Name | trimipramine maleate |
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Synonyms |
5H-Dibenz[b,f]azepine-5-propanamine, 10,11-dihydro-N,N,β-trimethyl-, (2Z)-2-butenedioate (1:1)
UNII:269K6498LD Trimipramine maleate (Z)-but-2-enedioic acid,3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N,2-trimethylpropan-1-amine Trimipramine maleate salt UNII:D28E1043W5 3-(10,11-Dihydro-5H-dibenzo[b,f]azepin-5-yl)-N,N,2-trimethylpropan-1-amine (2Z)-but-2-enedioate (1:1) Trimipramine 3-(10,11-Dihydro-5H-dibenzo[b,f]azepin-5-yl)-N,N,2-trimethyl-1-propanamine (2Z)-2-butenedioate (1:1) UNII:I412286V22 |
Description | Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. |
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Related Catalog | |
Target |
5-HT1C Receptor:6.39 (pKi) 5-HT2 Receptor:8.10 (pKi) 5-HT1A Receptor:4.66 (pKi) |
In Vitro | Trimipramine displays much higher affinity for 5-HT2 than for 5-HT1C receptors[1]. |
In Vivo | The chronic administration of Trimipramine (5 mg/kg/day), as delivered by the osmotic minipump in 14 days produce significant increases in the regional concentration of 5-HT. The increases are highest in the frontal cortex and the hippocampus, followed by the olfactory tubercles and the hypothalamus. The Trimipramine treatment also produces marked increases in brain 5-HIAA concentrations ranging from 63% in the hippocampus to 25% in the nucleus accumbens with intermediate values for the hypothalamus, olfactory tubercles, frontal cortex and nucleus accumbens. Trimipramine treatment produces significant increases in DA concentrations in the nucleus accumbens, striaturn, and olfactory tubercles reaching 43, 21 and 11% respectively. Chronic administration of Trimipramine produces a marked reduction in the number of frontal cortex 5-HT2 and striatal DA D2 receptors. The chronic administration of Trimipramine produces an increase in the brain regional level of monoamines and metabolites indicating a greater synthesis rate for DA and 5-HT coinciding with an adaptive down regulation of 5-HT2 and DA D2 receptors[2]. |
Animal Admin | Rats[2] Male Wistar rats weighing 220-250 g at the beginning of the experiment are used. The animals, housed in groups of 6-8 have free access to food and water and are kept on a 12 hr light/dark cycle (light on at 6a.m.) at a temperature. The rats are anaesthetized with pentobarbital (50 mg/kg i.p.) and an osmotic minipump is implanted subcutaneously in the dorsal thoracic interscapular region. Each pump delivers 5 mg/kg/day of Trimipramine or amitriptyline. Control rats are implanted with pumps filled with 0.9%, saline. The total volume of solution in the pump is sufficient for at least 14 days delivery of drugs. After implantation, the incision is cleaned and sutured and the animals kept warm until they recovered from anaesthesia[2]. |
References |
Density | 1.029g/cm3 |
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Boiling Point | 411.8ºC at 760mmHg |
Melting Point | 141-143ºC |
Molecular Formula | C24H30N2O4 |
Molecular Weight | 410.506 |
Flash Point | 183.3ºC |
Exact Mass | 410.220551 |
PSA | 81.08000 |
LogP | 3.89780 |
Storage condition | 2-8℃ |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
|
Symbol |
GHS07, GHS08 |
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Signal Word | Warning |
Hazard Statements | H302-H315-H319-H335-H361 |
Precautionary Statements | P280-P301 + P312 + P330-P305 + P351 + P338 |
Personal Protective Equipment | Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges |
Hazard Codes | Xn,T,F |
Risk Phrases | 22-36/37/38-63-36/38-23/25 |
RIDADR | UN 3249 |
RTECS | HN9260000 |
Packaging Group | III |
Hazard Class | 6.1(b) |