cinepazide
Cinepazide or cinepazide maleate is a vasodilator used in China for the treatment of cardiovascular and cerebrovascular diseases, and peripheral vascular diseases. It appears to work by potentiating A2 adenosine receptors. — Wikipedia
Clinical trial activity
3 trials · 3 clinical orgs · 0 marketing orgs
Earliest trial started Jul 1, 2008 (NCT01831011)
Timeline
2000s
- Jan 1, 2008
Earliest Phase 2 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Voltage-gated calcium channelINHIBITOR
Voltage-gated calcium channel inhibitor
Cinepazide maleate (CM) is a calcium-channel blocker with vasodilator action that can increase blood flow to the brain and peripheral organs, such as cardiac muscle, skeletal muscle, and kidneys. CM is known to potentiate the effects of adenosine by preventing both its degradation by deaminase and its accumulation by atrial tissue. CM was found to ameliorate diabetes exacerbated chronic cerebral hypoperfusion induced cognitive impairment by inhibiting astrocyte activation, preventing damage to cholinergic neurons, and reducing BACE1 expression in the hippocampus.
- Voltage-dependent T-type calcium channel subunit alpha-1H (CACNA1H) ↗
- Voltage-dependent calcium channel subunit alpha-2/delta-1 (CACNA2D1) ↗
- Voltage-dependent L-type calcium channel subunit alpha-1C (CACNA1C) ↗
- Voltage-dependent calcium channel subunit alpha-2/delta-3 (CACNA2D3) ↗
- Voltage-dependent L-type calcium channel subunit alpha-1S (CACNA1S) ↗
- Voltage-dependent calcium channel subunit alpha-2/delta-2 (CACNA2D2) ↗
- Voltage-dependent L-type calcium channel subunit alpha-1D (CACNA1D) ↗
- Voltage-dependent P/Q-type calcium channel subunit alpha-1A (CACNA1A) ↗
- Voltage-dependent N-type calcium channel subunit alpha-1B (CACNA1B) ↗
- Voltage-dependent T-type calcium channel subunit alpha-1G (CACNA1G) ↗
- Voltage-dependent calcium channel subunit alpha-2/delta-4 (CACNA2D4) ↗
- Voltage-dependent T-type calcium channel subunit alpha-1I (CACNA1I) ↗
- Voltage-dependent L-type calcium channel subunit alpha-1F (CACNA1F) ↗
- Voltage-dependent R-type calcium channel subunit alpha-1E (CACNA1E) ↗
- Voltage-dependent L-type calcium channel subunit beta-3 (CACNB3) ↗
- Voltage-dependent calcium channel gamma-7 subunit (CACNG7) ↗
- Voltage-dependent calcium channel gamma-5 subunit (CACNG5) ↗
- Voltage-dependent calcium channel gamma-2 subunit (CACNG2) ↗
- Voltage-dependent L-type calcium channel subunit beta-4 (CACNB4) ↗
- Voltage-dependent L-type calcium channel subunit beta-2 (CACNB2) ↗
- Voltage-dependent L-type calcium channel subunit beta-1 (CACNB1) ↗
- Voltage-dependent calcium channel gamma-4 subunit (CACNG4) ↗
- Voltage-dependent calcium channel gamma-8 subunit (CACNG8) ↗
- Voltage-dependent calcium channel gamma-3 subunit (CACNG3) ↗
- Voltage-dependent calcium channel gamma-6 subunit (CACNG6) ↗
- Voltage-dependent calcium channel gamma-1 subunit (CACNG1) ↗
- Voltage-gated T-type calcium channel alpha-1H subunit
- Voltage-gated calcium channel alpha2/delta subunit 1
- Voltage-gated L-type calcium channel alpha-1C subunit
- Voltage-gated N-type calcium channel alpha-1B subunit
- Voltage-gated L-type calcium channel alpha-1S subunit
- Voltage-gated L-type calcium channel alpha-1D subunit
- Voltage-gated calcium channel alpha2/delta subunit 2
- Voltage-gated P/Q-type calcium channel alpha-1A subunit
- Voltage-gated T-type calcium channel alpha-1G subunit
- Voltage-gated T-type calcium channel alpha-1I subunit
- Voltage-dependent R-type calcium channel subunit alpha-1E
- Voltage-gated L-type calcium channel
- Voltage-gated T-type calcium channel
- Voltage-dependent L-type calcium channel subunit beta-2
- Voltage-dependent N-type calcium channel subunit alpha-1B/Voltage-dependent calcium channel subunit alpha-2/delta-1/Voltage-dependent L-type calcium channel subunit beta-3
- Voltage-dependent L-type calcium channel alpha1C/alpha2delta/beta1b
- Voltage-dependent P/Q-type calcium channel alpha1A/alpha2delta/beta1b
- N-type calcium channel alpha-1b/alpha2delta-1/beta-1b
- L-type calcium channel alpha-1c/beta-2/alpha2delta-1
- Voltage-dependent L-type calcium channel subunit beta-3
- Voltage-dependent L-type calcium channel subunit alpha-1C/L-type calcium channel subunit beta-3/calcium channel subunit alpha-2/delta-1
- Unspecified targetOTHER
Unknown
Cinepazide maleate (CM) is a calcium-channel blocker with vasodilator action that can increase blood flow to the brain and peripheral organs, such as cardiac muscle, skeletal muscle, and kidneys. CM is known to potentiate the effects of adenosine by preventing both its degradation by deaminase and its accumulation by atrial tissue. CM was found to ameliorate diabetes exacerbated chronic cerebral hypoperfusion induced cognitive impairment by inhibiting astrocyte activation, preventing damage to cholinergic neurons, and reducing BACE1 expression in the hippocampus.
- Unspecified targetUnknown
Unknown
Cinepazide¿ maleate¿ (CM)¿ is¿ a¿ calcium-channel¿ blocker¿with¿ vasodilator¿ action¿ that¿ can¿ increase¿ blood¿ flow¿ to¿ the¿brain¿ and¿ peripheral¿ organs,¿ such¿ as¿ cardiac¿ muscle,¿ skeletal¿ muscle,¿ and¿ kidneys.¿CM¿is¿ known¿to¿ potentiate¿the¿ effects¿ of adenosine by preventing both its degradation by deaminase and its accumulation by atrial tissue. CM¿was¿found¿to¿ameliorate diabetes exacerbated ¿chronic cerebral hypoperfusion induced cognitive impairment ¿by¿inhibiting¿astrocyte¿ activation, preventing damage to cholinergic neurons, and reducing¿ BACE1¿ expression¿ in¿ the¿ hippocampus.
Chemistry & pharmacology
SMILES
COc1cc(/C=C/C(=O)N2CCN(CC(=O)N3CCCC3)CC2)cc(OC)c1OC- Mol. weight
- 417.51 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaCinepazide ↗
- ChEMBLCHEMBL1874750 ↗
Also known as
- 1-((1-pyrrolidinylcarbonyl)methyl)-4-(3,4,5-trimethoxycinnamoyl)piperazine
- 1-((1-pyrrolidynylcarbonyl)methyl)-4-(3,4,5-trimethoxycinnamoyl)piperazine maleate
- 67350-md
- 67350-md
- cinepazide
- cinepazide
- cinepazide
- cinepazide
- cinepazide
- cinepazide
- cinepazide
- cinepazide
- cinepazide maleate
- cinepazide maleate
- cinepazide maleate
- cinepazide maleate
- cinepazide maleate
- md-67350 [as maleate]
- md-67350 [as maleate]
- vasodistal
- vasodistal
- vasodistal
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04951232 | N/A | Jul 4, 2016 | Chinese Academy of Medical Sciences, Peking University |
| NCT01851759 | Phase 2 | Oct 1, 2013 | People's Liberation Army of China |
| NCT01831011 | Phase 2 | Jul 1, 2008 | People's Liberation Army of China |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| People's Liberation Army of China | Government | 2 | 2 | 1 | 2008 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 1 | 0 | 1 | 2016 |
| Peking University | Academic/Hospital | 1 | 1 | 1 | 2016 |