普罗地平

普罗地平
臨床資料
其他名稱	BY-101; 1-Isopropyl-4,4-diphenylpiperidine
给药途径	口服给药、靜脈注射
藥物類別	Antiparkinsonian agents
识别信息
	IUPAC命名法 4,4-diphenyl-1-propan-2-ylpiperidine; ;
CAS号	31314-38-2
PubChem CID	65775;
ChemSpider	59195;
UNII	51567MYG7V;
ChEMBL	ChEMBL277382;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID20185247 ;
化学信息
化学式	C20H25N
摩尔质量	279.43 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CC(C)N1CCC(CC1)(C2=CC=CC=C2)C3=CC=CC=C3;
	InChI InChI=1S/C20H25N/c1-17(2)21-15-13-20(14-16-21,18-9-5-3-6-10-18)19-11-7-4-8-12-19/h3-12,17H,13-16H2,1-2H3; Key:CFOOTBBXHJHHMT-UHFFFAOYSA-N;

普罗地平（英語：Prodipine，开发代号：BY-101）是一种含氮有机化合物，分子式C
20H
25N，结构上与叔丁哌苯相似，用作帕金森氏症治疗药物，从未上市销售^[2]^[3]^[1]。

参考文献

^ ^1.0 ^1.1 Przuntek H, Stasch JP. Biochemical and Pharmacologic Aspects of the Mechanism of Action of Budipine. Clinical Experiences with Budipine in Parkinson Therapy. Berlin, Heidelberg: Springer Berlin Heidelberg. 1985: 107–112. ISBN 978-3-540-13764-1. doi:10.1007/978-3-642-95455-9_15. Anticholinergics are widely used in addition to target drugs. A preliminary clinical trial (between 1974 and 1976) with prodipine in 161 patients with Parkinson's disease showed excellent to moderate improvement of resting tremor in 60 of the patients, while medication had to be discontinued in 98 patients owing to gastrointestinal side effects and hypotension. [...] Improvement of disability scores [with budipine] (Birkmayer and Neumayer 1972) gave evidence of a dopaminergic action although in some patients side effects were more frequent than with prodipine. [...] Budipine has less tendency to induce hyperactivity than its structural analogue prodipine and so with budipine anxious agitation states are a less frequent side effect. [...] Prodipin (1-isopropyl-4,4-diphenylpiperidine hydrochloride), the precursor of budipine, had already been found superior (unpublished study, Elena Klinik, Kassel, 1977) in this respect in a large number of patients. But the drug had one big disadvantage, it was tolerated on i.v. injection only. Oral doses caused nausea and vomiting and were thus not feasible. We now have high hopes for the product which was further developed, budipine.
^ Gerstenbrand F, Poewe W, Stern G. Clinical Experiences with Budipine in Parkinson Therapy. Springer Berlin Heidelberg. 1985: 80,107,142 [28 September 2024]. ISBN 978-3-642-95455-9.
^ Vidaluc JL. MPTP as a Molecular Paradigm for Neurodegeneration. A Review of its Connections with Relevant Molecules. Current Medicinal Chemistry. Bentham Science Publishers. 1996: 117–138 [28 September 2024]. Protective effect in the parkinsonian model with MPTP were displayed by prodipine (R=i-Pr) and budipine (R=t-Bu) in the 4,4-diphenylpiperidine series [110].

[PrzuntekStasch1985-1] 1.0 ^1.1 Przuntek H, Stasch JP. Biochemical and Pharmacologic Aspects of the Mechanism of Action of Budipine. Clinical Experiences with Budipine in Parkinson Therapy. Berlin, Heidelberg: Springer Berlin Heidelberg. 1985: 107–112. ISBN 978-3-540-13764-1. doi:10.1007/978-3-642-95455-9_15. Anticholinergics are widely used in addition to target drugs. A preliminary clinical trial (between 1974 and 1976) with prodipine in 161 patients with Parkinson's disease showed excellent to moderate improvement of resting tremor in 60 of the patients, while medication had to be discontinued in 98 patients owing to gastrointestinal side effects and hypotension. [...] Improvement of disability scores [with budipine] (Birkmayer and Neumayer 1972) gave evidence of a dopaminergic action although in some patients side effects were more frequent than with prodipine. [...] Budipine has less tendency to induce hyperactivity than its structural analogue prodipine and so with budipine anxious agitation states are a less frequent side effect. [...] Prodipin (1-isopropyl-4,4-diphenylpiperidine hydrochloride), the precursor of budipine, had already been found superior (unpublished study, Elena Klinik, Kassel, 1977) in this respect in a large number of patients. But the drug had one big disadvantage, it was tolerated on i.v. injection only. Oral doses caused nausea and vomiting and were thus not feasible. We now have high hopes for the product which was further developed, budipine.

[GerstenbrandPoewe1985-2] Gerstenbrand F, Poewe W, Stern G. Clinical Experiences with Budipine in Parkinson Therapy. Springer Berlin Heidelberg. 1985: 80,107,142 [28 September 2024]. ISBN 978-3-642-95455-9.

[Vidaluc1996-3] Vidaluc JL. MPTP as a Molecular Paradigm for Neurodegeneration. A Review of its Connections with Relevant Molecules. Current Medicinal Chemistry. Bentham Science Publishers. 1996: 117–138 [28 September 2024]. Protective effect in the parkinsonian model with MPTP were displayed by prodipine (R=i-Pr) and budipine (R=t-Bu) in the 4,4-diphenylpiperidine series [110].

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