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Palonidipine Sale

(Synonyms: 帕洛地平) 目录号 : GC36843

Palonidipine 是一种钙拮抗剂,有治疗心绞痛和高血压的潜力。

Palonidipine Chemical Structure

Cas No.:96515-73-0

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产品描述

Palonidipine is a calcium antagonist which is potential for the therapy of angina-pectoris and hypertension[1][2][3]. Calcium[1]

[1]. Okamiya Y, et al. [Effect of palonidipine hydrochloride (TC-81), a novel calcium antagonist, on the canine coronary artery]. Nihon Yakurigaku Zasshi. 1993 Jul;102(1):23-33. [2]. Kishimoto T, et al. [Effect of palonidipine hydrochloride (TC-81), a new dihydropyridine derivative, on various myocardial ischemic models]. Nihon Yakurigaku Zasshi. 1993 Aug;102(2):85-100. [3]. K. Sunakawa, et al. Effects of palonidipine hydrochloride on respiratory and cardiovascular systems. January 1993

Chemical Properties

Cas No. 96515-73-0 SDF
别名 帕洛地平
Canonical SMILES O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC([N+]([O-])=O)=CC=C2F)OCC(C)(C)CN(C)CC3=CC=CC=C3
分子式 C29H34FN3O6 分子量 539.6
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8532 mL 9.2661 mL 18.5322 mL
5 mM 0.3706 mL 1.8532 mL 3.7064 mL
10 mM 0.1853 mL 0.9266 mL 1.8532 mL
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Research Update

[Effect of Palonidipine hydrochloride (TC-81), a new dihydropyridine derivative, on various myocardial ischemic models]

Nihon Yakurigaku Zasshi 1993 Aug;102(2):85-100.PMID:8370558DOI:10.1254/fpj.102.85.

The antianginal effects of Palonidipine, a novel 1,4-dihydropyridine derivative, and nifedipine on various myocardial ischemic models were compared. (1) Palonidipine at 0.5 mg/kg, p.o. significantly inhibited vasopressin-induced ST depression of ECG in Donryu rats. This activity was about 5 times more potent than that of nifedipine and was long-lasting. (2) Palonidipine at 1 mg/kg, i.d. significantly inhibited ST depression induced by isoproterenol in Wistar rats. This activity of TC-81 was more potent than that of nifedipine. (3) Palonidipine at 3 micrograms/kg, i.v. produced an increase in regional myocardial tissue blood flow in the ischemic region of chronic coronary artery occluded dogs. (4) In isolated dog coronary artery, Palonidipine at a concentration of 10(-10) M or greater inhibited the amplitude of 3,4-DAP-induced cyclic contractions in a concentration-dependent manner. This activity was 10-30 times more potent than that of nifedipine. (5) An intracoronary injection of endothelin (30 pmol/kg) reduced the coronary blood flow, subepicardial tissue blood flow, and subepicardial pH in anesthetized dogs. The ST elevation of ECG over 0.1 mV also occurred in 8 of 10 cases. In all the cases, ventricular extrasystoles were noted, and 9 out of 10 animals died. Pretreatment with Palonidipine (3 micrograms/kg, i.v.) inhibited endothelin-induced ischemic changes, with a potency greater than that of nifedipine. These results suggest that Palonidipine may be useful for the therapy of angina-pectoris.

[Inhibitory effects of Palonidipine hydrochloride (TC-81) on contractions induced by various vasoconstrictors in rat aorta]

Nihon Yakurigaku Zasshi 1993 Apr;101(4):281-8.PMID:8514210DOI:10.1254/fpj.101.4_281.

Inhibitions by Palonidipine hydrochloride (TC-81), a new Ca entry blocker, of the contractile responses to norepinephrine (NE), serotonin (5-HT), prostaglandin F2 alpha (PGF2 alpha) and U-46619, a thromboxane A2 analog, were investigated in isolated rat aorta strips and compared with the inhibition of the high K+ response. TC-81 and nicardipine inhibited the contractile responses to NE, 5-HT, PGF2 alpha, and U-46619 in a concentration-dependent manner, but their relative inhibitions were less than 50% at 10(-8) M. In a Ca(2+)-free medium, 2-hr pretreatment with TC-81 or nicardipine did not inhibit the contractile responses to various vasoconstrictors, but it inhibited the responses to the addition of Ca. Their inhibitory potencies were less than the inhibition with high K+. Also, the treatment with TC-81 or nicardipine at 10(-7) M did not affect the tissue level of cyclic AMP. These results suggest that in isolated rat aorta, the inhibition by TC-81 of the contractile responses to NE, 5-HT, PGF2 alpha and U-46619 is not due to inhibition of intracellular Ca2+ release or an increase in cyclic AMP; rather, it is due to inhibition of the Ca2+ influx. This inhibitory effect was less than that seen on the high K+ response.

[Effect of Palonidipine hydrochloride (TC-81), a novel calcium antagonist, on the canine coronary artery]

Nihon Yakurigaku Zasshi 1993 Jul;102(1):23-33.PMID:8335285DOI:10.1254/fpj.102.23.

The effects of Palonidipine hydrochloride [TC-81: (+/-)-3-benzylmethylamino)-2,2-dimethylpropyl methyl 4-(2-fluoro-5-nitrophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate hydrochloride], a new calcium antagonist, on the coronary artery were studied in dogs. In the isolated canine coronary artery, TC-81 inhibited high K+ (60 mM)-induced contraction in a concentration-dependent manner. The relaxant activity of TC-81 was equal to that of nicardipine and more potent than those of nifedipine and diltiazem. TC-81 increased coronary blood flow in a dose-dependent manner after i.v.-administration in anesthetized open-chest dogs. The activity of TC-81 was equal to that of nifedipine or nicardipine, but the duration of its effect was longer than that of nifedipine or nicardipine. By oral administration in conscious dogs, TC-81 increased coronary blood flow at 0.1 mg/kg or more, and its activity was 10 times more potent than that of nifedipine. These results suggest that TC-81 increases coronary blood flow and is capable of improving the oxygen supply-demand relationship during angina pectoris.