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Muscarinic antagonist

Drug that binds to but does not activate muscarinic cholinergic receptors

Field	Value
Name	Muscarinic acetylcholine receptor antagonist
Image	L-Scopolamin.svg
ImageClass	skin-invert-image
Alt	Scopolamine
Synonyms	Muscarinic acetylcholine receptor antagonist; Antimuscarinic; Anti-muscarinic; mACh antagonist; mAChR antagonist; Muscarinic antagonist; Antimuscarinic agent; Antimuscarinic drug; Antimuscarinic medication
Use	Allergies, asthma, atrial fibrillation with bradycardia, motion sickness, Parkinson's disease, etc.
Caption	Skeletal formula of scopolamine, a nonselective antagonist of the muscarinic receptors
Biological_target	Muscarinic acetylcholine receptors
ATC_prefix	V
MeshID	D018727

A muscarinic acetylcholine receptor antagonist, also simply known as a muscarinic antagonist or as an antimuscarinic agent, is a type of anticholinergic drug that blocks the activity of the muscarinic acetylcholine receptors (mAChRs). The muscarinic receptors are proteins involved in the transmission of signals through certain parts of the nervous system, and muscarinic receptor antagonists work to prevent this transmission from occurring. Notably, muscarinic antagonists reduce the activation of the parasympathetic nervous system. The normal function of the parasympathetic system is often summarised as "rest-and-digest", and includes slowing of the heart, an increased rate of digestion, narrowing of the airways, promotion of urination, and sexual arousal. Muscarinic antagonists counter this parasympathetic "rest-and-digest" response, and also work elsewhere in both the central and peripheral nervous systems.

Drugs with muscarinic antagonist activity are widely used in medicine, in the treatment of low heart rate, overactive bladder, respiratory problems such as asthma and chronic obstructive pulmonary disease (COPD). A number of other drugs, such as antipsychotics and the tricyclic family of antidepressants, have incidental muscarinic antagonist activity which can cause unwanted side effects such as difficulty urinating, dry mouth and skin, and constipation.

Acetylcholine (often abbreviated ACh) is a neurotransmitter whose receptors are proteins found in synapses and other cell membranes. Besides responding to their primary neurochemical, neurotransmitter receptors can be sensitive to a variety of other molecules. Acetylcholine receptors are classified into two groups based on this:

muscarinic, which respond to muscarine
nicotinic, which respond to nicotine

Most muscarinic receptor antagonists are synthetic chemicals; however, the two most commonly used anticholinergics, scopolamine and atropine, are belladonna alkaloids, and are naturally extracted from plants such as Atropa belladonna, commonly known as deadly nightshade. The name "belladonna", Italian for "beautiful woman", is thought to derive from one of the antimuscarinic effects of these alkaloids, having been put into use by women for the cosmetic purpose of promoting dilation of the pupils.

Muscarinic antagonist effects and muscarinic agonist effects counterbalance each other for homeostasis.

Certain muscarinic antagonists can be classified into either long-acting muscarinic receptor antagonists (LAMAs) or short-acting muscarinic receptor antagonists (SAMAs), depending on when maximum effect occurs and for how long the effect persists.

Effects

Scopolamine and atropine have similar effects on the peripheral nervous system. However, scopolamine has greater effects on the central nervous system (CNS) than atropine due to its ability to cross the blood–brain barrier. At higher-than-therapeutic doses, atropine and scopolamine cause CNS depression characterized by amnesia, fatigue, and reduction in rapid eye movement sleep. Scopolamine (Hyoscine) has anti-emetic activity and is, therefore, used to treat motion sickness.

Antimuscarinics are also used as anti-parkinsonian drugs. In parkinsonism, there is imbalance between levels of acetylcholine and dopamine in the brain, involving both increased levels of acetylcholine and degeneration of dopaminergic pathways (nigrostriatal pathway). Thus, in parkinsonism there is decreased level of dopaminergic activity. One method of balancing the neurotransmitters is through blocking central cholinergic activity using muscarinic receptor antagonists.

Atropine acts on the M2 receptors of the heart and antagonizes the activity of acetylcholine. It causes tachycardia by blocking vagal effects on the sinoatrial node. Acetylcholine hyperpolarizes the sinoatrial node; this is overcome by MRAs, and thus they increase the heart rate. If atropine is given by intramuscular or subcutaneous injection, it causes initial bradycardia. This is because when administered intramuscularly or subcutaneously atropine acts on presynaptic M1 receptors (autoreceptors). Uptake of acetylcholine in axoplasm is prevented and the presynaptic nerve releases more acetylcholine into the synapse, which initially causes bradycardia.

In the atrioventricular node, the resting potential is lowered, which facilitates conduction. This is seen as a shortened PR-interval on an electrocardiogram. It has an opposite effect on blood pressure. Tachycardia and stimulation of the vasomotor center causes an increase in blood pressure. But, due to feedback regulation of the vasomotor center, there is a fall in blood pressure due to vasodilation.

Important muscarinic antagonists include atropine, hyoscyamine, hyoscine butylbromide and hydrobromide, ipratropium, tropicamide, cyclopentolate, pirenzepine and scopolamine.

Muscarinic antagonists such as ipratropium bromide can also be effective in treating asthma, since acetylcholine is known to cause smooth muscle contraction, especially in the bronchi.

Comparison table

Overview

Substance	Selectivity	Clinical use	Adverse effects	Notes	Trade names
Atropine (D/L-Hyoscyamine)	NS			CD	Symax, HyoMax, Anaspaz, Egazil, Buwecon, Cystospaz, Levsin, Levbid, Levsinex, Donnamar, NuLev, Spacol T/S and Neoquess
Atropine methonitrate	NS			title=Rang & Dale's pharmacology	author1=Rod Flower	author2=Humphrey P. Rang	author3=Maureen M. Dale	author4=Ritter, James M.	publisher=Churchill Livingstone	year=2007	isbn=978-0-443-06911-6	location=Edinburgh}}
Aclidinium bromide	Selective			Long acting antagonist	Tudorza
Benztropine	M1-selective			Reduces the effects of the relative central cholinergic excess that occurs as a result of dopamine deficiency.	Cogentin
Cyclopentolate	NS			Short acting, CD
Diphenhydramine	NS			Acts in the central nervous system, blood vessels and smooth muscle tissues	Benadryl, Nytol
Doxylamine	NS				Unisom
Dimenhydrinate				Combination of diphenhydramine with a methylxanthine salt	Dramamine, Gravol
Dicyclomine					Bentyl
Darifenacin	Selective for M3	Urinary incontinence	Few side effects		Enablex
Flavoxate					Urispas
Glycopyrrolate (Glycopyrronium bromide)	NS			last1=Chabicovsky	first1=Monika	last2=Winkler	first2=Swantje	last3=Soeberdt	first3=Michael	last4=Kilic	first4=Ana	last5=Masur	first5=Clarissa	last6=Abels	first6=Christoph	title=Pharmacology, toxicology and clinical safety of glycopyrrolate	journal=Toxicology and Applied Pharmacology	date=1 May 2019	volume=370	pages=154–169	doi=10.1016/j.taap.2019.03.016	pmid=30905688	s2cid=85498396	issn=1096-0333}}	Robinul, Cuvposa, Seebri
Hydroxyzine				Very mild/negligible action	Vistaril, Atarax
Ipratropium bromide	NS	Asthma and bronchitis		Lacks mucociliary excretion inhibition.	Atrovent and Apovent
Mebeverine				A muscolotropic spasmolytic with a strong and selective action on the smooth muscle spasm of the gastrointestinal tract, in particular of the colon.	Colofac, Duspatal, Duspatalin
Oxybutynin	M1/3/4 selective				Ditropan
Pirenzepine	M1-selective		(fewer than non-selective ones)	Inhibits gastric secretion
Procyclidine	NS		Overdose produces confusion, agitation and sleeplessness that can last up to or more than 24 hours. Pupils become dilated and unreactive to light. Tachycardia (fast heart beat), as well as auditory and visual hallucinations
Scopolamine (L-Hyoscine)	NS			CD	Scopace, Transderm-Scop, Maldemar, Buscopan
Solifenacin				Competitive antagonist	Vesicare
Tropicamide	NS			Short acting, CD
Tiotropium					Spiriva
Trihexyphenidyl/Benzhexol	M1 selective	PD	Drug at relative dose has 83% activity of atropine, thus has the same side-effects		Artane
Tolterodine					Detrusitol, Detrol

The muscarinic acetylcholine receptor subtype sectivities of a large number of antimuscarinic drugs have been reviewed.

Binding affinities

Anticholinergics

Compound	M1	M2	M3	M4	M5	Species	Ref
3-Quinuclidinyl benzilate	0.035–0.044	0.027–0.030	0.080–0.088	0.034–0.037	0.043–0.065	Human	vauthors = Bolden C, Cusack B, Richelson E	title = Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells	journal = J. Pharmacol. Exp. Ther.	volume = 260	issue = 2	pages = 576–80	year = 1992	pmid = 1346637 }}
4-DAMP	0.57–0.58	3.80–7.3	0.37–0.52	0.72–1.17	0.55–1.05	Human
AF-DX 250	427	55.0	692	162	3020	Human
AF-DX 384	30.9	6.03	66.1	10.0	537	Human
AQ-RA 741	28.8	4.27	63.1	6.46	832	Human
Atropine	0.21–0.50	0.76–1.5	0.15–1.1	0.13–0.6	0.21–1.7	Human	vauthors = Buckley NJ, Bonner TI, Buckley CM, Brann MR	title = Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells	journal = Mol. Pharmacol.	volume = 35	issue = 4	pages = 469–76	year = 1989	pmid = 2704370 }}
Benzatropine (benztropine)	0.231	1.4	1.1	1.1	2.8	Human
Biperiden	0.48	6.3	3.9	2.4	6.3	Human
Darifenacin	5.5–13	47–77	0.84–2.0	8.6–22	2.3–5.4	Human
Dicycloverine (dicyclomine)	57 (IC50)	415 (IC50)	67 (IC50)	97 (IC50)	53 (IC50)	Human/rat
Glycopyrrolate	0.37	1.38	1.31	0.41	1.30	Human
Hexahydrodifenidol	11	200	16	76 (IC50)	83	Human/rat
Hexahydrosiladifenidol	44	249	10	298 (IC50)	63	Human/rat
(R)-Hexbutinol	2.09	20.9	2.14	3.02	5.50	Human
Hexocyclium	2.3	23	1.4	5.5	3.7	Human/rat
Himbacine	107	10.0	93.3	11.0	490	Human
Ipratropium	0.49	1.5	0.51	0.66	1.7	Human	vauthors = Hirose H, Aoki I, Kimura T, Fujikawa T, Numazawa T, Sasaki K, Sato A, Hasegawa T, Nishikibe M, Mitsuya M, Ohtake N, Mase T, Noguchi K	title = Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity	journal = J. Pharmacol. Exp. Ther.	volume = 297	issue = 2	pages = 790–7	year = 2001	pmid = 11303071 }}
Methoctramine	16–50	3.6–14.4	118–277	31.6–38.0	57–313	Human
N-Methylscopolamine	0.054–0.079	0.083–0.251	0.052–0.099	0.026–0.097	0.106–0.125	Human	vauthors = Dörje F, Wess J, Lambrecht G, Tacke R, Mutschler E, Brann MR	title = Antagonist binding profiles of five cloned human muscarinic receptor subtypes	journal = J. Pharmacol. Exp. Ther.	volume = 256	issue = 2	pages = 727–33	year = 1991	pmid = 1994002 }}
Orphenadrine	48	213	120	170	129	Human
Otenzepad (AF-DX 116)	1300	186	838	1800 (IC50)	2800	Human/rat
Oxybutynin	0.66	13	0.72	0.54	7.4	Human
pFHHSiD	22.4	132	15.5	31.6	93.3	Human
Pirenzepine	6.3–8	224–906	75–180	17–37	66–170	Human
Procyclidine	4.6	25	12.4	7	24	Human
Propiverine	476	2970	420	536	109	Human
Scopolamine (hyoscine)	1.1	2.0	0.44	0.8	2.07	Human
Silahexacyclium	2.0	35	1.2	3.2	2.0	Human/rat
Timepidium	34	7.7	31	18	11	Human
Tiquizium	4.1	4.0	2.8	3.6	8.2	Human
Trihexyphenidyl	1.6	7	6.4	2.6	15.9	Human
Tripitamine (tripitramine)	1.58	0.27	38.25	6.41	33.87	Human	vauthors = Maggio R, Barbier P, Bolognesi ML, Minarini A, Tedeschi D, Melchiorre C	title = Binding profile of the selective muscarinic receptor antagonist tripitramine	journal = Eur. J. Pharmacol.	volume = 268	issue = 3	pages = 459–62	year = 1994	pmid = 7805774	doi = 10.1016/0922-4106(94)90075-2}}
Zamifenacin	55	153	10	68	34	Human
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

Antihistamines

Compound	M1	M2	M3	M4	M5	Species	Ref
Brompheniramine	25700	32400	50100	67600	28800	Human	vauthors = Yasuda SU, Yasuda RP	title = Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes	journal = Pharmacotherapy	volume = 19	issue = 4	pages = 447–51	year = 1999	pmid = 10212017	doi = 10.1592/phco.19.6.447.31041	s2cid = 39502992 }}
Chlorphenamine (chlorpheniramine)	19000	17000	52500	77600	28200	Human
Cyproheptadine	12	7	12	8	11.8	Human
Diphenhydramine	80–100	120–490	84–229	53–112	30–260	Human	vauthors = Krystal AD, Richelson E, Roth T	title = Review of the histamine system and the clinical effects of H1 antagonists: basis for a new model for understanding the effects of insomnia medications	journal = Sleep Med Rev	volume = 17	issue = 4	pages = 263–72	year = 2013	pmid = 23357028	doi = 10.1016/j.smrv.2012.08.001 }}
Doxylamine	490	2100	650	380	180	Human
Mequitazine	5.6	14	5.3	11.1	11.0	Human
Terfenadine	8710	8510	5250	30900	11200	Human
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

Antidepressants

Compound	M1	M2	M3	M4	M5	Species	Ref
Amitriptyline	14.7	11.8	12.8	7.2	15.7	Human	vauthors = Stanton T, Bolden-Watson C, Cusack B, Richelson E	title = Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics	journal = Biochem. Pharmacol.	volume = 45	issue = 11	pages = 2352–4	year = 1993	pmid = 8100134	doi = 10.1016/0006-2952(93)90211-e}}
Bupropion	35,000	35,000	35,000	35,000	35,000	Human
Citalopram	1430	ND	ND	ND	ND	Human	vauthors = Owens JM, Knight DL, Nemeroff CB	title = [Second generation SSRIS: human monoamine transporter binding profile of escitalopram and R-fluoxetine]	language = fr	journal = Encephale	volume = 28	issue = 4	pages = 350–5	year = 2002	pmid = 12232544 }}
Desipramine	110	540	210	160	143	Human
Desmethylcitalopram	10000	10000	10000	10000	10000	Human
Desmethyldesipramine	404	927	317	629	121	Human	vauthors = Deupree JD, Montgomery MD, Bylund DB	title = Pharmacological properties of the active metabolites of the antidepressants desipramine and citalopram	journal = Eur. J. Pharmacol.	volume = 576	issue = 1–3	pages = 55–60	year = 2007	pmid = 17850785	pmc = 2231336	doi = 10.1016/j.ejphar.2007.08.017 }}
Desvenlafaxine	10000	10000	10000	10000	10000	Human	vauthors = Deecher DC, Beyer CE, Johnston G, Bray J, Shah S, Abou-Gharbia M, Andree TH	title = Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor	journal = J. Pharmacol. Exp. Ther.	volume = 318	issue = 2	pages = 657–65	year = 2006	pmid = 16675639	doi = 10.1124/jpet.106.103382	s2cid = 15063064 }}
Dosulepin (dothiepin)	18	109	38	61	92	Human
Doxepin	18–38	160–230	25–52	20–82	5.6–75	Human
Escitalopram	1242	ND	ND	ND	ND	Human
Etoperidone	35000	35000	35000	35000	35000	Human
Femoxetine	92	150	220	470	400	Human
Fluoxetine	702–1030	2700	1000	2900	2700	Human
Fluvoxamine	31200	ND	ND	ND	ND	Human
Imipramine	42	88	60	112	83	Human
Lofepramine	67	330	130	340	460	Human
Norfluoxetine	1200	4600	760	2600	2200	Human
Nortriptyline	40	110	50	84	97	Human
Paroxetine	72–300	340	80	320	650	Human
Sertraline	427–1300	2100	1300	1400	1900	Human
Tianeptine	10000	10000	10000	10000	10000	Human	title = PDSP Ki Database	work = Psychoactive Drug Screening Program (PDSP)	author1 = Roth, BL	author2 = Driscol, J	publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health	access-date = 14 August 2017	url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testDDRadio=testDDRadio&testLigandDD=tianeptine&testLigand=&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}
Trazodone	35,000	35,000	35,000	35,000	35,000	Human
Venlafaxine	35000	35000	35000	35000	35000	Human
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

Antipsychotics

Compound	M1	M2	M3	M4	M5	Species	Ref
Amisulpride	10,000	10,000	10,000	10,000	10,000	Human	vauthors = Abbas AI, Hedlund PB, Huang XP, Tran TB, Meltzer HY, Roth BL	author6-link=Bryan Roth	title = Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo	journal = Psychopharmacology	volume = 205	issue = 1	pages = 119–28	year = 2009	pmid = 19337725	pmc = 2821721	doi = 10.1007/s00213-009-1521-8 }}
Aripiprazole	6780	3510	4680	1520	2330	Human	vauthors = Shapiro DA, Renock S, Arrington E, Chiodo LA, Liu LX, Sibley DR, Roth BL, Mailman R	title = Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology	journal = Neuropsychopharmacology	volume = 28	issue = 8	pages = 1400–11	year = 2003	pmid = 12784105	doi = 10.1038/sj.npp.1300203	doi-access = free }}
Asenapine	10000	10000	10000	10000	ND	Human
Bromperidol	7600	1800	7140	1700	4800	Human
Chlorprothixene	11	28	22	18	25	Human
Chlorpromazine	25	150	67	40	42	Human
Clozapine	1.4–31	7–204	6–109	5–27	5–26	Human	vauthors = Bymaster FP, Felder CC, Tzavara E, Nomikos GG, Calligaro DO, Mckinzie DL	title = Muscarinic mechanisms of antipsychotic atypicality	journal = Prog. Neuropsychopharmacol. Biol. Psychiatry	volume = 27	issue = 7	pages = 1125–43	year = 2003	pmid = 14642972	doi = 10.1016/j.pnpbp.2003.09.008	s2cid = 28536368 }}
Cyamemazine (cyamepromazine)	13	42	32	12	35	Human	vauthors = Hameg A, Bayle F, Nuss P, Dupuis P, Garay RP, Dib M	title = Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes	journal = Biochem. Pharmacol.	volume = 65	issue = 3	pages = 435–40	year = 2003	pmid = 12527336	doi = 10.1016/s0006-2952(02)01515-0}}
N-Desmethylclozapine	67.6	414.5	95.7	169.9	35.4	Human	title = PDSP Ki Database	work = Psychoactive Drug Screening Program (PDSP)	author1 = Roth, BL	author2 = Driscol, J	publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health	access-date = 14 August 2017	url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testDDRadio=testDDRadio&testLigandDD=1973&testLigand=&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}
Fluperlapine	8.8	71	41	14	17	Human
Fluphenazine	1095	7163	1441	5321	357	Human	title = PDSP Ki Database	work = Psychoactive Drug Screening Program (PDSP)	author1 = Roth, BL	author2 = Driscol, J	publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health	access-date = 14 August 2017	url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=fluphenazine&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}
Haloperidol	10000	10000	10000	10000	10000	Human
Iloperidone	4898	3311	10000	8318	10000	Human	vauthors = Kalkman HO, Subramanian N, Hoyer D	title = Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders	journal = Neuropsychopharmacology	volume = 25	issue = 6	pages = 904–14	year = 2001	pmid = 11750183	doi = 10.1016/S0893-133X(01)00285-8	doi-access = free }}
Loxapine	63.9–175	300–590	122–390	300–2232	91–241	Human	title = PDSP Ki Database	work = Psychoactive Drug Screening Program (PDSP)	author1 = Roth, BL	author2 = Driscol, J	publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health	access-date = 14 August 2017	url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=loxapine&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}
Melperone	15000	2400	15000	4400	15000	Human
Mesoridazine	10	15	90	19	60	Human
Molindone	ND	ND	10000	ND	ND	Human	vauthors = Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL	title = H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs	journal = Neuropsychopharmacology	volume = 28	issue = 3	pages = 519–26	year = 2003	pmid = 12629531	doi = 10.1038/sj.npp.1300027	doi-access = free }}
Olanzapine	1.9–73	18–96	13–132	10–32	6–48	Human	vauthors = Bymaster FP, Calligaro DO, Falcone JF, Marsh RD, Moore NA, Tye NC, Seeman P, Wong DT	title = Radioreceptor binding profile of the atypical antipsychotic olanzapine	journal = Neuropsychopharmacology	volume = 14	issue = 2	pages = 87–96	year = 1996	pmid = 8822531	doi = 10.1016/0893-133X(94)00129-N	doi-access = free }}
Perphenazine	ND	ND	1848	ND	ND	Human
Pimozide	ND	ND	1955	ND	ND	Human
Quetiapine	120–135	630–705	225–1320	660–2990	2990	Human
Remoxipride	10000	10000	10000	10000	ND	Human
Rilapine	190	470	1400	1000	1100	Human
Risperidone	11000	≥3700	13000	≥2900	15000	Human
Sertindole	ND	ND	2692	ND	ND	Human
Tenilapine	260	62	530	430	660	Human
Thioridazine	2.7	14	15	9	13	Human
Thiothixene	10000	10000	10000	10000	5376	Human	title = PDSP Ki Database	work = Psychoactive Drug Screening Program (PDSP)	author1 = Roth, BL	author2 = Driscol, J	publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health	access-date = 14 August 2017	url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testDDRadio=testDDRadio&testLigandDD=thiothixene&testLigand=&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}
cis-Thiothixene	2600	2100	1600	1540	4310	Human
Tiospirone	630	180	1290	480	3900	Human
Trifluoperazine	ND	ND	1001	ND	ND	Human
Ziprasidone	≥300	3000	1300	1600	1600	Human	title = PDSP Ki Database	work = Psychoactive Drug Screening Program (PDSP)	author1 = Roth, BL	author2 = Driscol, J	publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health	access-date = 14 August 2017	url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=ziprasidone&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}}
Zotepine	18	140	73	77	260	Human
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.

References

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(1 May 2019). "Pharmacology, toxicology and clinical safety of glycopyrrolate". Toxicology and Applied Pharmacology.
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