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PD 173212

Names

[ CAS No. ]:
217171-01-2

[ Name ]:
PD 173212

[Synonym ]:
PD173212

Biological Activity

[Description]:

PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel
Research Areas >> Neurological Disease

[Target]

IC50: 36 nM (VSCC)[1]


[In Vitro]

PD173212 (PD 173212, 300 nM) potently blocks recombinant B-class (N-type) calcium channel currents 78±7.8%, with an IC50 of 74 nM, by whole-cell voltage-clamp techniques. PD 173212 possesses selectivity for non L-type Ca2+ channels versus neuronal Na+, K+, and L-type Ca2+ channels[1].

[In Vivo]

PD173212 (30 mg/kg, i.v.) shows moderate efficacy in preventing tonic seizures in the audiogenic seizure model[1].

[References]

[1]. Hu LY, et al. Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2151-6.


[Related Small Molecules]

Neomycin sulfate | Nifedipine | Acetylcholine chloride | Ionomycin | (S)-(-)-Bay K 8644 | Nimodipine | Mibefradil dihydrochloride | Levetiracetam | CDN 1163 | Dantrolene sodium | Thapsigargin | Flufenamic Acid | ABT 639 | Ranolazine dihydrochloride | Cromolyn (sodium)

Chemical & Physical Properties

[ Molecular Formula ]:
C38H53N3O3

[ Molecular Weight ]:
599.84600

[ Exact Mass ]:
599.40900

[ PSA ]:
70.67000

[ LogP ]:
7.83360

[ Storage condition ]:
2-8℃


Related Compounds

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