BIMU-8

BIMU-8
IUPAC ime
	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
Identifikatori
CAS broj	134296-40-5
PubChem	CID 5311028
ChemSpider	4470566
Hemijski podaci
Formula	C19H26N4O2 · HCl
Molarna masa	342.44 g/mol (slobodna baza); 378.896 g/mol (HCl)
	SMILES Cl.O=C2N(c1ccccc1N2C(=O)NC4C[C@H]3N(C)[C@H](CC3)C4)C(C)C; ;
	InChI InChI=1S/C19H26N4O2.ClH/c1-12(2)22-16-6-4-5-7-17(16)23(19(22)25)18(24)20-13-10-14-8-9-15(11-13)21(14)3;/h4-7,12-15H,8-11H2,1-3H3,(H,20,24);1H/t13?,14-,15+; ; Key:NQYXXIUVFVOJCX-XZPOUAKSSA-N ;

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.

Upotreba

BIMU-8 doziran u kombinaciji sa opioidnim analgeticima sprečava opasnu hipoventilaciju, koja se javlja kad se opioidi koriste u ekcesivnim dozama.^[1] 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,^[2] koji je uzrokovao znatni broj smrtnih slučajeva kod ljudi. Klinička ispitivanja BIMU-8 još nisu sprovedena.

Druge aktivnosti

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.^[3]^[4]^[5]

Reference

^ 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. Bibcode:2003Sci...301..226M. PMID 12855812. S2CID 13641423. doi:10.1126/science.1084674.
^ 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. PMID 17576856. S2CID 27137794. doi:10.1161/HYPERTENSIONAHA.107.091033.
^ Bonhaus DW, Loury DN, Jakeman LB, Hsu SA, To ZP, Leung E, Zeitung KD, Eglen RM, Wong EH (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, J. K.; Gonzalez-Alvear, G. M.; Werling, L. L. (1997). „Regulation of 3Hnorepinephrine release from guinea pig hippocampus by sigma2 receptors”. European Journal of Pharmacology. 326 (2–3): 133—138. PMID 9196265. doi:10.1016/s0014-2999(97)85407-6.
^ Liu X, Nuwayhid S, Christie MJ, Kassiou M, Werling LL (2001). „Trishomocubanes: novel sigma-receptor ligands modulate amphetamine-stimulated [3H]dopamine release”. European Journal of Pharmacology. 422 (1–3): 39—45. PMID 11430911. doi:10.1016/s0014-2999(01)01071-8.

Spoljašnje veze

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[1] 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. Bibcode:2003Sci...301..226M. PMID 12855812. S2CID 13641423. doi:10.1126/science.1084674.

[2] 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. PMID 17576856. S2CID 27137794. doi:10.1161/HYPERTENSIONAHA.107.091033.

[pmid7965749-3] Bonhaus DW, Loury DN, Jakeman LB, Hsu SA, To ZP, Leung E, Zeitung KD, Eglen RM, Wong EH (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.

[4] Weatherspoon, J. K.; Gonzalez-Alvear, G. M.; Werling, L. L. (1997). „Regulation of 3Hnorepinephrine release from guinea pig hippocampus by sigma2 receptors”. European Journal of Pharmacology. 326 (2–3): 133—138. PMID 9196265. doi:10.1016/s0014-2999(97)85407-6.

[pmid11430911-5] Liu X, Nuwayhid S, Christie MJ, Kassiou M, Werling LL (2001). „Trishomocubanes: novel sigma-receptor ligands modulate amphetamine-stimulated [3H]dopamine release”. European Journal of Pharmacology. 422 (1–3): 39—45. PMID 11430911. doi:10.1016/s0014-2999(01)01071-8.

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