| Compound Code | KAT-SED-02 |
| Pharmacological Tag | Sedative antihistamine / Anticholinergic / Hypnotic |
| Structural Class | Ethanolamine H1 receptor inreverse agonist |
| Mechanism |
H1 receptor inverse agonist
Central histamine suppression
Muscarinic receptor blockade (anticholinergic load)
Mild serotonergic modulation (non-primary)
|
| Functional Role |
Sleep induction
Antiemetic (in combination with Vitamin B1)
|
| Structural Analogues |
Diphenhydramine
Promethazine
Carbinoxamine
Other first-generation ethanolamines
|
| Onset | ~30 minutes (oral) |
| Duration | 6–10 hours |
| Affinity Profile |
High CNS penetration
Strong H1 antagonism
Moderate muscarinic antagonism
Minimal selective receptor precision (dirty drug)
|
| Pharmacokinetics |
Oral bioavailability: high
Peak plasma: 2-3h
Half-life: ~10-12h
Hepatic metabolism
Renal elimination
|
| Secondary effects |
Somnolence
Dry mouth
Blurred vision
Cognitive slowing
Paradoxical excitation
|
| Interpretation |
Pre-receptor era sedative architecture
Histamine shutdown in behavioural control
Anticholinergic as therapeutic relevant
Legacy molecule still in use on modern insomnia
|