| Version |
1.0 |
| Creation Date |
2009-07-21 20:27:27 |
| Update Date |
2010-05-18 21:00:29 |
| Accession Number |
T3D2864 |
| Name |
Naltrexone |
| Compound Type |
- Alcohol Antagonist
- Anti-Craving Agent
- Depressant
- Drug
- Narcotic Antagonist
- Opiate Antagonist
|
| Description |
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of naloxone. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence. [PubChem] |
| Synonyms |
- naltrexone
|
| Chemical IUPAC Name |
4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7,9,11(18)-trien-14-one |
| Chemical Formula |
C20H23NO4 |
| Chemical Structure |
 |
| CAS Registry Number |
16590-41-3 |
| InChI Identifier |
InChI=1S/C20H23NO4/c22-13-4-3-12-9-15-20(24)6-5-14(23)18-19(20,16(12)17(13)25-18)7-8-21(15)10-11-1-2-11/h3-4,11,15,18,22,24H,1-2,5-10H2 |
| InChI Key |
InChIKey=DQCKKXVULJGBQN-UHFFFAOYSA-N |
| PubChem Compound ID |
5360515  |
| KEGG ID |
C07253  |
| UniProt ID |
Not Available |
| OMIM ID |
Not Available |
| ChEBI ID |
Not Available |
| BioCyc ID |
Not Available |
| SuperToxic ID |
Not Available |
| CTD ID |
Not Available |
| Stitch ID |
Naltrexone  |
| DrugBank ID |
DB00704  |
| PDB ID |
Not Available |
| ACToR ID |
Not Available |
| Wikipedia Link |
http://en.wikipedia.org/wiki/Naltrexone  |
| Monoisotopic Mass |
341.162708 |
| MOL File |
Show |
| PDB File |
Show |
| SDF File |
Show |
| SMILES |
OC1=CC=C2CC3N(CC4CC4)CCC45C(OC1=C24)C(=O)CCC35O |
| Appearance |
Not Available |
| Melting Point |
169-170 oC (274-276 oC for hydrochloride salt) |
| Solubility |
100 mg/mL (as hydrochloride salt) |
| Predicted LogP |
1.361 |
| Route of Exposure |
Oral |
| Mechanism of Action |
Naltrexone binds to the opioid mu receptor antagonistically, thereby preventing conventional opiate (heroin, morphine) drugs from binding and inducing opioid neural responses. The mechanism of action of naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. |
| Metabolism |
Hepatic. When administered orally, naltrexone undergoes extensive biotransformation and is metabolized to 6 beta-naltrexol (which may contribute to the therapeutic effect) and other minor metabolites. |
| Toxicity Values |
LD50: 1,100-1,550 mg/kg (oral, mouse)
LD50: 1,450 mg/kg (oral, rat)
LD50: 1,490 mg/kg (oral, guinea pig) |
| Lethal Dose |
Not Available |
| Carcinogenicity (IARC Classification) |
Not Available |
| Uses/Sources |
Used as an emmergency antidote, and for the treatment of alcohol dependence. [Wikipedia][PubChem] |
| Minimum Risk Level |
Not Available |
| Health Effects |
Tolerance can develop, in which the person needs larger doses to achieve the desired effect; this can lead to overdose and death. Accidents or injury can also occur due to the side effects of loss of coordination, slowed reaction time, sleepiness and impaired judgment. Drugs in this category have a high potential for physical and psychological dependence. |
| Symptoms |
High doses of naltrexone (generally ?1,000 mg/kg) produce salivation, depression/reduced activity, tremors, and convulsions. |
| Treatment |
Patients should be treated symptomatically in a closely supervised environment. (V650) |
| General References |
- U207 - Drugs.com
- U208 - Schmitz JM, Stotts AL, Rhoades HM, Grabowski J: Naltrexone and relapse prevention treatment for cocaine-dependent patients. Addict Behav. 2001 Mar-Apr;26(2):167-80. [PubMed
]
|
| Targets |
- Mu-type opioid receptor
- Tumor necrosis factor
- Kappa-type opioid receptor
- Delta-type opioid receptor
|
|
Target 1
[top]
|
| Target 1 ID |
1155 |
| Target 1 Name |
Mu-type opioid receptor |
| Target 1 Mechanism of Action |
Naltrexone binds to the opioid mu receptor antagonistically, thereby preventing conventional opiate (heroin, morphine) drugs from binding and inducing opioid neural responses. The mechanism of action of naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. |
| Target 1 Description |
Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for beta-endorphin |
| Target 1 Synonyms |
- MOR-1
|
| Target 1 Gene Name |
OPRM1 |
| Target 1 Protein Sequence |
>Mu-type opioid receptor
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP
PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT
STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF
RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI
FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI
YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI
EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
|
| Target 1 Number of Residues |
400 |
| Target 1 Molecular Weight |
44778.9 |
| Target 1 Theoretical pI |
8.29 |
| Target 1 GO Classification |
|
Function
|
peptide receptor activity, G-protein coupled
opioid receptor activity
mu-opioid receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 1 General Function |
Involved in mu-opioid receptor activity |
| Target 1 Pathways |
Not Available |
| Target 1 Reactions |
Not Available |
| Target 1 Signals |
|
| Target 1 Transmembrane Regions |
- 67-96
- 106-123
- 146-165
- 196-211
- 237-259
- 283-305
- 314-330
|
| Target 1 Essentiality |
Non Essential |
| Target 1 Domain Function |
PF00001:7tm_1 |
| Target 1 GenBank ID Protein |
Not Available |
| Target 1 UniProtKB ID |
P35372  |
| Target 1 Cellular Location |
Cell membrane |
| Target 1 Gene Sequence |
>1203 bp
ATGGACAGCAGCGCTGCCCCCACGAACGCCAGCAATTGCACTGATGCCTTGGCGTACTCA
AGTTGCTCCCCAGCACCCAGCCCCGGTTCCTGGGTCAACTTGTCCCACTTAGATGGCAAC
CTGTCCGACCCATGCGGTCCGAACCGCACCAACCTGGGCGGGAGAGACAGCCTGTGCCCT
CCGACCGGCAGTCCCTCCATGATCACGGCCATCACGATCATGGCCCTCTACTCCATCGTG
TGCGTGGTGGGGCTCTTCGGAAACTTCCTGGTCATGTATGTGATTGTCAGATACACCAAG
ATGAAGACTGCCACCAACATCTACATTTTCAACCTTGCTCTGGCAGATGCCTTAGCCACC
AGTACCCTGCCCTTCCAGAGTGTGAATTACCTAATGGGAACATGGCCATTTGGAACCATC
CTTTGCAAGATAGTGATCTCCATAGATTACTATAACATGTTCACCAGCATATTCACCCTC
TGCACCATGAGTGTTGATCGATACATTGCAGTCTGCCACCCTGTCAAGGCCTTAGATTTC
CGTACTCCCCGAAATGCCAAAATTATCAATGTCTGCAACTGGATCCTCTCTTCAGCCATT
GGTCTTCCTGTAATGTTCATGGCTACAACAAAATACAGGCAAGGTTCCATAGATTGTACA
CTAACATTCTCTCATCCAACCTGGTACTGGGAAAACCTCGTGAAGATCTGTGTTTTCATC
TTCGCCTTCATTATGCCAGTGCTCATCATTACCGTGTGCTATGGACTGATGATCTTGCGC
CTCAAGAGTGTCCGCATGCTCTCTGGCTCCAAAGAAAAGGACAGGAATCTTCGAAGGATC
ACCAGGATGGTGCTGGTGGTGGTGGCTGTGTTCATCGTCTGCTGGACTCCCATTCACATT
TACGTCATCATTAAAGCCTTGGTTACAATCCCAGAAACTACGTTCCAGACTGTTTCTTGG
CACTTCTGCATTGCTCTAGGTTACACAAACAGCTGCCTCAACCCAGTCCTTTATGCATTT
CTGGATGAAAACTTCAAACGATGCTTCAGAGAGTTCTGTATCCCAACCTCTTCCAACATT
GAGCAACAAAACTCCACTCGAATTCGTCAGAACACTAGAGACCACCCCTCCACGGCCAAT
ACAGTGGATAGAACTAATCATCAGCTAGAAAATCTGGAAGCAGAAACTGCTCCGTTGCCC
TAA
|
| Target 1 GenBank Gene ID |
Not Available |
| Target 1 GeneCard ID |
OPRM1  |
| Target 1 GenAtlas ID |
OPRM1  |
| Target 1 HGNC ID |
HGNC:8156  |
| Target 1 Chromosome Location |
Not Available |
| Target 1 Locus |
6q24-q25 |
| Target 1 SNPs |
SNPJam Report  |
| Target 1 Toxin References |
- S918 - Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
- U212 - Oslin DW, Berrettini W, Kranzler HR, Pettinati H, Gelernter J, Volpicelli JR, O'Brien CP: A functional polymorphism of the mu-opioid receptor gene is associated with naltrexone response in alcohol-dependent patients. Neuropsychopharmacology. 2003 Aug;28(8):1546-52. Epub 2003 Jun 18. [PubMed
]
- U214 - Yoburn BC, Purohit V, Patel K, Zhang Q: Opioid agonist and antagonist treatment differentially regulates immunoreactive mu-opioid receptors and dynamin-2 in vivo. Eur J Pharmacol. 2004 Sep 13;498(1-3):87-96. [PubMed
]
- U213 - Bartus RT, Emerich DF, Hotz J, Blaustein M, Dean RL, Perdomo B, Basile AS: Vivitrex, an injectable, extended-release formulation of naltrexone, provides pharmacokinetic and pharmacodynamic evidence of efficacy for 1 month in rats. Neuropsychopharmacology. 2003 Nov;28(11):1973-82. [PubMed
]
- U215 - Roy S, Guo X, Kelschenbach J, Liu Y, Loh HH: In vivo activation of a mutant mu-opioid receptor by naltrexone produces a potent analgesic effect but no tolerance: role of mu-receptor activation and delta-receptor blockade in morphine tolerance. J Neurosci. 2005 Mar 23;25(12):3229-33. [PubMed
]
|
| Target 1 General References |
7905839; 7957926; 7891175; 12589820; 15893644; 19077058; 14702039 |
|
Target 2
[top]
|
| Target 2 ID |
142 |
| Target 2 Name |
Tumor necrosis factor |
| Target 2 Mechanism of Action |
Naltrexone binds to the opioid mu receptor antagonistically, thereby preventing conventional opiate (heroin, morphine) drugs from binding and inducing opioid neural responses. The mechanism of action of naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. |
| Target 2 Description |
Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct action or by stimulation of interleukin-1 secretion and is implicated in the induction of cachexia, Under certain conditions it can stimulate cell proliferation and induce cell differentiation |
| Target 2 Synonyms |
- TNF-alpha; Tumor necrosis factor ligand superfamily member 2; TNF-a; Cachectin; Tumor necrosis factor, membrane form; Tumor necrosis factor, soluble form
|
| Target 2 Gene Name |
TNF |
| Target 2 Protein Sequence |
>Tumor necrosis factor
MSTESMIRDVELAEEALPKKTGGPQGSRRCLFLSLFSFLIVAGATTLFCLLHFGVIGPQR
EEFPRDLSLISPLAQAVRSSSRTPSDKPVAHVVANPQAEGQLQWLNRRANALLANGVELR
DNQLVVPSEGLYLIYSQVLFKGQGCPSTHVLLTHTISRIAVSYQTKVNLLSAIKSPCQRE
TPEGAEAKPWYEPIYLGGVFQLEKGDRLSAEINRPDYLDFAESGQVYFGIIAL
|
| Target 2 Number of Residues |
233 |
| Target 2 Molecular Weight |
25644.1 |
| Target 2 Theoretical pI |
6.92 |
| Target 2 GO Classification |
|
Function
|
signal transducer activity
receptor binding
cytokine activity
tumor necrosis factor receptor binding |
|
Process
|
response to stimulus
response to biotic stimulus
defense response
immune response |
|
Component
|
cell
membrane |
|
| Target 2 General Function |
Involved in cytokine activity |
| Target 2 Pathways |
REACT_578-Apoptosis; |
| Target 2 Reactions |
Not Available |
| Target 2 Signals |
|
| Target 2 Transmembrane Regions |
|
| Target 2 Essentiality |
Non Essential |
| Target 2 Domain Function |
PF00229:TNF |
| Target 2 GenBank ID Protein |
Not Available |
| Target 2 UniProtKB ID |
P01375  |
| Target 2 Cellular Location |
Tumor necrosis factor, soluble form:Secreted |
| Target 2 Gene Sequence |
>702 bp
ATGAGCACTGAAAGCATGATCCGGGACGTGGAGCTGGCCGAGGAGGCGCTCCCCAAGAAG
ACAGGGGGGCCCCAGGGCTCCAGGCGGTGCTTGTTCCTCAGCCTCTTCTCCTTCCTGATC
GTGGCAGGCGCCACCACGCTCTTCTGCCTGCTGCACTTTGGAGTGATCGGCCCCCAGAGG
GAAGAGTTCCCCAGGGACCTCTCTCTAATCAGCCCTCTGGCCCAGGCAGTCAGATCATCT
TCTCGAACCCCGAGTGACAAGCCTGTAGCCCATGTTGTAGCAAACCCTCAAGCTGAGGGG
CAGCTCCAGTGGCTGAACCGCCGGGCCAATGCCCTCCTGGCCAATGGCGTGGAGCTGAGA
GATAACCAGCTGGTGGTGCCATCAGAGGGCCTGTACCTCATCTACTCCCAGGTCCTCTTC
AAGGGCCAAGGCTGCCCCTCCACCCATGTGCTCCTCACCCACACCATCAGCCGCATCGCC
GTCTCCTACCAGACCAAGGTCAACCTCCTCTCTGCCATCAAGAGCCCCTGCCAGAGGGAG
ACCCCAGAGGGGGCTGAGGCCAAGCCCTGGTATGAGCCCATCTATCTGGGAGGGGTCTTC
CAGCTGGAGAAGGGTGACCGACTCAGCGCTGAGATCAATCGGCCCGACTATCTCGACTTT
GCCGAGTCTGGGCAGGTCTACTTTGGGATCATTGCCCTGTGA
|
| Target 2 GenBank Gene ID |
Not Available |
| Target 2 GeneCard ID |
TNF  |
| Target 2 GenAtlas ID |
TNF  |
| Target 2 HGNC ID |
HGNC:11892  |
| Target 2 Chromosome Location |
Not Available |
| Target 2 Locus |
6p21.3 |
| Target 2 SNPs |
SNPJam Report  |
| Target 2 Toxin References |
- U209 - Greeneltch KM, Haudenschild CC, Keegan AD, Shi Y: The opioid antagonist naltrexone blocks acute endotoxic shock by inhibiting tumor necrosis factor-alpha production. Brain Behav Immun. 2004 Sep;18(5):476-84. [PubMed
]
- U210 - Lin SL, Lee YM, Chang HY, Cheng YW, Yen MH: Effects of naltrexone on lipopolysaccharide-induced sepsis in rats. J Biomed Sci. 2005;12(2):431-40. [PubMed
]
- U211 - Davis RL, Buck DJ, Saffarian N, Stevens CW: The opioid antagonist, beta-funaltrexamine, inhibits chemokine expression in human astroglial cells. J Neuroimmunol. 2007 May;186(1-2):141-9. Epub 2007 May 1. [PubMed
]
|
| Target 2 General References |
3555974; 6392892; 3883195; 2995927; 3856324; 3932069; 8499947; 10202016; 14656967 |
|
Target 3
[top]
|
| Target 3 ID |
959 |
| Target 3 Name |
Kappa-type opioid receptor |
| Target 3 Mechanism of Action |
Naltrexone binds to the opioid mu receptor antagonistically, thereby preventing conventional opiate (heroin, morphine) drugs from binding and inducing opioid neural responses. The mechanism of action of naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. |
| Target 3 Description |
Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for dynorphins. May play a role in arousal and regulation of autonomic and neuroendocrine functions |
| Target 3 Synonyms |
- KOR-1
|
| Target 3 Gene Name |
OPRK1 |
| Target 3 Protein Sequence |
>Kappa-type opioid receptor
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV
|
| Target 3 Number of Residues |
380 |
| Target 3 Molecular Weight |
42644.7 |
| Target 3 Theoretical pI |
7.79 |
| Target 3 GO Classification |
|
Function
|
peptide receptor activity, G-protein coupled
opioid receptor activity
kappa-opioid receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 3 General Function |
Involved in kappa-opioid receptor activity |
| Target 3 Pathways |
Not Available |
| Target 3 Reactions |
Not Available |
| Target 3 Signals |
|
| Target 3 Transmembrane Regions |
- 59-85
- 96-117
- 133-154
- 174-196
- 223-247
- 276-299
- 312-333
|
| Target 3 Essentiality |
Non Essential |
| Target 3 Domain Function |
PF00001:7tm_1 |
| Target 3 GenBank ID Protein |
Not Available |
| Target 3 UniProtKB ID |
P41145  |
| Target 3 Cellular Location |
Cell membrane |
| Target 3 Gene Sequence |
>1143 bp
ATGGAATCCCCGATTCAGATCTTCCGCGGGGAGCCTGGCCCTACCTGCGCCCCGAGCGCC
TGCCTGCCCCCCAACAGCAGCGCCTGGTTTCCCGGCTGGGCCGAGCCCGACAGCAACGGC
AGCGCCGGCTCGGAGGACGCGCAGCTGGAGCCCGCGCACATCTCCCCGGCCATCCCGGTC
ATCATCACGGCGGTCTACTCCGTAGTGTTCGTCGTGGGCTTGGTGGGCAACTCGCTGGTC
ATGTTCGTGATCATCCGATACACAAAGATGAAGACAGCAACCAACATTTACATATTTAAC
CTGGCTTTGGCAGATGCTTTAGTTACTACAACCATGCCCTTTCAGAGTACGGTCTACTTG
ATGAATTCCTGGCCTTTTGGGGATGTGCTGTGCAAGATAGTAATTTCCATTGATTACTAC
AACATGTTCACCAGCATCTTCACCTTGACCATGATGAGCGTGGACCGCTACATTGCCGTG
TGCCACCCCGTGAAGGCTTTGGACTTCCGCACACCCTTGAAGGCAAAGATCATCAATATC
TGCATCTGGCTGCTGTCGTCATCTGTTGGCATCTCTGCAATAGTCCTTGGAGGCACCAAA
GTCAGGGAAGACGTCGATGTCATTGAGTGCTCCTTGCAGTTCCCAGATGATGACTACTCC
TGGTGGGACCTCTTCATGAAGATCTGCGTCTTCATCTTTGCCTTCGTGATCCCTGTCCTC
ATCATCATCGTCTGCTACACCCTGATGATCCTGCGTCTCAAGAGCGTCCGGCTCCTTTCT
GGCTCCCGAGAGAAAGATCGCAACCTGCGTAGGATCACCAGACTGGTCCTGGTGGTGGTG
GCGGTTTTCGTCGTCTGCTGGACTCCCATTCACATATTCATCCTGGTGGAGGCTCTGGGG
AGCACCTCCCACAGCACAGCTGCTCTCTCCAGCTATTACTTCTGCATCGCCTTAGGCTAT
ACCAACAGTAGCCTGAATCCCATTCTCTACGCCTTTCTTGATGAAAACTTCAAGCGGTGT
TTCCGGGACTTCTGCTTTCCACTGAAGATGAGGATGGAGCGGCAGAGCACTAGCAGAGTC
CGAAATACAGTTCAGGATCCTGCTTACCTGAGGGACATCGATGGGATGAATAAACCAGTA
TGA
|
| Target 3 GenBank Gene ID |
Not Available |
| Target 3 GeneCard ID |
OPRK1  |
| Target 3 GenAtlas ID |
OPRK1  |
| Target 3 HGNC ID |
HGNC:8154  |
| Target 3 Chromosome Location |
Not Available |
| Target 3 Locus |
8q11.2 |
| Target 3 SNPs |
SNPJam Report  |
| Target 3 Toxin References |
- S918 - Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
|
| Target 3 General References |
8060324; 7624359; 7869844; 15489334; 7929306; 12004055; 16431922; 17711303 |
|
Target 4
[top]
|
| Target 4 ID |
1185 |
| Target 4 Name |
Delta-type opioid receptor |
| Target 4 Mechanism of Action |
Naltrexone binds to the opioid mu receptor antagonistically, thereby preventing conventional opiate (heroin, morphine) drugs from binding and inducing opioid neural responses. The mechanism of action of naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. |
| Target 4 Description |
Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Highly stereoselective. receptor for enkephalins |
| Target 4 Synonyms |
- DOR-1
|
| Target 4 Gene Name |
OPRD1 |
| Target 4 Protein Sequence |
>Delta-type opioid receptor
MEPAPSAGAELQPPLFANASDAYPSAFPSAGANASGPPGARSASSLALAIAITALYSAVC
AVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL
CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG
VPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL
RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAAL
HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTAC
TPSDGPGGGAAA
|
| Target 4 Number of Residues |
372 |
| Target 4 Molecular Weight |
40412.3 |
| Target 4 Theoretical pI |
9.17 |
| Target 4 GO Classification |
|
Function
|
peptide receptor activity, G-protein coupled
opioid receptor activity
delta-opioid receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 4 General Function |
Involved in delta-opioid receptor activity |
| Target 4 Pathways |
Not Available |
| Target 4 Reactions |
Not Available |
| Target 4 Signals |
|
| Target 4 Transmembrane Regions |
- 46-75
- 85-102
- 125-144
- 175-190
- 216-238
- 262-284
- 294-310
|
| Target 4 Essentiality |
Non Essential |
| Target 4 Domain Function |
PF00001:7tm_1 |
| Target 4 GenBank ID Protein |
Not Available |
| Target 4 UniProtKB ID |
P41143  |
| Target 4 Cellular Location |
Cell membrane |
| Target 4 Gene Sequence |
>1119 bp
ATGGAACCGGCCCCCTCCGCCGGCGCCGAGCTGCAGCCCCCGCTCTTCGCCAACGCCTCG
GACGCCTACCCTAGCGCCTTCCCCAGCGCTGGCGCCAATGCGTCGGGGCCGCCAGGCGCG
CGGAGCGCCTCGTCCCTCGCCCTGGCAATCGCCATCACCGCGCTCTACTCGGCCGTGTGC
GCCGTGGGGCTGCTGGGCAACGTGCTTGTCATGTTCGGCATCGTCCGGTACACTAAGATG
AAGACGGCCACCAACATCTACATCTTCAACCTGGCCTTAGCCGATGCGCTGGCCACCAGC
ACGCTGCCTTTCCAGAGTGCCAAGTACCTGATGGAGACGTGGCCCTTCGGCGAGCTGCTC
TGCAAGGCTGTGCTCTCCATCGACTACTACAATATGTTCACCAGCATCTTCACGCTCACC
ATGATGAGTGTTGACCGCTACATCGCTGTCTGCCACCCTGTCAAGGCCCTGGACTTCCGC
ACGCCTGCCAAGGCCAAGCTGATCAACATCTGTATCTGGGTCCTGGCCTCAGGCGTTGGC
GTGCCCATCATGGTCATGGCTGTGACCCGTCCCCGGGACGGGGCAGTGGTGTGCATGCTC
CAGTTCCCCAGCCCCAGCTGGTACTGGGACACGGTGACCAAGATCTGCGTGTTCCTCTTC
GCCTTCGTGGTGCCCATCCTCATCATCACCGTGTGCTATGGCCTCATGCTGCTGCGCCTG
CGCAGTGTGCGCCTGCTGTCGGGCTCCAAGGAGAAGGACCGCAGCCTGCGGCGCATCACG
CGCATGGTGCTGGTGGTTGTGGGCGCCTTCGTGGTGTGTTGGGCGCCCATCCACATCTTC
GTCATCGTCTGGACGCTGGTGGACATCGACCGGCGCGACCCGCTGGTGGTGGCTGCGCTG
CACCTGTGCATCGCGCTGGGCTACGCCAATAGCAGCCTCAACCCCGTGCTCTACGCTTTC
CTCGACGAGAACTTCAAGCGCTGCTTCCGCCAGCTCTGCCGCAAGCCCTGCGGCCGCCCA
GACCCCAGCAGCTTCAGCCGCGCCCGCGAAGCCACGGCCCGCGAGCGTGTCACCGCCTGC
ACCCCGTCCGATGGTCCCGGCGGTGGCGCTGCCGCCTGA
|
| Target 4 GenBank Gene ID |
Not Available |
| Target 4 GeneCard ID |
OPRD1  |
| Target 4 GenAtlas ID |
OPRD1  |
| Target 4 HGNC ID |
HGNC:8153  |
| Target 4 Chromosome Location |
Not Available |
| Target 4 Locus |
1p36.1-p34.3 |
| Target 4 SNPs |
SNPJam Report  |
| Target 4 Toxin References |
- S918 - Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed
]
|
| Target 4 General References |
8201839; 7808419; 16710414; 12142540; 15086532; 10982041; 12847517 |