Dotarizin

Dotarizin
Dữ liệu lâm sàng
Đồng nghĩa	Dotarizine
Mã ATC	none;
Các định danh
	Tên IUPAC 1-[diphenylmethyl]-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]piperazine;
Số đăng ký CAS	84625-59-2;
PubChem CID	55285;
ChemSpider	49929 ;
Định danh thành phần duy nhất	IO7663S6D3;
ChEBI	CHEBI:138033;
ChEMBL	CHEMBL2106316 ;
Dữ liệu hóa lý
Công thức hóa học	C29H34N2O2
Khối lượng phân tử	442.592 g/mol
Mẫu 3D (Jmol)	Hình ảnh tương tác;
	SMILES C1CN(CCN1CCCC2(OCCO2)C3=CC=CC=C3)C(C4=CC=CC=C4)C5=CC=CC=C5;
	Định danh hóa học quốc tế InChI=1S/C29H34N2O2/c1-4-11-25(12-5-1)28(26-13-6-2-7-14-26)31-21-19-30(20-22-31)18-10-17-29(32-23-24-33-29)27-15-8-3-9-16-27/h1-9,11-16,28H,10,17-24H2 ; Key:LRMJAFKKJLRDLE-UHFFFAOYSA-N ;
(kiểm chứng)

Dotarizine là một loại thuốc được sử dụng trong điều trị chứng đau nửa đầu,^[1] hoạt động như một thuốc chẹn kênh calci,^[2] và cũng là một chất đối kháng ở thụ thể 5HT_2A, và ở mức độ thấp hơn ở các thụ thể 5HT_1A và 5HT_2C.^[3]^[4] Hành động chống đau nửa đầu được cho là do tác dụng của nó như một thuốc giãn mạch,^[5]^[6] nhưng nó cũng có một số tác dụng giải lo âu ^[7] và ngăn chặn chứng mất trí nhớ do sốc điện ở động vật.^[8]

Tham khảo

^ Ruiz-Nuño, A; Villarroya, M; Cano-Abad, M; Rosado, A; Balfagón, G; López, MG; García, AG (2001). “Mechanisms of blockade by the novel migraine prophylactic agent, dotarizine, of various brain and peripheral vessel contractility”. European Journal of Pharmacology. 411 (3): 289–99. doi:10.1016/S0014-2999(00)00897-9. PMID 11164387.
^ Ruiz-Nuño, A; Mayorgas, I; Hernández-Guijo, JM; Olivares, R; García, AG; Gandía, L (2003). “Antimigraine dotarizine blocks P/Q Ca2+ channels and exocytosis in a voltage-dependent manner in chromaffin cells”. European Journal of Pharmacology. 481 (1): 41–50. doi:10.1016/j.ejphar.2003.09.013. PMID 14637173.
^ Farré, M; Roset, PN; Llorente, M; Márquez, M; Albet, C; Pérez, JA; Herrero, E; Ortíz, JA (1997). “Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration”. Methods and findings in experimental and clinical pharmacology. 19 (5): 343–50. PMID 9379783.
^ Montiel, C; Herrero, CJ; García-Palomero, E; Renart, J; García, AG; Lomax, RB (1997). “Serotonergic effects of dotarizine in coronary artery and in oocytes expressing 5-HT2 receptors”. European Journal of Pharmacology. 332 (2): 183–93. doi:10.1016/S0014-2999(97)01073-X. PMID 9286620.
^ Kuridze, N; Gajkowska, B; Czernicki, Z; Jurkiewicz, J; Cervos-Navarro, J (1998). “The effect of Dotarizine--(Ca2+ channel blocker)--on vascular reactivity and ultrastructure of cerebral capillaries in animals subjected to anoxia”. Folia Neuropathologica. 36 (2): 101–8. PMID 9757621.
^ Kuridze, N; Czernicki, Z; Jarus-Dziedzic, K; Jurkiewicz, J; Cervos-Navarro, J (2000). “Regional differences of cerebrovascular reactivity effected by calcium channel blocker - dotarizine”. Journal of the Neurological Sciences. 175 (1): 13–6. doi:10.1016/S0022-510X(00)00275-6. PMID 10785251.
^ Petkov, VD; Belcheva, S; Konstantinova, E (1995). “Anxiolytic effects of dotarizine, a possible antimigraine drug”. Methods and findings in experimental and clinical pharmacology. 17 (10): 659–68. PMID 9053586.
^ Lazarova, M; Petkova, B; Petkov, VD (1995). “Effect of dotarizine on electroconvulsive shock or pentylenetetrazol-induced amnesia and on seizure reactivity in rats”. Methods and findings in experimental and clinical pharmacology. 17 (1): 53–8. PMID 7623521.

[1] Ruiz-Nuño, A; Villarroya, M; Cano-Abad, M; Rosado, A; Balfagón, G; López, MG; García, AG (2001). “Mechanisms of blockade by the novel migraine prophylactic agent, dotarizine, of various brain and peripheral vessel contractility”. European Journal of Pharmacology. 411 (3): 289–99. doi:10.1016/S0014-2999(00)00897-9. PMID 11164387.

[2] Ruiz-Nuño, A; Mayorgas, I; Hernández-Guijo, JM; Olivares, R; García, AG; Gandía, L (2003). “Antimigraine dotarizine blocks P/Q Ca2+ channels and exocytosis in a voltage-dependent manner in chromaffin cells”. European Journal of Pharmacology. 481 (1): 41–50. doi:10.1016/j.ejphar.2003.09.013. PMID 14637173.

[3] Farré, M; Roset, PN; Llorente, M; Márquez, M; Albet, C; Pérez, JA; Herrero, E; Ortíz, JA (1997). “Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration”. Methods and findings in experimental and clinical pharmacology. 19 (5): 343–50. PMID 9379783.

[4] Montiel, C; Herrero, CJ; García-Palomero, E; Renart, J; García, AG; Lomax, RB (1997). “Serotonergic effects of dotarizine in coronary artery and in oocytes expressing 5-HT2 receptors”. European Journal of Pharmacology. 332 (2): 183–93. doi:10.1016/S0014-2999(97)01073-X. PMID 9286620.

[5] Kuridze, N; Gajkowska, B; Czernicki, Z; Jurkiewicz, J; Cervos-Navarro, J (1998). “The effect of Dotarizine--(Ca2+ channel blocker)--on vascular reactivity and ultrastructure of cerebral capillaries in animals subjected to anoxia”. Folia Neuropathologica. 36 (2): 101–8. PMID 9757621.

[6] Kuridze, N; Czernicki, Z; Jarus-Dziedzic, K; Jurkiewicz, J; Cervos-Navarro, J (2000). “Regional differences of cerebrovascular reactivity effected by calcium channel blocker - dotarizine”. Journal of the Neurological Sciences. 175 (1): 13–6. doi:10.1016/S0022-510X(00)00275-6. PMID 10785251.

[7] Petkov, VD; Belcheva, S; Konstantinova, E (1995). “Anxiolytic effects of dotarizine, a possible antimigraine drug”. Methods and findings in experimental and clinical pharmacology. 17 (10): 659–68. PMID 9053586.

[8] Lazarova, M; Petkova, B; Petkov, VD (1995). “Effect of dotarizine on electroconvulsive shock or pentylenetetrazol-induced amnesia and on seizure reactivity in rats”. Methods and findings in experimental and clinical pharmacology. 17 (1): 53–8. PMID 7623521.

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