Cat. No.: HY-170032

Oxotremorine

Oxotremorine is a potent muscarinic acetylcholine receptor (mAChR) agonist capable of crossing the blood-brain barrier. Oxotremorine specifically binds to and activates mAChR, mediating synaptic transmission, influencing the survival and differentiation of nerve cells, and inducing symptoms associated with cholinergic overactivation in animals. Oxotremorine can be used as a pharmacological agent to induce symptoms such as tremors, hypothermia, and salivation in experimental animals. Oxotremorine is utilized in research on neurological disorders, including Parkinson’s disease and depression.

For research use only. We do not sell to patients.

CAS No.: 70-22-4
Formula: C₁₂H₁₈N₂O
Molecular Weight:206.28

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (289 KB)

Oxotremorine Chemical Structure

CAS No.: 70-22-4

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Induced Disease Models
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[4]

mAChR1

mAChR2

mAChR3

All mAChR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.0023 μM Compound: Oxotremorine	Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells. Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.	[PMID: 11597415]
CHO	IC₅₀	0.4 μM Compound: oxotremorine	Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2 Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2	[PMID: 9438027]
CHO	IC₅₀	17 μM Compound: oxotremorine	Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3 Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3	[PMID: 9438027]
CHO	IC₅₀	27.1 μM Compound: Oxotremorine	Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells. Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.	[PMID: 11597415]
CHO	IC₅₀	5 μM Compound: oxotremorine	Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4 Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4	[PMID: 9438027]
CHO	IC₅₀	8 μM Compound: oxotremorine	Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5 Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5	[PMID: 9438027]
CHO	IC₅₀	9 μM Compound: oxotremorine	Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M1 Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M1	[PMID: 9438027]
HEK293	EC₅₀	0.0016 μM Compound: Oxotremorine	Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay	[PMID: 25765911]
Vero C1008	IC₅₀	>2.0 × 10⁵M Compound: COVC-1214897898	Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging	10.6019/CHEMBL4651402

In Vitro

Cell Cycle RegulationApoptosisOthers

Cell Cycle Regulation

Apoptosis

Oxotremorine (200 μM; 1-7 days) induces cell growth arrest at the G0/G1 and G2/M phases in PC12M1 cells^[6].
Oxotremorine (200 μM; 1-24 h) inhibits DNA synthesis in PC12M1 cells^[6].
Oxotremorine (200 μM; 1-3 days) inhibits apoptosis in serum-deprived PC12M1 cells^[6].

Oxotremorine (200 μM; 24-48 h) promotes cell survival and inhibits apoptosis in growth factor-deprived PC12M1 neuronal cells^[6].

Others

Oxotremorine sesquifumarate (0.1 nM–100 μM; 120 min) competitively inhibits [3H]QNB binding in rat heart homogenates, with an IC₅₀ of 0.12 μM in the absence of sodium ions. In the presence of 140 mM sodium ions, the IC₅₀ is 1.00 μM; when combined with 1 μM Gpp(NH)p (HY-137167) and 140 mM Na⁺, the IC₅₀ reaches 5.40 μM^[11].
Oxotremorine sesquifumarate (3 μM; 20 min) significantly inhibits potassium-stimulated [3H]GABA release in rat thalamic slices^[12].
Oxotremorine sesquifumarate triggers dynamic mass redistribution (DMR) signals and activates endogenous M3 receptors in HCT-15, HT-29, SF268, PC3, and CCRF-CEM cells, while showing almost no activity in HeLa cells^[13].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[6]

Cell Line:

PC12M1 cells (serum-deprived)
Concentration:

200 μM
Incubation Time:

1, 2, 3 days
Result:

Inhibited serum deprivation-induced cell death, and this protective effect was blocked by Atropine (HY-B1205).

Apoptosis Analysis^[6]

Cell Line:

PC12M1 cells (serum-deprived)
Concentration:

200 μM
Incubation Time:

24 h, 48 h, 72 h
Result:

Significantly reduced the apoptotic cell population with subdiploid DNA content.

Cell Cycle Analysis^[6]

Cell Line:

PC12M1 cells (in serum-containing medium)
Concentration:

200 μM
Incubation Time:

1, 2, 3, and 7 days
Result:

Caused a gradual increase in the percentage of cells in the G2/M phase and a gradual decrease in the percentage of cells in the S phase, resulting in cell growth arrest at the G0/G1 and G2/M phases.

In Vivo

Oxotremorine (10-100 μg/kg; i.p.; single dose; tested 30 min post-injection) exhibits antinociceptive effects in the tail-flick test, hot-plate test, and a formalin-induced pain model in naked mole-rats^[3].
Oxotremorine (0.2 mg/kg; i.p.; once daily; for 10 consecutive days) restores impaired hippocampal neurogenesis, mitigates depression-like behaviors, and recovers hippocampal volume in a rat model of chronic restraint stress^[5].
Oxotremorine sesquifumarate (1.0-10.0 μg/side; bilateral microinjection into the nucleus accumbens; single administration; 2 h) reduces food and water intake and decreases locomotor activity in food-deprived Sprague-Dawley rats^[11].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Rat chronic restraint stress model^[5]
Dosage:

0.2 mg/kg
Administration:

i.p.; once daily; treated for 10 consecutive days post-stress.
Result:

Partially restored the stress-induced decrease in proliferation and survival of progenitor cells in the hippocampal SGZ and hilus.
Completely restored the differentiation of newly formed cells into neurons and reduced the abnormal increase in astrocyte differentiation.
Ameliorated stress-induced depression-like behavior by reducing immobility time in the forced swim test and restoring sucrose preference.
Restored the stress-induced reduction in total hippocampal volume.
Did not alter these physiological or behavioral parameters when administered alone to normal, unstressed rats.

Animal Model:

Rat^[11]
Dosage:

1.0, 10.0 μg/side
Administration:

bilateral microinfusion into the nucleus accumbens; single dose; tested for 2 h
Result:

Significantly reduced the food and water intake of starved rats over the 2-hour period.
Decreased locomotor activities such as rearing and ambulation, but did not decrease the number of approaches to the food monitor.

Related Protocols :

Synaptic current patch-clamp recording in brain slices

Induced Disease Models

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Induction of tremor and lacrimation model^[4]^[11]

Background

Oxotremorine produces potent parasympathomimetic and central effects by non-selectively activating central and peripheral muscarinic acetylcholine receptors^[4].

Specific Modeling Methods

Mice: male albino mice (Haffkine strain)
Administration: Oxotremorine (0.5 mg/kg) • single intraperitoneal injection
Mice: male ICR mice • 25-35 g
Administration: (1) Oxotremorine sesquifumarate (0.5 mg/kg) • Single subcutaneous (s.c.) injection; (2) 0.5 mg/kg • Single subcutaneous (s.c.) injection, following a 20-minute pretreatment with Phenylephrine (10 µg/kg; i.p.)

Note

(1) Since the onset of tremors following drug administration is almost immediate, the recording of tremors must begin immediately after the drug is administered.
(2) Behavioral assessments, such as the evaluation of tremors, must be conducted while the animals are in a conscious state.

Modeling Indicators

Animal Behavior Analysis : Presence of severe tremors, a significant drop in rectal temperature, signs of analgesia (loss of pain sensation), and noticeable lacrimation (tearing)

Related Products: Phenylephrine (HY-B0769)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 70-22-4
Molecular Weight 206.28
Formula C₁₂H₁₈N₂O
SMILES

O=C1N(CCC1)CC#CCN2CCCC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wang N, et al. Nicotinic acetylcholine receptor alpha5 subunits modulate oxotremorine-induced salivation and tremor. J Neurol Sci. 2004 Jul 15;222(1-2):87-91. [Content Brief]

[2]. Overstreet DH, et al. Genetic animal models of depression and ethanol preference provide support for cholinergic and serotonergic involvement in depression and alcoholism. Biol Psychiatry. 1992 May 1;31(9):919-36. [Content Brief]

[3]. Dulu TD, et al. The effects of oxotremorine, epibatidine, atropine, mecamylamine and naloxone in the tail-flick, hot-plate, and formalin tests in the naked mole-rat (Heterocephalus glaber). In Vivo. 2014 Jan-Feb;28(1):39-48. [Content Brief]

[4]. Barar FS, et al. Tremorine-oxotremorine-induced tremor, hypothermia and analgesia, and physostigmine toxicity, in mice after pretreatment with beta-adrenoceptor antagonists. J Pharm Pharmacol. 1976 Apr;28(4):286-9. [Content Brief]

[5]. Veena J, et al. Oxotremorine treatment restores hippocampal neurogenesis and ameliorates depression-like behaviour in chronically stressed rats. Psychopharmacology (Berl). 2011 Sep;217(2):239-53. [Content Brief]

[6]. Lindenboim L, et al. Activation of muscarinic receptors inhibits apoptosis in PC12M1 cells. J Neurochem. 1995 Jun;64(6):2491-9. [Content Brief]

[7]. Howell G 3rd, et al. In vivo antimuscarinic actions of the third generation antihistaminergic agent, desloratadine. BMC Pharmacol. 2005 Aug 18;5:13. [Content Brief]

[8]. Jones CK, et al. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J Neurosci. 2008 Oct 8;28(41):10422-33. [Content Brief]

[9]. Overstreet DH, et al. Stress-induced immobility in rats with cholinergic supersensitivity. Biol Psychiatry. 1986 Jun;21(7):657-64. [Content Brief]

[10]. Martin JR, et al. Drug induced hypothermia in adult and senescent rats. Neurobiol Aging. 1985 Summer;6(2):121-4. [Content Brief]

[11]. Pratt WE, et al. Nucleus accumbens acetylcholine and food intake: decreased muscarinic tone reduces feeding but not food-seeking. Behav Brain Res. 2009 Mar 2;198(1):252-7. [Content Brief]

[12]. Rosenberger LB, et al. Cardiac muscarinic cholinergic receptor binding is regulated by Na+ and guanyl nucleotides. J Biol Chem. 1980 Feb 10;255(3):820-3. [Content Brief]

[13]. Deng H, et al. Label-free cell phenotypic assessment of the biased agonism and efficacy of agonists at the endogenous muscarinic M3 receptors. J Pharmacol Toxicol Methods. 2013 Nov-Dec;68(3):323-33. [Content Brief]

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Oxotremorine

All mAChR Isoforms