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2s 3 1s 1 3 4 dichlorophenyl ethyl amino 2 hydroxypropyl phenylmethyl phosphinic acid hydrochloride cgp 55845

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(2S)-3-[[(1S)-1-(3,4-dichlorophenyl)ethyl]amino-2-hydroxypropyl] (phenylmethyl) phosphinic acid hydrochloride (CGP-55845) is a chemical compound. It functions as a selective GABA(B) receptor antagonist.

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3 protocols using 2s 3 1s 1 3 4 dichlorophenyl ethyl amino 2 hydroxypropyl phenylmethyl phosphinic acid hydrochloride cgp 55845

1

Synthesis and Properties of α-Conotoxins

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α-Conotoxins Vc1.1, cyclized-Vc1.1 (c-Vc1.1), and PeIA were synthesized as described previously (Clark et al., 2006 (link), 2010 (link); Daly et al., 2011 (link)). Synthetic Vc1.1 and PeIA are 16–amino acid residue peptides with a characteristic helical region and two disulfide bonds in a I–III, II–IV arrangement (Clark et al., 2006 (link), 2010 (link); Daly et al., 2011 (link)). c-Vc1.1 exhibits better properties than the linear Vc1.1 (also known as ACV1), including high chemical stability, resistance to cleavage by proteases, and improved potency to inhibit N-type VGCCs (Clark et al., 2010 (link)). Most data on α-conotoxin effects on various Cav2 channels were obtained using c-Vc1.1, unless otherwise noted. GABA, baclofen, guanosine 5′-[β-thio]diphosphate trilithium salt (GDP-β-S), and pertussis toxin (PTX) were purchased from Sigma-Aldrich. (2S)-3-[[(1S)-1-(3,4-dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl) phosphinic acid hydrochloride (CGP55845) and pp60c-Src peptide (521–533) were purchased from Tocris Bioscience.
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2

Microdialysis Experiments with Pharmacological Agents

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The aCSF for the microdialysis experiments was purchased from Tocris Biosciences (Bristol, UK). 3,5-dichloro-N-[1-(2,2-dimethyl-tetrahydro-pyran-4-ylmethyl)-4-fluoro-piperidin-4-yl-methyl]-benzamide (TTA-P2) was a kind gift from Merck Inc. (USA). TTA-P2 was dissolved in DMSO (2% of final solution) before addition to aCSF. An identical concentration of DMSO was added to the aCSF solutions. (2S)-3-[[(1S)-1-(3,4-dichlorophenyl)ethyl]amino-2-hydroxypropyl] (phenylmethyl) phosphinic acid hydrochloride (CGP-55845) was purchased from Tocris (UK). The pH of all dialysis solutions was 7.
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3

Microdialysis Experiments with Pharmacological Agents

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The aCSF for the microdialysis experiments was purchased from Tocris Biosciences (Bristol, UK). 3,5-dichloro-N-[1-(2,2-dimethyl-tetrahydro-pyran-4-ylmethyl)-4-fluoro-piperidin-4-yl-methyl]-benzamide (TTA-P2) was a kind gift from Merck Inc. (USA). TTA-P2 was dissolved in DMSO (2% of final solution) before addition to aCSF. An identical concentration of DMSO was added to the aCSF solutions. (2S)-3-[[(1S)-1-(3,4-dichlorophenyl)ethyl]amino-2-hydroxypropyl] (phenylmethyl) phosphinic acid hydrochloride (CGP-55845) was purchased from Tocris (UK). The pH of all dialysis solutions was 7.
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