Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T61972
|
||||
| Former ID |
TTDI03214
|
||||
| Target Name |
GABAB receptor
|
||||
| Target Type |
Research
|
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| Antagonist | 2-hydroxy-saclofen | Drug Info | [1] | ||
| CGP 46381 | Drug Info | [2] | |||
| CGP 54626A | Drug Info | [3] | |||
| CGP 55845 | Drug Info | [2] | |||
| CGP 62349 | Drug Info | [3] | |||
| saclofen | Drug Info | [3] | |||
| [125I]CGP 64213 | Drug Info | [4] | |||
| [125I]CGP 71872 | Drug Info | [1] | |||
| [3H]CGP 54626 | Drug Info | [5] | |||
| [3H]CGP 62349 | Drug Info | [6] | |||
| Agonist | amino-propylphosphinic acid | Drug Info | [7] | ||
| [3H](R)-(-)-baclofen | Drug Info | [7] | |||
| Modulator (allosteric modulator) | compound 14 | Drug Info | [8] | ||
| References | |||||
| REF 1 | Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors. Nature. 1997 Mar 20;386(6622):239-46. | ||||
| REF 2 | The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. Br J Pharmacol. 2000 Nov;131(6):1050-4. | ||||
| REF 3 | Pharmacological characterisation of a cell line expressing GABA B1b and GABA B2 receptor subunits. Biochem Pharmacol. 2003 Apr 1;65(7):1103-13. | ||||
| REF 4 | Ca(2+) requirement for high-affinity gamma-aminobutyric acid (GABA) binding at GABA(B) receptors: involvement of serine 269 of the GABA(B)R1 subunit. Mol Pharmacol. 2000 Mar;57(3):419-26. | ||||
| REF 5 | GABA(B) receptors function as a heteromeric assembly of the subunits GABA(B)R1 and GABA(B)R2. Nature. 1998 Dec 17;396(6712):674-9. | ||||
| REF 6 | Characterisation and partial purification of the GABA(B) receptor from the rat cerebellum using the novel antagonist [3H]CGP 62349. Brain Res Mol Brain Res. 1999 Aug 25;71(2):279-89. | ||||
| REF 7 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 242). | ||||
| REF 8 | Discovery of a Negative Allosteric Modulator of GABAB Receptors. ACS Med Chem Lett. 2014 May 27;5(7):742-7. | ||||
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