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84057-84-1

84057-84-1 structure
84057-84-1 structure
  • Name: lamotrigine
  • Chemical Name: lamotrigine
  • CAS Number: 84057-84-1
  • Molecular Formula: C9H7Cl2N5
  • Molecular Weight: 256.091
  • Catalog: API Nervous system medication Antiepileptic and anticonvulsant
  • Create Date: 2018-03-03 08:00:00
  • Modify Date: 2024-01-01 20:15:09
  • Lamotrigine(BW430C) is a novel anticonvulsant drug for inhibition of 5-HT and sodium channelTarget: Sodium ChannelLamotrigine stabilises presynaptic neuronal membranes by blockade of voltage-dependent sodium channels, thus preventing the release of excitatory neurotransmitters, particularly glutamate and aspartate [1]. In rat cerebral cortex tissue incubated with veratrine 10 mg/L, lamotrigine is twice as potent in inhibiting the release of glutamate and aspartate (ED 50 = 5.38 mg/L for each) than the release of GABA (ED50 = 11.2 mg/L), and is much less potent in inhibiting acetylcholine release (ED50 = 25.6 mg/L) when cortical slices is exposed to veratrine 75 mg/L. Basal glutamate release is unaffected [2]. Lamotrigine inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels [3]. Lamotrigine (Lamictal), a phenyltriazine derivative, is a well established anticonvulsant agent that has shown efficacy in the prevention of mood episodes in adult patients with bipolar I disorder. lamotrigine significantly delayed time to intervention for a depressive episode and showed limited efficacy in delaying time to intervention for a manic/hypomanic episode, compared with placebo. Lamotrigine is generally well tolerated [4].
Name lamotrigine
Synonyms Lamictal
Lamotrigin
6-(2,3-Dichlorophenyl)-1,2,4-triazine-3,5-diamine
EINECS 281-901-8
6-(2,3-Dichlorophenyl)-3-imino-3,4-dihydro-1,2,4-triazin-5-amine
1,2,4-Triazin-5-amine, 6-(2,3-dichlorophenyl)-3,4-dihydro-3-imino-
Crisomet
Lamictal CD
HYDROXYMETHYL PROGESTERONE
6-O-TRITYL-1,2,3,4-TETRA-O-ACETYL-ALPHA-D-MANNOPYRANOSE
BW 430C
LAMOTRIGENE
LAMOTRIGINE API
MFCD00865333
LAMOTRIGINE / 6-(2,3-DICHLOROPHENYL)-1,2,4-TRIAZINE-3,5-DIAMINE
Lamictal XR
1,2,4-Triazine-3,5-diamine, 6-(2,3-dichlorophenyl)-
LAMOTRIGINE-13C3
LAMOTRIGINE (10 MG )
Lamotrigina
1,2,4-TRIAZINE-3,5-DIAMINE,6-(2,3-DICHLOROPHENYL)-
Labileno
Lamotriginum
Lamotrigine
Description Lamotrigine(BW430C) is a novel anticonvulsant drug for inhibition of 5-HT and sodium channelTarget: Sodium ChannelLamotrigine stabilises presynaptic neuronal membranes by blockade of voltage-dependent sodium channels, thus preventing the release of excitatory neurotransmitters, particularly glutamate and aspartate [1]. In rat cerebral cortex tissue incubated with veratrine 10 mg/L, lamotrigine is twice as potent in inhibiting the release of glutamate and aspartate (ED 50 = 5.38 mg/L for each) than the release of GABA (ED50 = 11.2 mg/L), and is much less potent in inhibiting acetylcholine release (ED50 = 25.6 mg/L) when cortical slices is exposed to veratrine 75 mg/L. Basal glutamate release is unaffected [2]. Lamotrigine inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels [3]. Lamotrigine (Lamictal), a phenyltriazine derivative, is a well established anticonvulsant agent that has shown efficacy in the prevention of mood episodes in adult patients with bipolar I disorder. lamotrigine significantly delayed time to intervention for a depressive episode and showed limited efficacy in delaying time to intervention for a manic/hypomanic episode, compared with placebo. Lamotrigine is generally well tolerated [4].
Related Catalog
References

[1]. Goa, K.L., S.R. Ross, and P. Chrisp, Lamotrigine. A review of its pharmacological properties and clinical efficacy in epilepsy. Drugs, 1993. 46(1): p. 152-76.

[2]. Leach, M.J., C.M. Marden, and A.A. Miller, Pharmacological studies on lamotrigine, a novel potential antiepileptic drug: II. Neurochemical studies on the mechanism of action. Epilepsia, 1986. 27(5): p. 490-7.

[3]. Cheung, H., D. Kamp, and E. Harris, An in vitro investigation of the action of lamotrigine on neuronal voltage-activated sodium channels. Epilepsy Res, 1992. 13(2): p. 107-12.

[4]. Goldsmith, D.R., et al., Lamotrigine: a review of its use in bipolar disorder. Drugs, 2003. 63(19): p. 2029-50.
Density 1.6±0.1 g/cm3
Boiling Point 503.1±60.0 °C at 760 mmHg
Melting Point 177-181°C
Molecular Formula C9H7Cl2N5
Molecular Weight 256.091
Flash Point 258.1±32.9 °C
Exact Mass 255.007858
PSA 90.71000
LogP -0.19
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.706
Storage condition 2-8°C
Water Solubility DMSO: 20 mg/mL at 60 °C, soluble

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XY5850700
CHEMICAL NAME :
1,2,4-Triazine-3,5-diamine, 6-(2,3-dichlorophenyl)-
CAS REGISTRY NUMBER :
84057-84-1
LAST UPDATED :
199706
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C9-H7-Cl2-N5
MOLECULAR WEIGHT :
256.11

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
19 mg/kg
TOXIC EFFECTS :
Behavioral - muscle contraction or spasticity Sense Organs and Special Senses (Eye) - effect, not otherwise specified Cardiac - EKG changes not diagnostic of specified effects
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 342,1552,1993
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
2 mg/kg/30H-I
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)
REFERENCE :
PEDIAU Pediatrics. (American Academy of Pediatrics, P.O. Box 1034, Evanston, IL 60204) V.1- 1948- Volume(issue)/page/year: 98,294,1996
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
205 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EPILAK Epilepsia (New York). (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) Ser.1-3: 1909-55; Ser.4: V.1- 1959- Volume(issue)/page/year: 25,655,1984
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
245 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EPILAK Epilepsia (New York). (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) Ser.1-3: 1909-55; Ser.4: V.1- 1959- Volume(issue)/page/year: 25,655,1984
Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
Personal Protective Equipment Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
Hazard Codes T: Toxic;
Risk Phrases R25
Safety Phrases S45
RIDADR UN 2811 6.1/PG 3
WGK Germany 3
RTECS XY5850700
Packaging Group III
Hazard Class 6.1(b)
HS Code 2933699090
84689-20-3 structure

84689-20-3

~82%

84057-84-1 structure

84057-84-1
Literature: ALEMBIC LIMITED Patent: WO2009/69073 A1, 2009 ; Location in patent: Page/Page column 3; 5 ;
6574-97-6 structure

6574-97-6
2582-30-1 structure

2582-30-1

~%

84057-84-1 structure

84057-84-1
Literature: US4847249 A1, ;
77668-42-9 structure

77668-42-9

~%

84057-84-1 structure

84057-84-1
Literature: US6111101 A1, ;
71-23-8 structure

71-23-8
6574-97-6 structure

6574-97-6
2582-30-1 structure

2582-30-1

~%

84057-84-1 structure

84057-84-1
Literature: EP247892 B1, ;
879573-84-9 structure

879573-84-9

~76%

84057-84-1 structure

84057-84-1
Literature: Ulomskii; Shestakova; Deev; Rusinov; Chupakhin Russian Chemical Bulletin, 2005 , vol. 54, # 3 p. 726 - 732
130801-01-3 structure

130801-01-3

~%

84057-84-1 structure

84057-84-1
Literature: Russian Chemical Bulletin, , vol. 54, # 3 p. 726 - 732
32768-54-0 structure

32768-54-0

~%

84057-84-1 structure

84057-84-1
Literature: Russian Chemical Bulletin, , vol. 54, # 3 p. 726 - 732
57915-78-3 structure

57915-78-3

~%

84057-84-1 structure

84057-84-1
Literature: Russian Chemical Bulletin, , vol. 54, # 3 p. 726 - 732
HS Code 2933699090
Summary 2933699090 other compounds containing an unfused triazine ring (whether or not hydrogenated) in the structure。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:20.0%

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