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Details

Stereochemistry ABSOLUTE
Molecular Formula C38H53N3O3
Molecular Weight 599.8457
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PD-173212

SMILES

CC(C)C[C@H](N(C)CC1=CC=C(C=C1)C(C)(C)C)C(=O)N[C@@H](CC2=CC=C(OCC3=CC=CC=C3)C=C2)C(=O)NC(C)(C)C

InChI

InChIKey=GCDHMGROXQUFNR-HEVIKAOCSA-N
InChI=1S/C38H53N3O3/c1-27(2)23-34(41(9)25-29-15-19-31(20-16-29)37(3,4)5)36(43)39-33(35(42)40-38(6,7)8)24-28-17-21-32(22-18-28)44-26-30-13-11-10-12-14-30/h10-22,27,33-34H,23-26H2,1-9H3,(H,39,43)(H,40,42)/t33-,34-/m0/s1

HIDE SMILES / InChI

Molecular Formula C38H53N3O3
Molecular Weight 599.8457
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

PD 173212 is a potent, selective N-type voltage-gated Ca2+ channel blocker (IC50 = 36 nM), it possesses selectivity for non L-type Ca ÷2 channels versus neuronal Na ÷, K ÷, and L-type Ca ÷2 channels. PD 173212 demonstrated potent in vitro activity in the IMR-32 assay as well as in electrophysiology, and it was efficacious in the audiogenic seizure mouse model.

CNS Activity

Curator's Comment: PD 173212 showed moderate efficacy in preventing tonic seizures in the mouse audiogenic seizure model

Originator

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
36.0 nM [IC50]
Conditions

Conditions

PubMed

PubMed

TitleDatePubMed
Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers.
1999 Jul 5
Patents

Sample Use Guides

Mice: 30 mg/kg, IV
Route of Administration: Intravenous
PD 173212 potently blocked recombinant B-class (N-type) calcium channel currents 78 -+ 7.8% at 300 nM, with an IC50 of 74 nM using whole-cell voltage-clamp techniques.
Substance Class Chemical
Created
by admin
on Sat Dec 16 09:29:54 GMT 2023
Edited
by admin
on Sat Dec 16 09:29:54 GMT 2023
Record UNII
Z7UUP5FPKC
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PD-173212
Common Name English
L-TYROSINAMIDE, N-((4-(1,1-DIMETHYLETHYL)PHENYL)METHYL)-N-METHYL-L-LEUCYL-N-(1,1-DIMETHYLETHYL)-O-(PHENYLMETHYL)-
Systematic Name English
Code System Code Type Description
CAS
217171-01-2
Created by admin on Sat Dec 16 09:29:55 GMT 2023 , Edited by admin on Sat Dec 16 09:29:55 GMT 2023
PRIMARY
FDA UNII
Z7UUP5FPKC
Created by admin on Sat Dec 16 09:29:55 GMT 2023 , Edited by admin on Sat Dec 16 09:29:55 GMT 2023
PRIMARY
EPA CompTox
DTXSID10432752
Created by admin on Sat Dec 16 09:29:55 GMT 2023 , Edited by admin on Sat Dec 16 09:29:55 GMT 2023
PRIMARY
PUBCHEM
9916734
Created by admin on Sat Dec 16 09:29:55 GMT 2023 , Edited by admin on Sat Dec 16 09:29:55 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY