Bioactivity | (S)-(-)-Bay-K-8644 is an agonist of L-type Ca2+ channel. (S)-(-)-Bay-K-8644 activates Ba2+ currents (IBa) (EC50=32 nM). | ||||||||||||
Target | EC50: 32 nM (IBa) | ||||||||||||
Invitro | (±)-Bay K 8644, a conventional racemic mixture of Bay K 8644, is widely used as an L-type Ca2+ channel agonist. Each optical isomer possesses opposite effects on IBa (R(+)-Bay K 8644 as an antagonist and (S)-(-)-Bay-K-8644 as an agonist. (S)-(-)-Bay-K-8644 can prevent the inhibitory actions of two distinct cyclic nucleotide pathways on IBa in gastric myocytes of the guinea pig antrum[1]. The Ca2+ channel activity is enhanced by 3–30 μM (S)-(-)-Bay-K-8644 an agonist of L-type Ca2+ channels[2]. The interactions of two Ca2+ channel activators (S)-(-)-Bay-K-8644 and FPL 64176 is examined on smooth muscle L-type Ca2+ channels. FPL 64176 (300 nM) causes a sustained contraction of rat tail artery strips. This contractile response is inhibited by approximately 70% by (S)-(-)-Bay-K-8644 (EC50=14 nM). (S)-(-)-Bay-K-8644 (100 nM) increases whole-cell Ca2+ currents in A7r5 smooth muscle cells but effectively blocks further stimulation by 1 μM FPL 64176[3]. | ||||||||||||
Name | (S)-(-)-Bay-K-8644 | ||||||||||||
CAS | 98625-26-4 | ||||||||||||
Formula | C16H15F3N2O4 | ||||||||||||
Molar Mass | 356.30 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Zhu HL, et al. Antagonistic actions of S(-)-Bay K 8644 on cyclic nucleotide-induced inhibition of voltage-dependent Ba(2+) currents in guinea pig gastric antrum. Naunyn Schmiedebergs Arch Pharmacol. 2008 Dec;378(6):609-15. [2]. Mironov SL, et al. L-type Ca2+ channels in inspiratory neurones of mice and their modulation by hypoxia. J Physiol. 1998 Oct 1;512 ( Pt 1):75-87. [3]. Rampe D, et al. Functional interactions between two Ca2+ channel activators, (S)-Bay K 8644 and FPL 64176, in smooth muscle. Mol Pharmacol. 1992 Apr;41(4):599-602. |