DT-Web

DB00913 - Anileridine


Identification
Name Anileridine
Accession Number DB00913 (APRD00741)
Type small molecule
Description Anileridine is a synthetic opioid and strong analgesic medication. It is a narcotic pain reliever used to treat moderate to severe pain. Narcotic analgesics act in the central nervous system (CNS) to relieve pain. Some of their side effects are also caused by actions in the CNS.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 352.4699
Groups illicit
Monoisotopic Weight 352.21507815
Pharmacology
Indication For treatment and management of pain (systemic) and for use as an anesthesia adjunct.
Mechanism of action Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Opioids such as anileridine close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Absorption Anileridine is absorbed by all routes of administration.
Protein binding > 95%
Biotransformation Hepatic
Route of elimination Not Available
Toxicity Symptoms of overexposure include dizziness, perspiration, a feeling of warmth, dry mouth, visual difficulty, itching, euphoria, restlessness, nervousness and excitement have been reported.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions
  • Take without regard to meals.

Targets


Mu-type opioid receptor
Name Mu-type opioid receptor
Gene Name OPRM1
Pharmacological action yes
Actions agonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.44

Predictions


Id Partner name Gene Name Score
467 Delta-type opioid receptor OPRD1 0.2329
696 Kappa-type opioid receptor OPRK1 0.2156
4512 Cytochrome P450 3A4 CYP3A4 0.0398
4119 Cytochrome P450 2D6 CYP2D6 0.0383
1716 Tripartite motif-containing protein 13 TRIM13 0.0335
6107 Cytochrome P450 3A7 CYP3A7 0.0261
1262 Corticotropin-lipotropin POMC 0.0243
4118 Cytochrome P450 3A5 CYP3A5 0.0184
1588 Multidrug resistance protein 1 ABCB1 0.0157
174 Sigma 1-type opioid receptor SIGMAR1 0.0153
4137 Nociceptin receptor OPRL1 0.0113
4924 Cytochrome P450 2C8 CYP2C8 0.0106
4757 Cytochrome P450 2C9 CYP2C9 0.0104
319 Opioid receptor, sigma 1 OPRS1 0.01
6030 Cytochrome P450 2B6 CYP2B6 0.009
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0085
6180 UDP-glucuronosyltransferase 2B4 UGT2B4 0.0084
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0081
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.0072
6078 Neuronal acetylcholine receptor subunit beta-4 CHRNB4 0.0065
4120 NADPH--cytochrome P450 reductase POR 0.006
3811 Cytochrome P450 19A1 CYP19A1 0.0058
6079 Neuronal acetylcholine receptor subunit alpha-3 CHRNA3 0.0058
341 5-hydroxytryptamine 3 receptor HTR3A 0.0057
587 Serum albumin ALB 0.0051
824 Sodium-dependent serotonin transporter SLC6A4 0.0049
1291 cAMP response element-binding protein CREB1 0.0049
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0048
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0048
4210 Toll-like receptor 4 TLR4 0.0044
6016 Cytochrome P450 2C19 CYP2C19 0.0043
4200 Cytochrome P450 1A2 CYP1A2 0.0041
392 Voltage-dependent P/Q-type calcium channel subunit alpha-1A CACNA1A 0.004
1181 Alpha-1-acid glycoprotein 1 ORM1 0.004
6106 Cytochrome P450 2C18 CYP2C18 0.0038
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0037
94 5-hydroxytryptamine 4 receptor HTR4 0.0035
6181 UDP-glucuronosyltransferase 1-8 UGT1A8 0.0035
20 Prostaglandin G/H synthase 1 PTGS1 0.0029
465 Calmodulin CALM1 0.0028
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0026
885 5-hydroxytryptamine 1B receptor HTR1B 0.0025
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0025
6145 Solute carrier family 22 member 1 SLC22A1 0.0025
590 5-hydroxytryptamine 2C receptor HTR2C 0.0024
136 Estrogen receptor ESR1 0.0024
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0023
320 5-hydroxytryptamine 1A receptor HTR1A 0.0023
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0022
6013 Cytochrome P450 2E1 CYP2E1 0.0018
5718 Cytochrome P450 2A6 CYP2A6 0.0015
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0015
↑