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Zolmitriptan

Zolmitriptan
Zolmitriptan structure
CAS No.
139264-17-8
Chemical Name:
Zolmitriptan
Synonyms
Zomi;Zomig;311c90;bw311c90;Zolmitrptan;zolmitripan;Zolmitriptan;ZOLMITRIPTANE;ZOLIMITRIPTAN;ZolMitriptan API
CBNumber:
CB3313219
Molecular Formula:
C16H21N3O2
Formula Weight:
287.35684
MOL File:
139264-17-8.mol

Zolmitriptan Properties

Melting point:
136-141°C
alpha 
D22 -5.79° (c = 0.5 in methanol)
Boiling point:
563.3±38.0 °C(Predicted)
Density 
1.217±0.06 g/cm3(Predicted)
storage temp. 
Refrigerator
solubility 
Soluble in DMSO at 5mg/ml
pka
9.64(at 25℃)
form 
powder
color 
white to beige
optical activity
[α]/D -3 to -8°, c = 1 in methanol
λmax
225nm(lit.)
Merck 
14,10189
InChIKey
ULSDMUVEXKOYBU-ZDUSSCGKSA-N
CAS DataBase Reference
139264-17-8(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P264-P270-P301+P312+P330-P501
Hazard Codes  Xi,Xn
Risk Statements  36/37/38-22
Safety Statements  26-36
WGK Germany  3
RTECS  RQ2707000
HS Code  29349990

Zolmitriptan price More Price(11)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML0248 Zolmitriptan ≥98% (HPLC) 139264-17-8 10mg $82.9 2018-11-20 Buy
Sigma-Aldrich 1727009 Zolmitriptan United States Pharmacopeia (USP) Reference Standard 139264-17-8 200mg $352.8 2018-11-13 Buy
TCI Chemical Z0024 Zolmitriptan >98.0%(HPLC)(T) 139264-17-8 1g $255 2018-11-22 Buy
TCI Chemical Z0024 Zolmitriptan >98.0%(HPLC)(T) 139264-17-8 200mg $72 2018-11-22 Buy
Alfa Aesar J60616 Zolmitriptan 139264-17-8 100mg $115 2018-11-13 Buy

Zolmitriptan Chemical Properties,Uses,Production

Description

Zolmitriptan is a selective serotonin receptor agonist of the 1B and 1D subtypes. It is mainly used in the acute treatment of migraine attacks with or without aura and cluster headaches. Zolmitriptan takes effect through binding to human 5-HT1Band 5-HT1Dreceptors, leading to cranial blood vessel constriction and the release of sensory neuropeptides through nerve endings in the trigeminal system. 

Chemical Properties

White Crystalline Powder

Originator

Zeneca (UK)

Uses

A Serotonin 5HTID-receptor agonist

Uses

adrenergic agonist, nasal decongestant

brand name

Zomig (AstraZeneca); Zomig (IPR).

General Description

Zolmitriptan, the second triptan marketed (approved in1997), has a much better bioavailability (40%–48%) thansumatriptan. It is rapidly absorbed after oral or nasal sprayadministration. It also has an orally disintegrating tablet formulation(Zomig ZMT), which can be taken without water.Zolmitriptan undergoes rapid N-demethylation via CYP1A2to a more potent, active metabolite, N-desmethylzolmitriptan,which is 2 to 6 times more potent than the parentdrug. This active metabolite was detected 5 minutesafter dosing and accounts for about two thirds of the plasmaconcentration of the administered dose of the parent drug.284Thus, it is reasonable to assume that the therapeutic effectsand especially the CNS side effects of zolmitriptan must bein part attributed to the plasma levels of this active metabolite,at least until it is further degraded by hepatic MAO-Ato its inactive indole acetic acid derivatives.

Clinical Use

Zomig was launched in Germany, Denmark, Sweden and the UK for use as an antimigraine agent (with and without aura). It can be prepared by three related routes of 5 to 7 steps starting from L-4-nitrophenylalanine. Zomig is a 5-HT1D/1B receptor agonist (10 fold ratio) with modest (< 100x) affinity for 5-HT1A and 5-HT1F receptors. It has no affinity for other serotonin receptors or receptors of other neurotransmitters. It has a novel dual action mechanism: centrally it acts on the trigeminal nucleus caudalis and peripherally is acts on the trigeminovascular system. Zomig was effective in treating headaches and nonheadache (photophobia, phonophobia and nausea) symptoms. It was 2-3 times more potent than sumatriptan and is metabolized to three compounds, one of which is 2-8 times more active than the parent. It caused a 40-50% decrease in headache after 1 h and a 73-77% after 4 h. There was a 30% reoccurance of headache but 90% effective treatment with a second dose. It blocks neurogenic inflammation by inhibiting release of peptides, causes vasoconstriction, and inhibits neuronal depolarization at peripheral sites in the cranium. It is 40% bioavailable and a 10 time theraputic dose showed no safety concerns.

References

https://www.drugbank.ca/drugs/DB00315
Rothner, A. D., et al. "Zolmitriptan oral tablet in migraine treatment: high placebo responses in adolescents." Headache the Journal of Head & Face Pain 46.1(2006):101.
Hedlund, C, et al. "Zolmitriptan nasal spray in the acute treatment of cluster headache: a meta-analysis of two studies. " Neurology49.9(2009):1315–1323.

Zolmitriptan Preparation Products And Raw materials

Raw materials

Preparation Products


Zolmitriptan Suppliers

Global( 302)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
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Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
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career henan chemical co
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0371-55170693
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View Lastest Price from Zolmitriptan manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-07-23 Zolmitriptan
139264-17-8
US $4500.00 / KG 1KG 99% 500KG career henan chemical co

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