Darodipine Explained

Darodipine is an experimental calcium channel blocker that based on animal models may reduce neuronal cytoskeletal alterations during aging and in neurodegenerative disorders. Studies performed on rats have shown darodipine to have an effect on brain serotonergic systems. Darodipine increased the 5-HIAA/5-HT ratio within various parts of the brain.^[1] Darodipine has also been shown to impair memory and learning processes on mice.^[2]

The longterm effect of darodipine was tested in the rats and it shows that there is no significant change in their body and brain weight values but, there is a significant change in their alkaline phosphate reactive capillary profile values. Alkaline phosphate enzymes plays an important role in the functioning of the cerebral capillary activities.^[3] The effect of darodipine on plasma concentration was also tested on a group of healthy male human volunteers. The result showed that darodipine resulted in the change in heart rate and diastolic blood pressure which is related to the plasma concentration.^[4]

Darodipine (50–500 nM), the sensitivity of DMPO‐COO.− adduct decreased by more than that of the DMPO‐OH adduct and the concentration-dependent drop in signal intensity. It has additional preventive effects, because of its calcium antagonistics, against free-radical mediated electrophysiological alterations; it is likely because of the trapping of such radical molecules.

See also

• Isradipine, a structural isomer of darodipine

Further reading

• Matucci R, Ottaviani MF, Barbieri M, Cerbai E, Mugelli A . Protective effect of darodipine, a calcium antagonist, on rat cardiomyocytes against oxygen radical-mediated injury . British Journal of Pharmacology . 122 . 7 . 1353–60 . December 1997 . 9421282 . 1565083 . 10.1038/sj.bjp.0701525 .

Notes and References

1. Gaggi R, Dall'Olio R, Roncada P, Gianni AM . Effects of isradipine and darodipine on serotonergic system of the rat brain . Pharmacology, Biochemistry, and Behavior . 51 . 2–3 . 183–7 . June–July 1995 . 7545305 . 10.1016/0091-3057(94)00389-Z . 6704491 .
2. Lamberti C, Bartolini A, Ghelardini C, Giotti A, Malmberg-Aiello P . Dec 1994. Effects of the calcium-channel blockers darodipine and nimodipine on amnesia induced by three different hypoxic methods. Pharmacological Research. 30. 4. 359. 10.1016/1043-6618(94)80030-8.
3. Amenta F, Ferrante F, Mancini M, Sabbatini M, Vega JA, Zaccheo D . Effect of long-term treatment with the dihydropyridine-type calcium channel blocker darodipine (PY 108-068) on the cerebral capillary network in aged rats . Mechanisms of Ageing and Development . 78 . 1 . 27–37 . January 1995 . 7603088 . 10.1016/0047-6374(94)01513-L . 42325236 .
4. Sannita WG, Garbarino S, Gesino D, Massimilla S, Ogliastro C . Plasma concentration and CNS effects of Ca antagonists darodipine and nimodipine after single-dose oral administration to healthy volunteers . Neuropsychobiology . 40 . 3 . 158–70 . September 1999 . 10494052 . 10.1159/000026614 . 36345887 .