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Submit ReviewSKF 97541
Description: Highly potent GABAB agonist; also GABAA-ρ antagonist
Alternative Names: CGP 35024
Chemical Name: 3-Aminopropyl(methyl)phosphinic acid
Biological Activity for SKF 97541
SKF 97541 is a potent GABAB agonist (EC50 = 50 nM). SKF 97541 depresses striatal synaptic potentials and hyperpolarizes nigral neurons (EC50 values = 92 nM and 150 nM, respectively). SKF 97541 shows antidepressant effects in animal models and is also a GABAA-ρ antagonist.
Technical Data for SKF 97541
| M. Wt | 137.12 |
| Formula | C4H12NO2P |
| Storage | Desiccate at RT |
| CAS Number | 127729-35-5 |
| PubChem ID | 5230 |
| InChI Key | NHVRIDDXGZPJTJ-UHFFFAOYSA-N |
| Smiles | NCCCP(O)(C)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SKF 97541
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 13.71 | 100 |
Preparing Stock Solutions for SKF 97541
The following data is based on the product molecular weight 137.12. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 7.29 mL | 36.46 mL | 72.93 mL |
| 5 mM | 1.46 mL | 7.29 mL | 14.59 mL |
| 10 mM | 0.73 mL | 3.65 mL | 7.29 mL |
| 50 mM | 0.15 mL | 0.73 mL | 1.46 mL |
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Product Datasheets for SKF 97541
References for SKF 97541
References are publications that support the biological activity of the product.
Bon and Galvan (1996) Electrophysiological characterization of GABAB agonists and antagonists in dorso-lateral septal neurones in vitro. Br.J.Pharmacol. 118 961 PMID: 8799569
Froestl et al (1995) Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J.Med.Chem. 38 3297 PMID: 7650684
Johnston (1996) GABAC receptors: relatively simple transmitter-gated ion channels? TiPS 17 319 PMID: 8885697
Seabrook et al (1990) Electrophysiological characterization of potent agonists and antagonists on pre- and postsynaptic GABAB receptors on neurones in brain slices. Br.J.Pharmacol. 101 949 PMID: 1964824
If you know of a relevant reference for SKF 97541, please let us know.
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Keywords: SKF 97541, SKF 97541 supplier, potent, GABAB, agonists, GABAC, antagonists, Receptors, SKF97541, CGP35024, CGP, 35024, GABAA-rho, 0379, Tocris Bioscience
8 Citations for SKF 97541
Citations are publications that use Tocris products. Selected citations for SKF 97541 include:
Ignell et al (2009) Presynaptic peptidergic modulation of olfactory receptor neurons in Drosophila. Br J Pharmacol 106 13070 PMID: 19625621
Root et al (2008) A presynaptic gain control mechanism fine-tunes olfactory behavior. Neuron 59 311 PMID: 18667158
Chen et al (2008) Differential regulation of mor. antinociceptive effects by endogenous enkephalinergic system in the forebrain of mice. Mol Pain 4 41 PMID: 18826595
Ki and Lim (2019) Sleep-promoting effects of threonine link amino acid metabolism in Drosophila neuron to GABAergic control of sleep drive. Elife 8 PMID: 31313987
Lecat-Guillet (2017) FRET-based sensors unravel activation and allosteric modulation of the GABAB receptor. Cell Chem Biol 24 360 PMID: 28286129
Martelli and Fiala (2019) Slow presynaptic mechanisms that mediate adaptation in the olfactory pathway of Drosophila. Elife 8 PMID: 31169499
Piqueras and Martínez (2004) Peripheral GABAB agonists stimulate gastric acid secretion in mice. Br J Pharmacol 142 1038 PMID: 15210585
Wood et al (2000) The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. Mol Pain 131 1050 PMID: 11082110
Do you know of a great paper that uses SKF 97541 from Tocris? Please let us know.
Reviews for SKF 97541
Average Rating: 4 (Based on 1 Review.)
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Test of potential modulation of 5HT-1B receptor effects.
By
Sergiy Sylantyev on 12/10/2023
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Arcuate nucleus
SKF 97541 was used to test a (potential) impact of GABA-B receptors on the effect of 5HT-1B receptors on neurotransmitter vesicle release in interneuronal synapse. Picture: membrane capacitance fluctuation of living neuron after series of electrical stimuli delivered to acute neural tissue. Left: control. Right: activation of GABA-B receptors (with 1 microM SKF 97541), mGlu receptors and ACh receptors do not show a significant effect. Grey traces: individual recordings; red: averaged trace.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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