BIMU-8
(Preusmjereno sa stranice BIMU8)
BIMU-8 je lek koji deluje kao selektivni agonist 5-HT4 receptora. BIMU-8 je bio jedno od prvih jedinjenja u oboj klasi. Ovaj ligand povišava brzinu respiracije.
(IUPAC) ime | |||
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N-[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]-2-oxo-3-(propan-2-yl)-2,3-dihydro-1H-benzimidazole-1-carboxamide hydrochloride | |||
Klinički podaci | |||
Identifikatori | |||
CAS broj | 134296-40-5 | ||
ATC kod | ? | ||
PubChem[1][2] | 5311028 | ||
ChemSpider[3] | 4470566 | ||
Hemijski podaci | |||
Formula | C19H26N4O2 · HCl | ||
Mol. masa | 342.44 g/mol (slobodna baza) 378.896 g/mol (HCl) | ||
SMILES | eMolekuli & PubHem | ||
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Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status |
Upotreba uredi
BIMU-8 doziran u kombinaciji sa opioidnim analgeticima sprečava opasnu hipoventilaciju, koja se javlja kad se opioidi koriste u ekcesivnim dozama.[4] BIMU-8 nema uticaja na opijatno suzbijanje bola. Ispitivanja na pacovima su pokazala da je BIMU-8 efektivan u sprečavanju hipoventilacije izazvane potentnim opioidom fentanilom,[5] koji je uzrokovao znatni broj smrtnih slučajeva kod ljudi. Klinička ispitivanja BIMU-8 još nisu sprovedena.
Druge aktivnosti uredi
Kao i nekoliko drugih 5-HT4 liganda, za BIMU-8 je nađeno da ima znatan afinitet za sigma receptore. On deluje kao antagonist σ2 receptora.[6][7][8]
Literatura uredi
- ↑ 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.
- ↑ 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.
- ↑ Manzke T, Guenther U, Ponimaskin E, Haller M, Dutschmann M, Schwarzacher S, Richter D (2003). „5-HT4(a) receptors avert opioid-induced breathing depression without loss of analgesia”. Science 301 (5630): 226–9. DOI:10.1126/science.1084674. PMID 12855812.
- ↑ Wang, X; Dergacheva, O; Kamendi, H; Gorini, C; Mendelowitz, D (2007). „5-Hydroxytryptamine 1A/7 and 4alpha receptors differentially prevent opioid-induced inhibition of brain stem cardiorespiratory function.”. Hypertension 50 (2): 368–76. DOI:10.1161/HYPERTENSIONAHA.107.091033. PMID 17576856.
- ↑ Bonhaus DW, Loury DN, Jakeman LB, Hsu SA, To ZP, Leung E, Zeitung KD, Eglen RM, Wong EH (October 1994). „[3H]RS-23597-190, a potent 5-hydroxytryptamine4 antagonist labels sigma-1 but not sigma-2 binding sites in guinea pig brain”. The Journal of Pharmacology and Experimental Therapeutics 271 (1): 484–93. PMID 7965749.
- ↑ Weatherspoon JK, Gonzalez-Alvear GM, Werling LL. Regulation of [3H]norepinephrine release from guinea pig hippocampus by sigma2 receptors. European Journal of Pharmacology. 1997 May 20;326(2-3):133-8. PMID 9196265
- ↑ Liu X, Nuwayhid S, Christie MJ, Kassiou M, Werling LL (June 2001). „Trishomocubanes: novel sigma-receptor ligands modulate amphetamine-stimulated [3H]dopamine release”. European Journal of Pharmacology 422 (1-3): 39–45. PMID 11430911.