Roksindol

Roksindol (EMD-49,980), orijinal olarak Merck KGaA tarafından şizofreni tedavisi için geliştirilmiş bir dopaminerjik ve serotonerjik ilaçtır.^[1]^[2]^[3] Klinik deneylerde antipsikotik etkinliği azdı, ancak beklenmedik bir şekilde güçlü ve hızlı antidepresan ve anksiyolitik etkiler ürettiği bulundu.^[2]^[3] Sonuç olarak, bunun yerine depresyon tedavisi için roksindol daha fazla araştırıldı.^[1]^[4] Ayrıca Parkinson hastalığı ve prolaktinoma için bir tedavi olarak araştırılmıştır.^[5]^[6]

Roxindol, aşağıdaki reseptörlerde bir agonist olarak etki eder:^[7]^[8]

D₂ reseptörü (pK, = 8.55)
D₃ reseptörü (pK, = 8.93)
D₄ reseptörü (pK, = 8.23)
5-HT_1A reseptörü (pK, = 9.42)

Kaynakça

^ ^a ^b "Roxindole, a dopamine autoreceptor agonist, in the treatment of major depression". Psychopharmacology. 111 (1): 123-6. 1993. doi:10.1007/BF02257418. PMID 7870927.
^ ^a ^b "Antipsychotic efficacy of the dopaminergic autoreceptor agonist EMD 49980 (Roxindol). Results of an open clinical study". Pharmacopsychiatry. 24 (4): 107-12. July 1991. doi:10.1055/s-2007-1014451. PMID 1684439.
^ ^a ^b "Early clinical results with the neuroleptic roxindole (EMD 49,980) in the treatment of schizophrenia--an open study". European Neuropsychopharmacology. 2 (1): 91-5. March 1992. doi:10.1016/0924-977X(92)90041-6. PMID 1353388.
^ "Roxindole, a potential antidepressant. I. Effect on the dopamine system". Journal of Neural Transmission. 103 (5): 627-41. 1996. doi:10.1007/bf01273159. PMID 8811507.
^ "Treatment of Parkinson's disease with the partial dopamine agonist EMD 49980". Movement Disorders. 8 (2): 195-7. April 1993. doi:10.1002/mds.870080214. PMID 8097280.
^ "Treatment of prolactinoma patients with the new non-ergot dopamine agonist roxindol: first results". The Clinical Investigator. 72 (6): 451-6. June 1994. doi:10.1007/bf00180520. PMID 7950157.
^ "Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 359 (6): 447-53. June 1999. doi:10.1007/pl00005374. PMID 10431754. 11 Şubat 2013 tarihinde kaynağından arşivlendi.
^ "Indolebutylamines as selective 5-HT(1A) agonists". Journal of Medicinal Chemistry. 47 (19): 4677-83. September 2004. doi:10.1021/jm040792y. PMID 15341483.

[pmid7870927-1] "Roxindole, a dopamine autoreceptor agonist, in the treatment of major depression". Psychopharmacology. 111 (1): 123-6. 1993. doi:10.1007/BF02257418. PMID 7870927.

[pmid1684439-2] "Antipsychotic efficacy of the dopaminergic autoreceptor agonist EMD 49980 (Roxindol). Results of an open clinical study". Pharmacopsychiatry. 24 (4): 107-12. July 1991. doi:10.1055/s-2007-1014451. PMID 1684439.

[pmid1353388-3] "Early clinical results with the neuroleptic roxindole (EMD 49,980) in the treatment of schizophrenia--an open study". European Neuropsychopharmacology. 2 (1): 91-5. March 1992. doi:10.1016/0924-977X(92)90041-6. PMID 1353388.

[pmid8811507-4] "Roxindole, a potential antidepressant. I. Effect on the dopamine system". Journal of Neural Transmission. 103 (5): 627-41. 1996. doi:10.1007/bf01273159. PMID 8811507.

[pmid8097280-5] "Treatment of Parkinson's disease with the partial dopamine agonist EMD 49980". Movement Disorders. 8 (2): 195-7. April 1993. doi:10.1002/mds.870080214. PMID 8097280.

[pmid7950157-6] "Treatment of prolactinoma patients with the new non-ergot dopamine agonist roxindol: first results". The Clinical Investigator. 72 (6): 451-6. June 1994. doi:10.1007/bf00180520. PMID 7950157.

[pmid10431754-7] "Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 359 (6): 447-53. June 1999. doi:10.1007/pl00005374. PMID 10431754. 11 Şubat 2013 tarihinde kaynağından arşivlendi.

[pmid15341483-8] "Indolebutylamines as selective 5-HT(1A) agonists". Journal of Medicinal Chemistry. 47 (19): 4677-83. September 2004. doi:10.1021/jm040792y. PMID 15341483.

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