Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T27376
|
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| Former ID |
TTDI01909
|
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| Target Name |
GABA A receptor delta subunit
|
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| Gene Name |
GABRD
|
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| Synonyms |
GABA(A) receptor subunit delta; Gammaaminobutyric acid receptor subunit delta; GABRD
|
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| Target Type |
Successful
|
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| Disease | Anesthesia [ICD9: 338; ICD10: R20.0] | ||||
| Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42] | |||||
| Epilepsy [ICD10: G40] | |||||
| Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0] | |||||
| Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0] | |||||
| Unspecified [ICD code not available] | |||||
| Function |
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
|
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| BioChemical Class |
Ligand-gated ion channel
|
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| UniProt ID | |||||
| Sequence |
MDAPARLLAPLLLLCAQQLRGTRAMNDIGDYVGSNLEISWLPNLDGLIAGYARNFRPGIG
GPPVNVALALEVASIDHISEANMEYTMTVFLHQSWRDSRLSYNHTNETLGLDSRFVDKLW LPDTFIVNAKSAWFHDVTVENKLIRLQPDGVILYSIRITSTVACDMDLAKYPMDEQECML DLESYGYSSEDIVYYWSESQEHIHGLDKLQLAQFTITSYRFTTELMNFKSAGQFPRLSLH FHLRRNRGVYIIQSYMPSVLLVAMSWVSFWISQAAVPARVSLGITTVLTMTTLMVSARSS LPRASAIKALDVYFWICYVFVFAALVEYAFAHFNADYRKKQKAKVKVSRPRAEMDVRNAI VLFSLSAAGVTQELAISRRQRRVPGNLMGSYRSVGVETGETKKEGAARSGGQGGIRARLR PIDADTIDIYARAVFPAAFAAVNVIYWAAYAM |
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| Drugs and Mode of Action | |||||
| Drug(s) | Gaboxadol | Drug Info | Approved | Insomnia | [1], [2] |
| Ganaxolone | Drug Info | Phase 2 | Epilepsy | [3] | |
| PF-4480682 | Drug Info | Discontinued in Phase 2 | Neuropathic pain | [4] | |
| PF-2393296 | Drug Info | Discontinued in Phase 1 | Neuropathic pain | [5] | |
| Co-60549 | Drug Info | Terminated | Anxiety disorder | [6] | |
| Org-20599 | Drug Info | Terminated | Anesthesia | [7] | |
| Modulator | Co-60549 | Drug Info | [8] | ||
| Gaboxadol | Drug Info | ||||
| Ganaxolone | Drug Info | ||||
| Org-20599 | Drug Info | [9] | |||
| PF-4480682 | Drug Info | [10] | |||
| RU-5135 | Drug Info | ||||
| Agonist | PF-2393296 | Drug Info | [11] | ||
| Blocker (channel blocker) | TBPS | Drug Info | [11] | ||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
| Retrograde endocannabinoid signaling | |||||
| GABAergic synapse | |||||
| Morphine addiction | |||||
| Nicotine addiction | |||||
| References | |||||
| REF 1 | (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. (Ligand id: 4322). | ||||
| REF 2 | Highway driving performance and cognitive functioning the morning after bedtime and middle-of-the-night use of gaboxadol, zopiclone and zolpidem. J Sleep Res. 2009 Jun 22. | ||||
| REF 3 | Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43. Epub 2008 Nov 12. | ||||
| REF 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025530) | ||||
| REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027949) | ||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007012) | ||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003651) | ||||
| REF 8 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007012) | ||||
| REF 9 | The anaesthetic action and modulation of GABAA receptor activity by the novel water-soluble aminosteroid Org 20599. Neuropharmacology. 1996;35(9-10):1209-22. | ||||
| REF 10 | WO patent application no. 2014,1515,17, Methods of improving microvascular integrity. | ||||
| REF 11 | (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: 416). | ||||
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