| Bioactivity | Bay K 8644 ((±)-Bay K 8644) is a racemate consisting of two isomers (R)-(+)-Bay-K-8644 and (S)-(-)-Bay-K-8644[1]. Bay K 8644 is a L-type Ca2+ channel agonist with an EC50 of 17.3 nM. Bay K 8644 increases Ca2+ influx through sarcolemmal Ca2+ channels by increasing the open time of the channel. Bay K 8644 has vasoconstrictive effects[2][3]. | ||||||||||||
| Invitro | In newborn rat ventricular cardiomyocytes, Bay K 8644 (1 μM) treatment increases L-type calcium current density in 2-day-old cells. The higher increase of L-type calcium current density by Bay K 8644 in 2-day- than in 7-day-old cultured cells could be interpreted as the result of a difference in the phosphorylation level of calcium channels for each stage of development[4]. | ||||||||||||
| In Vivo | A one time dose as low as 10 μg/kg of Bay K 8644 significantly elevates mean arterial pressure (MAP) in endotoxin-treated hypotensive rats while having minimal effects in normal rats. Bay K 8644 also causes a dose-dependent decrease in heart rate of 37% in endotoxin-treated rats and 39% in control rats[5]. | ||||||||||||
| Name | Bay K 8644 | ||||||||||||
| CAS | 71145-03-4 | ||||||||||||
| Formula | C16H15F3N2O4 | ||||||||||||
| Molar Mass | 356.30 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. W Schreibmayer, et al. Kinetic modulation of guinea-pig cardiac L-type calcium channels by fendiline and reversal of the effects of Bay K 8644. Br J Pharmacol. 1992 May;106(1):151-6. [2]. G A Rae, et al. Interactions of calcium antagonists and the calcium channel agonist Bay K 8644 on neurotransmission of the mouse isolated vas deferens. Br J Pharmacol. 1989 Feb;96(2):333-40. [3]. H Satoh, et al. Bay K 8644 increases resting Ca2+ spark frequency in ferret ventricular myocytes independent of Ca influx: contrast with caffeine and ryanodine effects. Circ Res. 1998 Dec 14-28;83(12):1192-204. [4]. J P Gomez, et al. Effects of Bay K 8644 on L-type calcium current from newborn rat cardiomyocytes in primary culture. J Mol Cell Cardiol. 1996 Oct;28(10):2217-29. [5]. N Ives,et al. BAY k 8644, a calcium channel agonist, reverses hypotension in endotoxin-shocked rats. Eur J Pharmacol. 1986 Nov 4;130(3):169-75. |
Bay K 8644
CAS: 71145-03-4 F: C16H15F3N2O4 W: 356.30
Bay K 8644 ((±)-Bay K 8644) is a racemate consisting of two isomers (R)-(+)-Bay-K-8644 and (S)-(-)-Bay-K-8644. Bay K 86
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