otenzepad

cardioselective muscarinic receptor antagonist; structure given in first source

Also Known As:

11-((2-((diethylamino)methyl)-1-piperidinyl)acetyl)-5,11-dihydro-6H-pyrido(2,3-b)(1-4)benzodiazepine-6-one; AF-DX 116; AF-DX-116; AFDX 116; 6H-Pyrido(2,3-b)(1,4)benzodiazepin-6-one, 11-((2-((diethylamino)methyl)-1-piperidinyl)acetyl)-5,11-dihydro-

Networked: 31 relevant articles (0 outcomes, 4 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Benzazepines: 5
      - Benzodiazepines: 8452
        Benzodiazepinones
        Pirenzepine: 520
        otenzepad: 31

Experts

1.	Fu, M L: 2 articles (10/2001 - 01/2001)
2.	Matsui, S: 2 articles (10/2001 - 01/2001)
3.	Alvarez-Cervera, Fernando J: 1 article (06/2014)
4.	Bata-García, José L: 1 article (06/2014)
5.	Erosa-Rivero, Helena B: 1 article (06/2014)
6.	Góngora-Alfaro, José L: 1 article (06/2014)
7.	Heredia-López, Francisco J: 1 article (06/2014)
8.	Hsieh, Dennis Jine-Yuan: 1 article (11/2002)
9.	Liao, Ching-Fong: 1 article (11/2002)
10.	Hayase, M: 1 article (10/2001)

Related Diseases

1.	Bradycardia 10/01/1991 - "We conclude that AF-DX 116 may be a useful drug for the treatment of bradycardia. " 05/05/1986 - "AF-DX 116, for its pronounced cardioselectivity, may have a therapeutic potential in the treatment of sinus bradycardia." 01/01/1991 - "When marked bradycardia (approximately 75% of control value) was reached, rats were given atropine sulfate (2 mg/kg, i.p.) or AF-DX 116 (20 mg/kg, i.p.). " 05/05/1986 - "In the conscious dog intravenous AF-DX 116 increased basal heart rate, and completely reversed the reflex bradycardia induced by clonidine. " 05/05/1986 - "In pithed rats AF-DX 116 inhibits vagally-induced bradycardia, an M2 response, (ED50 32 micrograms/kg i.v.) in preference to the M1-mediated pressor response to McN-A-343 (ED50 211 micrograms/kg i.v.). "
2.	Cardiomyopathies (Cardiomyopathy) 10/01/2001 - "In this study, we investigated the effect of M2-antagonist (otenzepad) on M2-peptide-induced cardiomyopathy in rabbits. "
3.	Dilated Cardiomyopathy (Cardiomyopathy, Congestive) 01/01/2001 - "This study indicates that anti-beta1-adrenoceptor and anti-M2-muscarinic receptor antibodies are of pathogenic importance in the development of human dilated cardiomyopathy, and that beta-adrenoceptor blockade, bisoprolol, and M2-muscarinic receptor antagonist, otenzepad, might be clinically useful for treatment of dilated cardiomyopathy."
4.	Tachycardia (Tachyarrhythmias) 01/01/1994 - "AF-DX 116 induced a tachycardia without a decrease of salivary flow in agreement with its selectivity profile (M2 > M1 > M3). " 02/01/1991 - "AF-DX 116 (10-100 micrograms/kg) had no effect on the preganglionic SNS-induced tachycardia. " 12/01/1989 - "AF-DX 116 induces a tachycardia together with an increased salivary flow in agreement with its selectivity profile (M2 greater than M1 greater than M3). " 01/01/1997 - "Although AF-DX 116 increased the heart rate, under the present experimental conditions of increased atrial rate, the extent of tachycardia was not strong enough to suppress the 24-h coronary ligation and digitalis-induced arrhythmias. " 02/01/1993 - "Finally, AF-DX 116, at doses inducing marked tachycardia, had a minor intestinal effect and no mydriatic effect. "
5.	Neuroblastoma 01/01/1991 - "Muscarinic receptors in N1E 115 mouse neuroblastoma cells were characterized by competition binding experiments using three agonists and five antagonists, including 4-DAMP and AF-DX 116, and by studying the effect of agonist stimulation on the cellular cAMP and cGMP content. " 07/31/1989 - "The cardioselective muscarinic antagonist, AF-DX 116 [11[2-[(diethyl-amino)-methyl]-O-1-piperidinyl]-5,11-dihydro-6H-pyrido- [2,3-b][1,4]-benzodiazepine-6-one), was weak at blocking the M2 muscarinic receptor-mediated inhibition of cyclic adenosine monophosphate (cAMP) formation in mouse neuroblastoma cells (clone N1E-115). "

Related Drugs and Biologics

1.	Oxotremorine
2.	Muscarinic Agonists
3.	Bisoprolol (Concor)
4.	Adrenergic Receptors (Adrenergic Receptor)
5.	Antibodies
6.	BIBN 99
7.	Pirenzepine
8.	Atropine
9.	Muscarinic Receptors (Muscarinic Acetylcholine Receptor)
10.	Cholinergic Agents (Cholinergics)

Related Therapies and Procedures

1.	Oral Administration
2.	Ligation
3.	Injections
4.	Induced Hypothermia
5.	Induced Hyperthermia (Thermotherapy)