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
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
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10465535
Curator's Comment: PD 173212 showed moderate efficacy in preventing tonic seizures in the mouse audiogenic seizure model
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10406647 | https://www.ncbi.nlm.nih.gov/pubmed/10465535
Curator's Comment: # Pfizer (Parke-Davis Pharmaceutical)
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4478 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10465535 |
36.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10465535
Mice: 30 mg/kg, IV
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10465535
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
Edited
Sat Dec 16 09:29:54 GMT 2023
by
admin
on
Sat Dec 16 09:29:54 GMT 2023
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Record UNII |
Z7UUP5FPKC
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Record Status |
Validated (UNII)
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Record Version |
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