Rauvolscin

Rauvolscin
(IUPAC) ime
	metil estar 17α-hidroksi-20α-johimban-16β-karboksilne kiseline
Klinički podaci
Identifikatori
CAS broj	131-03-3 6211-32-1 (HCl)
ATC kod	nije dodeljen
PubChem	643606
ChemSpider	558737
ChEBI	CHEBI:48562
ChEMBL	CHEMBL10347
Hemijski podaci
Formula	C21H26N2O3
Mol. masa	354,44 g/mol
InChI
	InChI=1S/C21H26N2O3/c1-26-21(25)19-15-10-17-20-14(13-4-2-3-5-16(13)22-20)8-9-23(17)11-12(15)6-7-18(19)24/h2-5,12,15,17-19,22,24H,6-11H2,1H3/t12-,15+,17+,18+,19+/m1/s1 ; Key: BLGXFZZNTVWLAY-DIRVCLHFSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	Nije kontrolisan
Način primene	Oralno

Rauvolscin (izojohimbin, α-johimbin, i korinantidin) je alkaloid koji je prisutan kod više vrsta biljki iz rodova Rauwolfia i Pausinystalia.^[5] On je stereoizomer johimbina.^[5] Rauvolscin je stimulant centralnog nervnog sistema, lokalni anestetik i u izvesnoj meri afrodizijak.^[5]

Rauvolscin deluje predominantno kao antagonist α₂-adrenergičnog receptora.^[6] On takođe deluje kao parcijalni agonist 5-HT_1A receptora i antagonist 5-HT_2A i 5-HT_2B receptora.^[7]^[8]^[9]

Reference[uredi - уреди | uredi izvor]

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. doi:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. doi:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. doi:10.1093/nar/gkr777. PMID 21948594. edit
↑ ^5.0 ^5.1 ^5.2 KOHLI JD, DE NN (June 1956). "Pharmacological action of rauwolscine". Nature 177 (4521): 1182. doi:10.1038/1771182a0. PMID 13334509.
↑ Perry BD, U'Prichard DC (December 1981). "[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors". European Journal of Pharmacology 76 (4): 461–4. doi:10.1016/0014-2999(81)90123-0. PMID 6276200.
↑ Arthur JM, Casañas SJ, Raymond JR (June 1993). "Partial agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors". Biochemical Pharmacology 45 (11): 2337–41. doi:10.1016/0006-2952(93)90208-E. PMID 8517875.
↑ Kaumann AJ (June 1983). "Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors". Naunyn-Schmiedeberg's Archives of Pharmacology 323 (2): 149–54. doi:10.1007/BF00634263. PMID 6136920.
↑ Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (January 1998). "[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor". Naunyn-Schmiedeberg's Archives of Pharmacology 357 (1): 17–24. doi:10.1007/PL00005133. PMID 9459568.

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[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. doi:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. doi:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. doi:10.1093/nar/gkr777. PMID 21948594. edit

[pmid13334509-5] 5.0 ^5.1 ^5.2 KOHLI JD, DE NN (June 1956). "Pharmacological action of rauwolscine". Nature 177 (4521): 1182. doi:10.1038/1771182a0. PMID 13334509.

[pmid6276200-6] Perry BD, U'Prichard DC (December 1981). "[3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors". European Journal of Pharmacology 76 (4): 461–4. doi:10.1016/0014-2999(81)90123-0. PMID 6276200.

[pmid8517875-7] Arthur JM, Casañas SJ, Raymond JR (June 1993). "Partial agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors". Biochemical Pharmacology 45 (11): 2337–41. doi:10.1016/0006-2952(93)90208-E. PMID 8517875.

[pmid6136920-8] Kaumann AJ (June 1983). "Yohimbine and rauwolscine inhibit 5-hydroxytryptamine-induced contraction of large coronary arteries of calf through blockade of 5 HT2 receptors". Naunyn-Schmiedeberg's Archives of Pharmacology 323 (2): 149–54. doi:10.1007/BF00634263. PMID 6136920.

[pmid9459568-9] Wainscott DB, Sasso DA, Kursar JD, Baez M, Lucaites VL, Nelson DL (January 1998). "[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor". Naunyn-Schmiedeberg's Archives of Pharmacology 357 (1): 17–24. doi:10.1007/PL00005133. PMID 9459568.

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Rauvolscin

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