Tolterodine tartrate(Kabi-2234 PNU-200583E)

Molecular Weight (MW)	475.57
Formula	C22H31NO.C4H6O6
CAS No.	124937-52-6
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 95 mg/mL (199.8 mM)
Water: 17 mg/mL (35.7 mM)
Ethanol: 6 mg/mL (12.6 mM)
Other info	Chemical Name: (R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-methylphenol (2R,3R)-2,3-dihydroxysuccinate InChi Key: TWHNMSJGYKMTRB-KXYUELECSA-N InChi Code: InChI=1S/C22H31NO.C4H6O6/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24;5-1(3(7)8)2(6)4(9)10/h6-12,15-17,20,24H,13-14H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)/t20-;1-,2-/m11/s1 SMILES Code: OC1=CC=C(C)C=C1[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C.O=C(O)[C@H](O)[C@@H](O)C(O)=O
Synonyms	PNU-200583 E; PNU200583E; Tolterodine tartrate; PNU-200583E; PNU 200583E; Detrol LA; Detrusitol.

Molecular Weight (MW)

475.57

Formula

C22H31NO.C4H6O6

CAS No.

124937-52-6

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 95 mg/mL (199.8 mM)

Water: 17 mg/mL (35.7 mM)

Ethanol: 6 mg/mL (12.6 mM)

Other info

Chemical Name: (R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-methylphenol (2R,3R)-2,3-dihydroxysuccinate

InChi Key: TWHNMSJGYKMTRB-KXYUELECSA-N

InChi Code: InChI=1S/C22H31NO.C4H6O6/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24;5-1(3(7)8)2(6)4(9)10/h6-12,15-17,20,24H,13-14H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)/t20-;1-,2-/m11/s1

SMILES Code: OC1=CC=C(C)C=C1[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C.O=C(O)[C@H](O)[C@@H](O)C(O)=O

Synonyms

PNU-200583 E; PNU200583E; Tolterodine tartrate; PNU-200583E; PNU 200583E; Detrol LA; Detrusitol.

In Vitro	In vitro activity: Tolterodine has a high affinity and specificity for muscarinic receptors in vitro and it exhibits selectivity for the urinary bladder over salivary glands in vivo. Tolterodine is a new muscarinic receptor antagonist intended for the treatment of urinary urge incontinence and other symptoms related to an overactive bladder. Tolterodine effectively inhibits carbachol-induced contractions of isolated strips of urinary bladder from guinea pigs in a concentration-dependent, competitive manner. Tolterodine binds with high affinity to muscarinic receptors in urinary bladder (Ki 2.7 nM), heart (Ki 1.6 nM), cerebral cortex (Ki 0.75 nM) and parotid gland (Ki 4.8 nM) from guinea pigs and in urinary bladder from humans (Ki 3.3 nM).
In Vivo	Tolterodine (1 mg/kg, i.v.) is significantly more potent in inhibiting acetylcholine-induced urinary bladder contraction than electrically-induced salivation in the anaesthetised cat. Tolterodine administered intravenously increases the mean micturition interval, bladder capacity and micturition volume in normal rats and resiniferatoxin treated rats. Tolterodine (2 nM/kg) significantly increases bladder capacity (BC) in saline vehicle- cerebral infarct rats without increasing residual volume but it has no effects on BC in resiniferatoxin- cerebral infarct rats. Tolterodine tartrate (0.1 and 1.0 mg/kg) significantly decreases the number and amplitude of non-voiding contractions by 38-74% and 29-44%, respectively, and increases bladder capacity by 19-51% in female rats with bladder outlet obstruction.
Animal model	Cat
Formulation & Dosage	1 mg/kg, i.v.
References	Eur J Pharmacol. 1997 May 30;327(2-3):195-207; J Urol. 2007 Jul;178(1):326-31.

In Vitro

In vitro activity: Tolterodine has a high affinity and specificity for muscarinic receptors in vitro and it exhibits selectivity for the urinary bladder over salivary glands in vivo. Tolterodine is a new muscarinic receptor antagonist intended for the treatment of urinary urge incontinence and other symptoms related to an overactive bladder. Tolterodine effectively inhibits carbachol-induced contractions of isolated strips of urinary bladder from guinea pigs in a concentration-dependent, competitive manner. Tolterodine binds with high affinity to muscarinic receptors in urinary bladder (Ki 2.7 nM), heart (Ki 1.6 nM), cerebral cortex (Ki 0.75 nM) and parotid gland (Ki 4.8 nM) from guinea pigs and in urinary bladder from humans (Ki 3.3 nM).

In Vivo

Tolterodine (1 mg/kg, i.v.) is significantly more potent in inhibiting acetylcholine-induced urinary bladder contraction than electrically-induced salivation in the anaesthetised cat. Tolterodine administered intravenously increases the mean micturition interval, bladder capacity and micturition volume in normal rats and resiniferatoxin treated rats. Tolterodine (2 nM/kg) significantly increases bladder capacity (BC) in saline vehicle- cerebral infarct rats without increasing residual volume but it has no effects on BC in resiniferatoxin- cerebral infarct rats. Tolterodine tartrate (0.1 and 1.0 mg/kg) significantly decreases the number and amplitude of non-voiding contractions by 38-74% and 29-44%, respectively, and increases bladder capacity by 19-51% in female rats with bladder outlet obstruction.

Animal model

Cat

Formulation & Dosage

1 mg/kg, i.v.

References

Eur J Pharmacol. 1997 May 30;327(2-3):195-207; J Urol. 2007 Jul;178(1):326-31.

CAS NO:	124937-52-6
规格:	≥98%

包装	价格(元)
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议