From: Does sumatriptan cross the blood–brain barrier in animals and man?
References | Dose of sumatriptan | Parameter used | Results | Indicates passage of sumatriptan across BBB |
---|---|---|---|---|
Sleight et al. (1990) [11] | 50 and 500 μg/kg (i.p.) (guinea pig) | Extracellular 5-HT levels in the frontal cortex as measured by microdialysis | No effect of systemic sumatriptan (sumatriptan 10−8–10−7 M in microlysate caused a decrease of 5-HT) | – |
Skingle et al. (1990) [24] | Dose 1–100 mg/kg (rodents) | Antinociceptive effect by (various tests) | No antinociceptive effect (in some tests 100 mg/kg had an effect) | – |
Nozaki et al. (1992) [36] | 720 nmol/kg (300 μg/kg) (rat) | c-fos expression in the trigeminal nucleus caudalis after autologous blood in cisterna magna | Sumatriptan reduced c-fos positive cells in trigeminal nucleus caudalis by 31% | (−/+) see commenta |
Moskowitz et al. (1993) [37] | 300 μg/kg (rats | c-fos expression in trigeminal nucleus caudalis after repeated CSD | Sumatriptan reduced c-fos expression | (−/+) see commenta |
Kaube et al. (1993) [12] | 100 μg/kg (cat) | Single units activity and trigeminal somatosensory evoked potentials after SSS stimulation | No effect of sumatriptan (after blood–brain barrier disruption with mannitol sumatriptan decreased the peak-to-peak amplitude of evoked potentials) | – |
Shepheard et al. (1995) [13] | 1,000 μg/kg (rat) | Expression of c-fos mRNA in trigeminal nucleus caudalis after stimulation of trigeminal ganglion | No effect of sumatriptan (after blood–brain barrier disruption with mannitol sumatriptan decreased expression of c-fos mRNA with 63% | – |
Ghehardini et al. 1996 [28] | 5–30 mg/kg (mouse)) | Antinociceptive effect (hot-plate test) | There was an antinociceptive effect, most likely mediated by the 5-HT1A receptor | ? |
Mitsikostas et al. (1996) [30] | 0.3–0.9 mg/kg (rat) | Brain monoamines concentration | 0.6 mg/kg decreased hypothalamic serotonin concentration | + |
Hoskin and Goadsby (1996) [29] | 85 μg/kg (cat) | c-fos expression in trigeminal nucleus caudalis after dilatation of SSS | Reduction of c-fos expression | (+/−) see commentsb |
Knyihár-Csillik et al. (1997) [14] | 120 μg/kg (rat) | c-fos in caudal trigeminal nucleus after stereo electrical stimulation of the trigeminal ganglion | No effect of sumatriptan on c-fos expression | – |
Ingvardsen et al. (1997) [27] | 300 μg/kg (rat) | c-fos in TNC after CSD | No effect of sumatriptan on c-fos expression | – |
Hoskin and Goadsby (1998) [5] | 85 μg/kg (rat) | c-fos expression in trigeminal nucleus caudalis after SSS stimulation | No effect on c-fos expressionb | – |
Read et al. (1999) [31] | 300 μg/kg (rat) | Nitric oxide formation in the cerebral cortex after nitroglycerin | Decrease of NO formation | + |
Read and Parsons [32] | 300 μg/kg (rat and cat) | Nitric oxide formation in the cerebral after CSD | Decrease of NO formation and decrease of partial oxygen tension | + |
Read et al. (2001) [25] | 300 μg/kg (rat) | CGMP after CSD | No effect on brain stem cGMP after 3 days | – |
Johnson et al. (2001) [20] | 3.2 mg/kg (rat) | Measurements of sumatriptan concentrations in microdialysate. Central release of 5-HT | Concentrations of sumatriptan up to 8 nM was observed. No effect on central release of 5-HT | + |
Kayser et al. (2002) [33] | 100 μg/kg (rat) | Mechanical allodynia-like behaviour after ligature of n. infraorbitalis | A significant reduction of mechanical allodynia-like behaviour on injured and contralateral side of the facec | + |
Dobson et al. (2004) [34] | 300–1,000 μg/kg (rat) | Serotonin synthesis in brain | Given acutely a decrease in 5-HT synthesis in certain regions of the brain was observed | + |
Pardutz et al. (2004) [26] | 600 μg/kg (rat) | Nitroglycerin-induced nNOS immunoreactive neurones in trigeminal nucleus caudalis | nNOS expression could not be prevented | – |
Levy et al. (2004) [21] | 300 μg/kg (rat) | Changes in spontaneous activity of trigeminal peripheral and central neurones after inflammatory soup on dura | Sumatriptan blocked the induction of central sensitization most likely by a presynaptic inhibition | + |
Edelmayer et al. (2009) [22] | 600 μg/kg (rat) | Prevention of facial allodynia after inflammatory mediators on the dura | Sumatriptan prevented or reversed facial allodynia | + |
Bates et al. (2009) [35] | 600 μg/kg i.p. and 0.06 μg intrathecal (mouse) | Prevention of thermal and mechanical allodynia | Systemic sumatriptan inhibited thermal allodynia but not mechanical allodynia. Intrathecal sumatriptan inhibited both | + |