Categories
Sarpogrelate hydrochloride
- CAS: 135159-51-2
- Purity: 99%
- Manufacturer supply good quality Sarpogrelate hydrochloride 135159-51-2 with stock
Manufacturer supply good quality Sarpogrelate hydrochloride 135159-51-2 with stock
- Molecular Formula:C24H32ClNO6
- Molecular Weight:465.974
- Appearance/Colour:colorless liquid
- Vapor Pressure:1.43E-14mmHg at 25°C
- Melting Point:145-148°C
- Boiling Point:585.9 °C at 760 mmHg
- Flash Point:308.1 °C
- PSA：85.30000
- LogP:3.99940
Sarpogrelate hydrochloride(Cas 135159-51-2) Usage
|
Biological Activity |
Selective 5-HT 2A receptor antagonist (pK i values are 8.52, 7.43 and 6.57 for 5-HT 2A , 5-HT 2C and 5-HT 2B receptors respectively). Displays selectivity over 5-HT 1 , 5-HT 3 , 5-HT 4 H 1 , H 2 , M 3 , α 1 -adrenergic, α 2 -adrenergic and β -adrenergic receptors. Displays cardioprotective activity in vivo . |
|
in vitro |
the major metabolite (r,s)-m-1, and m-1 enantiomers of sarpogrelate specifically blocked 5-ht at 5-ht2a receptors. the stereochemical configuration of the ligands does not obviously play a key role at binding to the 5-ht2a receptor [2]. |
|
in vivo |
pad patients were divided into two groups. one group treated with 100 mg sarpogrelate in oral 3 times one day for 12 weeks (n = 10), while the other group who remained on conventional therapy as control group (n = 11). forearm blood flow (fbf) and leg blood flow (lbf) responses to reactive hyperemia (rh) and sublingual administration of nitroglycerin (ntg) were measured by strain-gauge plethysmography. after twelve weeks of its administration, fbf and lbf responses during rh exhibited significant increases from 13.2 6 1.7 to 18.1 6 2.2 ml/min every 100 ml tissue (p , 0.01) and from 8.2 6 0.9 to 14.2 6 2.1 ml/min every 100 ml tissue (p , 0.05), respectively. augmentation of fbf and lbf induced by sarpogrelate responses to rh was maintained at 24 weeks. the control group had no change observed in at each follow-up time point. the changes in fbf and lbf after sublingual ntg were similar during follow-up periods in the two groups. these findings suggest that longterm oral administration of sarpogrelate improves vascular function in patients with pad [3]. |
|
references |
[1] nishio h1, inoue a, nakata y. binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. arch int pharmacodyn ther. 1996 mar-apr;331(2):189-202.[2] pertz h1, elz s. in-vitro pharmacology of sarpogrelate and the enantiomers of its major metabolite: 5-ht2a receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-ht contractions in rat tail artery. j pharm pharmacol. 1995 apr;47(4):310-6.[3] miyazaki m1, higashi y, goto c, chayama k, yoshizumi m, sanada h, orihashi k, sueda t. sarpogrelate hydrochloride, a selective 5-ht2a antagonist, improves vascular function in patients with peripheral arterial disease. j cardiovasc pharmacol. 2007 apr;49(4):221-7. |
|
Brand name |
Anplag |
InChI:InChI=1/C24H31NO6.ClH/c1-25(2)16-21(31-24(28)14-13-23(26)27)17-30-22-10-5-4-8-19(22)12-11-18-7-6-9-20(15-18)29-3;/h4-10,15,21H,11-14,16-17H2,1-3H3,(H,26,27);1H
135159-51-2 Relevant articles
METHODS FOR PREPARING SARPOGRELATE HYDROCHLORIDE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
-
Paragraph 0084; 0086-0090; 0158, (2020/10/20)
The present invention provides hydrochlo...
Crystallizine Sapogrelate Hydrochloride and a method for forming the same
-
Paragraph 0057; 0058, (2019/10/08)
Disclosed are sarpogrelate hydrochloride...
Process for preparing sand Greythe ester is new hydrochloric acid
-
Paragraph 0019; 0023; 0027, (2018/07/10)
The present invention discloses a prepar...
Syntheses and Platelet Aggregation Inhibitory and Antithrombotic Properties of ethyl>benzenes
Kikumoto, Ryoji,Hara, Hiroto,Ninomiya, Kunihiro,Osakabe, Masanori,Sugano, Mamoru,et al.
, p. 1818 - 1823 (2007/10/02)
A series of ethyl>benzene derivatives we...
135159-51-2 Process route
-
-
108-30-5
succinic acid anhydride
-
![(±)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol hydrochloride](/upload/2026/10/99669c1bede945eb86e0e63cab193a5c_f1b8f37c-24d7-458b-b527-8c3e750794f1.png)
-
135261-74-4
(±)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol hydrochloride
-
-
135159-51-2,86819-20-7
sarpogrelate hydrochloride
| Conditions | Yield |
|---|---|
|
(±)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol hydrochloride;
With
sodium hydroxide;
In
dichloromethane; water;
succinic acid anhydride;
In
tetrahydrofuran;
at 35 - 40 ℃;
With
hydrogenchloride;
In
water;
for 1h;
pH=3;
|
95.4% |
|
succinic acid anhydride; (±)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol hydrochloride;
With
triethylamine;
In
acetone;
for 1h;
Reflux;
With
hydrogenchloride;
In
water;
|
94.6% |
|
In
acetone;
for 1h;
Heating;
|
-
-
108-30-5
succinic acid anhydride
-
-
135963-42-7,127003-40-1
(R,S)-1-<2-<2-(3-methoxyphenyl)ethyl>phenoxy>-3-(dimethylamino)-2-propanol
-
-
135159-51-2,86819-20-7
sarpogrelate hydrochloride
| Conditions | Yield |
|---|---|
|
succinic acid anhydride; (R,S)-1-<2-<2-(3-methoxyphenyl)ethyl>phenoxy>-3-(dimethylamino)-2-propanol;
In
acetone;
for 6h;
Reflux;
With
hydrogenchloride;
In
acetone;
at 0 - 20 ℃;
for 8h;
pH=1 - 2;
Concentration;
|
92.5% |
135159-51-2 Upstream products
-
108-30-5
succinic acid anhydride
-
135261-74-4
(±)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol hydrochloride
-
167145-13-3
2-[2-(3-methoxyphenyl)ethyl]phenol
-
135963-42-7
(R,S)-1-<2-<2-(3-methoxyphenyl)ethyl>phenoxy>-3-(dimethylamino)-2-propanol
135159-51-2 Downstream products
-
110-15-6
succinic acid
-
135963-42-7
(R,S)-1-<2-<2-(3-methoxyphenyl)ethyl>phenoxy>-3-(dimethylamino)-2-propanol
