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.
^Gaggi R, Dall'Olio R, Roncada P, Gianni AM (June–July 1995). "Effects of isradipine and darodipine on serotonergic system of the rat brain". Pharmacology, Biochemistry, and Behavior. 51 (2–3): 183–7. doi:10.1016/0091-3057(94)00389-Z. PMID 7545305. S2CID 6704491.
^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. doi:10.1016/1043-6618(94)80030-8.
^Amenta F, Ferrante F, Mancini M, Sabbatini M, Vega JA, Zaccheo D (January 1995). "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. doi:10.1016/0047-6374(94)01513-L. PMID 7603088. S2CID 42325236.
^Sannita WG, Garbarino S, Gesino D, Massimilla S, Ogliastro C (September 1999). "Plasma concentration and CNS effects of Ca antagonists darodipine and nimodipine after single-dose oral administration to healthy volunteers". Neuropsychobiology. 40 (3): 158–70. doi:10.1159/000026614. PMID 10494052. S2CID 36345887.
Further readingedit
Matucci R, Ottaviani MF, Barbieri M, Cerbai E, Mugelli A (December 1997). "Protective effect of darodipine, a calcium antagonist, on rat cardiomyocytes against oxygen radical-mediated injury". British Journal of Pharmacology. 122 (7): 1353–60. doi:10.1038/sj.bjp.0701525. PMC1565083. PMID 9421282.</ref>
This biochemistry article is a stub. You can help Wikipedia by expanding it.
darodipine, experimental, calcium, channel, blocker, that, based, animal, models, reduce, neuronal, cytoskeletal, alterations, during, aging, neurodegenerative, disorders, studies, performed, rats, have, shown, darodipine, have, effect, brain, serotonergic, sy. 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 Darodipine Names Preferred IUPAC name Diethyl 4 2 1 3 benzoxadiazol 4 yl 2 6 dimethyl 1 4 dihydropyridine 3 5 dicarboxylate Other names 4 2 1 3 Benzoxadiazol 7 yl 2 6 dimethyl 1 4 dihydropyridine 3 5 dicarboxylic acid diethyl ester Identifiers CAS Number 72803 02 2 3D model JSmol Interactive image ChEMBL ChEMBL2104154 ChemSpider 46790 PubChem CID 51701 UNII N4AL7X96GL Y CompTox Dashboard EPA DTXSID90223125 InChI InChI 1 C19H21N3O5 c1 5 25 18 23 14 10 3 20 11 4 15 19 24 26 6 2 16 14 12 8 7 9 13 17 12 22 27 21 13 h7 9 16 20H 5 6H2 1 4H3Key QERUYFVNIOLCHV UHFFFAOYAW SMILES O C OCC C3 C N C C C O OCC C3c1cccc2nonc12 C C Properties Chemical formula C 19H 21N 3O 5 Molar mass 371 393 g mol 1 Except where otherwise noted data are given for materials in their standard state at 25 C 77 F 100 kPa Infobox references 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 editIsradipine a structural isomer of darodipineReferences edit Gaggi R Dall Olio R Roncada P Gianni AM June July 1995 Effects of isradipine and darodipine on serotonergic system of the rat brain Pharmacology Biochemistry and Behavior 51 2 3 183 7 doi 10 1016 0091 3057 94 00389 Z PMID 7545305 S2CID 6704491 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 doi 10 1016 1043 6618 94 80030 8 Amenta F Ferrante F Mancini M Sabbatini M Vega JA Zaccheo D January 1995 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 doi 10 1016 0047 6374 94 01513 L PMID 7603088 S2CID 42325236 Sannita WG Garbarino S Gesino D Massimilla S Ogliastro C September 1999 Plasma concentration and CNS effects of Ca antagonists darodipine and nimodipine after single dose oral administration to healthy volunteers Neuropsychobiology 40 3 158 70 doi 10 1159 000026614 PMID 10494052 S2CID 36345887 Further reading editMatucci R Ottaviani MF Barbieri M Cerbai E Mugelli A December 1997 Protective effect of darodipine a calcium antagonist on rat cardiomyocytes against oxygen radical mediated injury British Journal of Pharmacology 122 7 1353 60 doi 10 1038 sj bjp 0701525 PMC 1565083 PMID 9421282 lt ref gt nbsp This biochemistry article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Darodipine amp oldid 1150301588, wikipedia, wiki, book, books, library,
