|Accession Number||DB00913 (APRD00741)|
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.
|Approved Prescription Products|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|Brand mixtures||Not Available|
|Weight||Average: 352.4699 |
For treatment and management of pain (systemic) and for use as an anesthesia adjunct.
|Structured Indications||Not Available|
Anileridine, a potent analgesic, is an analog of pethidine. Anileridine is useful for the relief of moderate to severe pain. It may also be used as an analgesic adjunct in general anesthesia in the same manner as meperidine to reduce the amount of anesthetic needed, to facilitate relaxation, and to reduce laryngospasm. In addition, anileridine exerts mild antihistaminic, spasmolytic and antitussive effects. Anileridine's main pharmacologic action is exerted on the CNS. Respiratory depression, when it occurs, is of shorter duration than that seen with morphine or meperidine when equipotent analgesic doses are used.
|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.
Anileridine is absorbed by all routes of administration.
|Volume of distribution||Not Available|
|Route of elimination||Not Available|
|Half life||Not Available|
Symptoms of overexposure include dizziness, perspiration, a feeling of warmth, dry mouth, visual difficulty, itching, euphoria, restlessness, nervousness and excitement have been reported.
|Pharmacogenomic Effects/ADRs||Not Available|
|Drug Interactions||Not Available|
Weijlard, J.and Pfister, K., Ill; US. Patent 2,966,490; December 27, 1960; assigned to Merck & Co., Inc.
|General References||Not Available|
|ATC Codes||N01AH05 — Anileridine|
|AHFS Codes||Not Available|
|PDB Entries||Not Available|
|FDA label||Not Available|
|Clinical Trials||Not Available|
|Predicted ADMET features|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of chemical entities known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.|
|Super Class||Organic compounds|
|Alternative Parents||Piperidinecarboxylic acids / Phenethylamines / Aniline and substituted anilines / Aralkylamines / Primary aromatic amines / Trialkylamines / Carboxylic acid esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds|
|Substituents||Phenylpiperidine / Phenethylamine / Piperidinecarboxylic acid / Aniline or substituted anilines / Aralkylamine / Monocyclic benzene moiety / Primary aromatic amine / Benzenoid / Amino acid or derivatives / Carboxylic acid ester/ Tertiary amine / Tertiary aliphatic amine / Monocarboxylic acid or derivatives / Carboxylic acid derivative / Azacycle / Primary amine / Organic oxide / Organopnictogen compound / Organic oxygen compound / Organooxygen compound / Organonitrogen compound / Amine / Carbonyl group / Hydrocarbon derivative / Organic nitrogen compound / Aromatic heteromonocyclic compound|
|Molecular Framework||Aromatic heteromonocyclic compounds|
|External Descriptors||ethyl ester, substituted aniline, piperidinecarboxylate ester (CHEBI:61203 )|
- Pharmacological action
- General Function:
- Voltage-gated calcium channel activity
- Specific Function:
- Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociati...
- Gene Name:
- Uniprot ID:
- Uniprot Name:
- Mu-type opioid receptor
- Molecular Weight:
- 44778.855 Da
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