Target Information

Target General Infomation
Target ID
T27376
Former ID
TTDI01909
Target Name
GABA A receptor delta subunit
Gene Name
GABRD
Synonyms
GABA(A) receptor subunit delta; Gammaaminobutyric acid receptor subunit delta; GABRD
Target Type
Successful
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.
BioChemical Class
Ligand-gated ion channel
UniProt ID
O14764
Sequence
MDAPARLLAPLLLLCAQQLRGTRAMNDIGDYVGSNLEISWLPNLDGLIAGYARNFRPGIG
GPPVNVALALEVASIDHISEANMEYTMTVFLHQSWRDSRLSYNHTNETLGLDSRFVDKLW
LPDTFIVNAKSAWFHDVTVENKLIRLQPDGVILYSIRITSTVACDMDLAKYPMDEQECML
DLESYGYSSEDIVYYWSESQEHIHGLDKLQLAQFTITSYRFTTELMNFKSAGQFPRLSLH
FHLRRNRGVYIIQSYMPSVLLVAMSWVSFWISQAAVPARVSLGITTVLTMTTLMVSARSS
LPRASAIKALDVYFWICYVFVFAALVEYAFAHFNADYRKKQKAKVKVSRPRAEMDVRNAI
VLFSLSAAGVTQELAISRRQRRVPGNLMGSYRSVGVETGETKKEGAARSGGQGGIRARLR
PIDADTIDIYARAVFPAAFAAVNVIYWAAYAM
Drugs and Mode of Action
Drug(s) Gaboxadol Drug Info Approved Insomnia [467660], [537521]
Ganaxolone Drug Info Phase 2 Epilepsy [536934]
PF-4480682 Drug Info Discontinued in Phase 2 Neuropathic pain [548430]
PF-2393296 Drug Info Discontinued in Phase 1 Neuropathic pain [548716]
Co-60549 Drug Info Terminated Anxiety disorder [546228]
Org-20599 Drug Info Terminated Anesthesia [545545]
Modulator Co-60549 Drug Info [546229]
Gaboxadol Drug Info
Ganaxolone Drug Info
Org-20599 Drug Info [534312]
PF-4480682 Drug Info [550179]
RU-5135 Drug Info
Agonist PF-2393296 Drug Info [543815]
Blocker (channel blocker) TBPS Drug Info [543815]
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 467660(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 536934Progress 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 537521Highway 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 545545Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003651)
Ref 546228Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007012)
Ref 548430Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025530)
Ref 548716Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027949)
Ref 534312The anaesthetic action and modulation of GABAA receptor activity by the novel water-soluble aminosteroid Org 20599. Neuropharmacology. 1996;35(9-10):1209-22.
Ref 543815(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).
Ref 546229Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007012)
Ref 550179WO patent application no. 2014,1515,17, Methods of improving microvascular integrity.

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