General
Preferred name
CARFENTANIL
Synonyms
Carfentanil, C-11 ()
CARFENTANIL CITRATE ()
(4-carbomethoxy fentanyl) ()
R 31833 ()
Carfentanyl ()
4-carbomethoxyfentanyl ()
Carfentanil ()
[11C]-CARFENTANIL ()
R 33,799 ()
R-33799 ()
Carfentanil (CRM) ()
Carfentanil-13C6 (CRM) ()
P&D ID
PD008798
CAS
59708-52-0
98598-83-5
61380-27-6
Tags
available
drug candidate
drug
Drug Status
illicit
investigational
approved
vet_approved
Max Phase
Phase 2
Drug indication
Analgesic (narcotic)
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS
Carfentanil acts primarily on the mu (some kappa and delta) opioid receptors as an agonist. It will induce similar effects of analgesia as other opioids, however, due to its potency, it will also induce strong side effects such as sedation. Consequently, that is why it is used as a tranquilizer for large animals.; ; Carfentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the brain, spinal cord, and other tissues. It exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Carfentanil also depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
MOA
Carfentanil binds very strongly to mu opioid receptors and acts as a competitive agonist. ; 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 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.
DESCRIPTION
Carfentanil is an analogue of the synthetic opioid analgesic , but it is ~100 times more potent.
(GtoPdb)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
7
ChEMBL Drugs
DrugBank Approved Drugs
DrugMAP
DrugMatrix
Guide to Pharmacology
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
40
Molecular Weight
394.23
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
0
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
2
cLogP
3.68
TPSA
49.85
Fraction CSP3
0.42
Chiral centers
0.0
Largest ring
6.0
QED
0.67
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Source data
