Selective relaxant binding agents (SRBAs) are a new class of drugs that selectively encapsulates and binds neuromuscular blocking agents (NMBAs). The first drug introduction of an SRBA is sugammadex. Sugammadex is a modified gamma cyclodextrin that specifically encapsulates and binds the aminosteroid NMBAs: rocuronium>vecuronium>>pancuronium. SRBAs exert a chelating action that effectively terminates an NMBA ability to bind to nicotinic receptors.
Discovery of SRBAs
The discovery of SRBA as a new class of drug is the result of work done by Organon laboratories at the Newhouse research site in Scotland. Cyclodextrins were explored as a means to solubilize rocuronium bromide (a steroidal NMBA) in a neutral aqueous solution. Upon creating numerous modified cyclodextrins, one particular molecule was found to possess extremely high affinity for the rocuronium molecule. Originally known as Org25969, it is now generically named sugammadex sodium.
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| mAChRs |
| Agonists |
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| Antagonists |
- 3-Quinuclidinyl benzilate
- 4-DAMP
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Aclidinium bromide (+formoterol)
- Abediterol
- AF-DX 250
- AF-DX 384
- Ambutonium bromide
- Anisodamine
- Anisodine
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Antihistamines (first-generation) (e.g., brompheniramine, buclizine, captodiame, chlorphenamine (chlorpheniramine), cinnarizine, clemastine, cyproheptadine, dimenhydrinate, dimetindene, diphenhydramine, doxylamine, meclizine, mequitazine, perlapine, phenindamine, pheniramine, phenyltoloxamine, promethazine, propiomazine, triprolidine)
- AQ-RA 741
- Atropine
- Atropine methonitrate
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Atypical antipsychotics (e.g., clozapine, fluperlapine, olanzapine (+fluoxetine), rilapine, quetiapine, tenilapine, zotepine)
- Benactyzine
- Benzatropine (benztropine)
- Benzilone
- Benzilylcholine mustard
- Benzydamine
- BIBN 99
- Biperiden
- Bornaprine
- Camylofin
- CAR-226,086
- CAR-301,060
- CAR-302,196
- CAR-302,282
- CAR-302,368
- CAR-302,537
- CAR-302,668
- Caramiphen
- Cimetropium bromide
- Clidinium bromide
- Cloperastine
- CS-27349
- Cyclobenzaprine
- Cyclopentolate
- Darifenacin
- DAU-5884
- Desfesoterodine
- Dexetimide
- DIBD
- Dicycloverine (dicyclomine)
- Dihexyverine
- Difemerine
- Diphemanil metilsulfate
- Ditran
- Drofenine
- EA-3167
- EA-3443
- EA-3580
- EA-3834
- Emepronium bromide
- Etanautine
- Etybenzatropine (ethybenztropine)
- Fenpiverinium
- Fentonium bromide
- Fesoterodine
- Flavoxate
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Glycopyrronium bromide (+beclometasone/formoterol, +indacaterol, +neostigmine)
- Hexahydrodifenidol
- Hexahydrosiladifenidol
- Hexbutinol
- Hexocyclium
- Himbacine
- HL-031,120
- Homatropine
- Imidafenacin
-
Ipratropium bromide (+salbutamol)
- Isopropamide
- J-104,129
- Hyoscyamine
- Mamba toxin 3
- Mamba toxin 7
- Mazaticol
- Mebeverine
- Meladrazine
- Mepenzolate
- Methantheline
- Methoctramine
- Methylatropine
- Methylhomatropine
- Methylscopolamine
- Metixene
- Muscarinic toxin 7
- N-Ethyl-3-piperidyl benzilate
- N-Methyl-3-piperidyl benzilate
- Nefopam
- Octatropine methylbromide (anisotropine methylbromide)
- Orphenadrine
- Otenzepad (AF-DX 116)
- Otilonium bromide
- Oxapium iodide
- Oxitropium bromide
- Oxybutynin
- Oxyphencyclimine
- Oxyphenonium bromide
- PBID
- PD-102,807
- PD-0298029
- Penthienate
- Pethidine
- pFHHSiD
- Phenglutarimide
- Phenyltoloxamine
- Pipenzolate bromide
- Piperidolate
- Pirenzepine
- Piroheptine
- Pizotifen
- Poldine
- Pridinol
- Prifinium bromide
- Procyclidine
- Profenamine (ethopropazine)
- Propantheline bromide
- Propiverine
- Quinidine
- 3-Quinuclidinyl thiochromane-4-carboxylate
- Revefenacin
- Rociverine
- RU-47,213
- SCH-57,790
- SCH-72,788
- SCH-217,443
- Scopolamine (hyoscine)
- Scopolamine butylbromide (hyoscine butylbromide)
- Silahexacyclium
- Sofpironium bromide
- Solifenacin
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SSRIs (e.g., femoxetine, paroxetine)
- Telenzepine
- Terodiline
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Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin, mirtazapine)
- Tiemonium iodide
- Timepidium bromide
- Tiotropium bromide
- Tiquizium bromide
- Tofenacin
- Tolterodine
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Tricyclic antidepressants (e.g., amitriptyline (+perphenazine), amitriptylinoxide, butriptyline, cidoxepin, clomipramine, desipramine, desmethyldesipramine, dibenzepin, dosulepin (dothiepin), doxepin, imipramine, lofepramine, nitroxazepine, northiaden (desmethyldosulepin), nortriptyline, protriptyline, quinupramine, trimipramine)
- Tridihexethyl
- Trihexyphenidyl
- Trimebutine
- Tripitamine (tripitramine)
- Tropacine
- Tropatepine
- Tropicamide
- Trospium chloride
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Typical antipsychotics (e.g., chlorpromazine, chlorprothixene, cyamemazine (cyamepromazine), loxapine, mesoridazine, thioridazine)
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Umeclidinium bromide (+vilanterol)
- WIN-2299
- Xanomeline
- Zamifenacin
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Precursors (and prodrugs)
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| nAChRs |
Agonists (and PAMs) |
- 5-HIAA
- 6-Chloronicotine
- A-84,543
- A-366,833
- A-582,941
- A-867,744
- ABT-202
- ABT-418
- ABT-560
- ABT-894
- Acetylcholine
- Altinicline
- Anabasine
- Anatabine
- Anatoxin-a
- AR-R17779
- Bephenium hydroxynaphthoate
- Butinoline
- Butyrylcholine
- Carbachol
- Choline
- Cotinine
- Cytisine
- Decamethonium
- Desformylflustrabromine
- Dianicline
- Dimethylphenylpiperazinium
- Epibatidine
- Epiboxidine
- Ethanol (alcohol)
- Ethoxysebacylcholine
- EVP-4473
- EVP-6124
- Galantamine
- GTS-21
- Ispronicline
- Ivermectin
- JNJ-39393406
- Levamisole
- Lobeline
- MEM-63,908 (RG-3487)
- Morantel
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Nicotine (tobacco)
- NS-1738
- PHA-543,613
- PHA-709,829
- PNU-120,596
- PNU-282,987
- Pozanicline
- Pyrantel
- Rivanicline
- RJR-2429
- Sazetidine A
- SB-206553
- Sebacylcholine
- SIB-1508Y
- SIB-1553A
- SSR-180,711
- Suberyldicholine
- Suxamethonium (succinylcholine)
- Suxethonium (succinyldicholine)
- TC-1698
- TC-1734
- TC-1827
- TC-2216
- TC-5214
- TC-5619
- TC-6683
- Tebanicline
- Tribendimidine
- Tropisetron
- UB-165
- Varenicline
- WAY-317,538
- XY-4083
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Antagonists (and NAMs) |
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Precursors (and prodrugs)
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