyl-,hydrochloride
BY-101
ANTHEN
prodipin hydrochloride
UNII-89CCP8Z2PS