Almotriptan Malate(PNU180638)|cas 181183-52-8|DC Chemicals

Cas No.:	181183-52-8
Chemical Name:	Almotriptan malate
Synonyms:	ALMOTRIPTAN;BUTANEDIOIC ACID, HYDROXY-, COMPD WITH 1-[[[3-[2-(DIMETHYLAMINO)ETHYL]-1H-INDOL-5-YL]METHYL]SULFONYL]PYRROLIDINE;ALMOTRIPTAN MALATE;AlmotriptanMaleate;1-[[[2-(Dimethyl-amino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine Malate;1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidine Malate;LAS-31416 Malate;Lactose Monohydrate;AlMotriptan Malate See: A575201;Almotriptan Malate See: A575201;PNU180638;N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]ethanamine,2-hydroxybutanedioic acid;3-[2-(Dimethylamino)ethyl]-5-(pyrrolidin-1-ylsulfonylmethyl )-1H-indole malate;N,N-Dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]ethanamine;Amotriptan malate;AlMotriptan Malate (Axert);Almotriptan Malate (200 mg);PNU 180638;3-[2-(Dimethylamino)ethyl]-5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indole Malate;1-[[[3-[2-(dimeth;Almotriptan maleate;Almotriptan (malate);LAS 31416 D,L-malate acid;PNU 180638E;LAS 31416;AK110510;Almotriptan malate [USAN];Almotriptan malate (USAN);1-(((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)sulfonyl)pyrrolidine, hydroxybutanedionate (1:1);1-(((3-(2-(Dimethylamino)ethyl)indol-5-yl)methyl)sulfonyl)pyrrolidine malate (1:1);N,N-dimethyl-2-[5-(pyrrolidin-1
SMILES:	OC(=O)CC(O)C(O)=O.CN(C)CCC1C2=C(NC=1)C=CC(CS(=O)(=O)N3CCCC3)=C2
Formula:	C₂₁H₃₁N₃O₇S
M.Wt:	469.5517
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.IC50:Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) ReceptorAlmotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Almotriptan showed low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors in several species, including the human, while affinity for 5-HT receptors other than 5-HT(1B/1D) was clearly less. Almotriptan did not exhibit significant affinity for several non-5-HT receptors studied up to 100 microM. Almotriptan inhibited forskolin-stimulated cyclic AMP accumulation in HeLa cells transfected with 5-HT(1B) or 5-HT(1D) human receptors [1]. Almotriptan had a mild antiemetic effect and a slight, transient diuretic effect in dogs, although the latter effect is probably of no clinical relevance. In addition, no effect on the respiratory system of conscious guinea pigs was observed following almotriptan treatment. These results indicate that almotriptan has a favourable safety profile with respect to the central nervous, renal and respiratory systems [2].

References:

[1]. Bou J , et al. Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine. Eur J Pharmacol, 2000. 410(1): p. 33-41. [2]. Gras J, et al. Safety profile of almotriptan, a new antimigraine agent. Effects on central nervous system, renal function and respiratory dynamics. Arzneimittelforschung, 2001. 51(9): p. 726-32.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC72326	Tabernanthalog	Tabernanthalog is a water-soluble, non-hallucinogenic and non-toxic analogue of ibogaine. Tabernanthalog is a 5-HT2A agonist. Tabernanthalog is found to promote structural neural plasticity, reduce alcohol- and heroin-seeking behaviour, and produce antidepressant-like effects in rodents.
DC71747	Aripiprazole monohydrate	Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19.
DC71510	Ansofaxine hydrochloride	Ansofaxine hydrochloride (LY03005, LPM570065), a triple reuptake inhibitor, inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.
DC71221	CJ033466	CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect.
DC70441	GR-127935	GR-127935 is a potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor; displays >100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types; blocks porcine carotid vascular response to sumatriptan in vivo; orally bioavailable and centrally active.
DC70176	AGH-107	AGH-107 is a potent, selective 5-HT7 receptor agonist with Ki of 6 nM and EC50 of 19 nM, 176-fold selectivity over 5-HT1AR.AGH-107 exhibited high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.
DC49608	RS 67333 hydrochloride	RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.
DC46455	SB 204741	SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1.
DC45564	F13714 fumarate	F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress.
DC44781	Pimethixene maleate	Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.,5-HT2B [1](Cell-free assay) 5-HT2A [1](Cell-free assay) Histamine H1 Receptor [1](Cell-free assay) Muscarinic M2 [1](Cell-free assay) Muscarinic M1 [1](Cell-free assay) View More 10.44(pKi) 10.22(pKi) 10.14(pKi) 9.38(pKi) 8.61(pKi)