Otenzepad

Modify Date: 2024-01-10 23:30:47

Otenzepad Structure
Otenzepad structure
Common Name Otenzepad
CAS Number 102394-31-0 Molecular Weight 421.53500
Density 1.171 g/cm3 Boiling Point 573.2ºC at 760 mmHg
Molecular Formula C24H31N5O2 Melting Point N/A
MSDS Chinese USA Flash Point 300.5ºC
Symbol GHS07
GHS07
Signal Word Warning

 Use of Otenzepad


Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively[1].

 Names

Name 11-[[2-[(Diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
Synonym More Synonyms

 Otenzepad Biological Activity

Description Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively[1].
Related Catalog
Target

640 nM (M2 muscarinic acetylcholine receptor in rabbit peripheral lung), 386 nM (M2 muscarinic acetylcholine receptor in rat heart)[1].

In Vivo Otenzepad (0.5, 1 mg/kg, s.c., in rats) significantly improved win-stay acquisition relative to vehicle-injected controls[2]. Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls[2]. Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory[3]. Animal Model: Forty-eight male Long-Evans rats (325-350 g)[2]. Dosage: 0.25, 0.5, 1.0 and 2.0 mg/kg. Administration: S.C. on the dorsum of the neck once. Result: Doses of 0.5 and 1.0 mg/kg significantly improved acquisition relative to vehicle controls, while doses of 0.25 and 2.0 mg/kg had no effect. Animal Model: Adult male Swiss mice (age 60–70 days; weight 25-30 g)[3]. Dosage: 0.3, 1.0, or 3.0 mg/kg. Administration: IP once. Result: Enhanced retention in an inverted-U dose–response manner, with significant enhancement seen at 1.0 mg/kg (U15,15 = 49, p < 0.02, compared with saline-saline-injected control group).
References

[1]. Bloom JW, et al. Heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116. Life Sci. 1987 Jul 27;41(4):491-6.

[2]. Packard MG, et al. Post-training injection of the acetylcholine M2 receptor antagonist AF-DX 116 improves memory. Brain Res. 1990 Jul 30;524(1):72-6.

[3]. Kopf SR, et al. AF-DX 116, a presynaptic muscarinic receptor antagonist, potentiates the effects of glucose and reverses the effects of insulin on memory. Neurobiol Learn Mem. 1998 Nov;70(3):305-13.

 Chemical & Physical Properties

Density 1.171 g/cm3
Boiling Point 573.2ºC at 760 mmHg
Molecular Formula C24H31N5O2
Molecular Weight 421.53500
Flash Point 300.5ºC
Exact Mass 421.24800
PSA 74.23000
LogP 3.21440
Storage condition 2-8°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UV0697000
CHEMICAL NAME :
6H-Pyrido(2,3-b)(1,4)benzodiazepin-6-one, 5,11-dihydro-11-((2-((diethylamino) methyl)-7-piperidinyl)acetyl)-
CAS REGISTRY NUMBER :
102394-31-0
LAST UPDATED :
199612
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C24-H31-N5-O2
MOLECULAR WEIGHT :
421.60

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1533 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,30,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
83 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,30,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
600 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,30,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
50 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,30,1991

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Hazard Codes Xi
RIDADR NONH for all modes of transport

 Articles26

More Articles
Acetylcholine activity in selective striatal regions supports behavioral flexibility.

Neurobiol. Learn. Mem. 91(1) , 13-22, (2009)

Daily living often requires individuals to flexibly respond to new circumstances. There is considerable evidence that the striatum is part of a larger neural network that supports flexible adaptations...

Nucleus accumbens acetylcholine and food intake: Decreased muscarinic tone reduces feeding but not food-seeking

Behav. Brain Res. 198(1) , 252-7, (2009)

Separate groups of food-deprived rats were given 2 h access to food after receiving bilateral nucleus accumbens infusions of the muscarinic antagonist scopolamine methyl bromide (at 0, 1.0, and 10.0 μ...

Loss of muscarinic and purinergic receptors in urinary bladder of rats with hydrochloric acid-induced cystitis.

Urology 76(4) , 1017.e7-12, (2010)

To clarify the basic mechanism involved in the pathophysiology of cystitis by characterizing the urodynamic parameters, pharmacologically relevant (muscarinic and purinergic) receptors, and the in viv...

 Synonyms

NPEC-caged-dopamine
ethyl)-7-piperidinyl)acetyl)
AF-DX 116