Muscle relaxant

Pridinol is a piperidine substituted at position 1 by a 3-hydroxy-3,3-diphenylpropyl group. It has a role as a muscle relaxant and an antiparkinson drug. It is a tertiary alcohol and a member of piperidines.. Pridinol can be prepared by Grignard reaction of ethyl 3-piperidinopropionate with phenylmagnesium bromide. May be prepared from ethyl 1-piperidinepropionate and phenylmagnesium bromide

A randomized, double-blind, placebo-controlled three-way cross-over study was performed to investigate the effect of two muscle relaxants (tolperisone hydrochloride and pridinol mesilate) on experimental jaw-muscle pain and jaw-stretch reflexes. Fifteen healthy men participated in three randomized sessions separated by at least 1 week. In each session 300 mg tolperisone, 8 mg pridinol mesilate or placebo was administered orally as a single dose. One hour after drug administration 0.3 mL hypertonic saline (5.8%) was injected into the right masseter to produce muscle pain. Subjects continuously rated their perceived pain intensity on an electronic 10-cm visual analogue scale (VAS). The pressure pain threshold (PPT) was measured and short-latency reflex responses were evoked in the pre-contracted (15% maximal voluntary contraction) masseter and temporalis muscles by a standardised stretch device (1 mm displacement, 10 ms ramp time) before (baseline), 1 hr after medication (post-drug), during ongoing experimental muscle pain (pain-post-drug), and 15 min after pain had vanished (post-pain). Analysis of variance demonstrated significantly lower VAS peak pain scores (5.9 +/- 0.4 cm) after administration of tolperisone hydrochloride compared with pridinol mesilate (6.8 +/- 0.4 cm) and placebo (6.6 +/- 0.4 cm) (P=0.020). Administration of pridinol mesilate was associated with a significant decrease in PPTs compared with tolperisone hydrochloride and placebo (P=0.002) after medication, but not after experimental jaw-muscle pain. The normalized peak-to-peak amplitude of the stretch reflexes were not significantly influenced by the test medication (P=0.762), but were in all sessions significantly facilitated during ongoing experimental jaw-muscle pain (P=0.034). In conclusion, tolperisone hydrochloride provides a small, albeit significant reduction in the perceived intensity of experimental jaw-muscle pain whereas the present dose had no effect on the short-latency jaw-stretch reflex. /Tolperisone hydrochloride and pridinol mesilate/

The intraperitoneal LD50 for mice is 100 mg/kg.
Antidote and First Aid Measures
/SRP:/ Immediately take first aid measures: Ensure adequate decontamination has been performed. If the patient stops breathing, begin artificial respiration immediately, preferably using a demand ventilator, bag-valve-mask, or simple breathing mask, and follow the training instructions. Perform cardiopulmonary resuscitation if necessary. Immediately flush contaminated eyes with running water. Do not induce vomiting. If vomiting occurs, tilt the patient forward or place them in the left lateral decubitus position (head down if possible) to maintain an open airway and prevent aspiration. Keep the patient calm and maintain normal body temperature. Seek medical attention. /Toxins A and B/ Currance, PL Clements, B., Bronstein, AC (Eds).; First Aid for Hazardous Substance Exposure. 3rd ed., Elsevier Mosby, St. Louis, Missouri, 2005, p. 100. 160
/SRP:/ Basic treatment: Establish a patent airway (using oropharyngeal or nasopharyngeal airways if necessary). Suction if necessary. Observe for signs of respiratory failure and provide assisted ventilation if necessary. Administer oxygen via a non-invasive mask at a flow rate of 10 to 15 liters per minute. Monitor for pulmonary edema and treat as necessary… Monitor for shock and treat as necessary… Anticipate seizures and treat as necessary… If eyes are contaminated, flush with water immediately. During transport, continuously flush each eye with 0.9% normal saline (NS)… Do not use emetics. If swallowed, rinse mouth and dilute with 5 mL/kg to 200 mL of water, provided the patient is able to swallow, has a strong gag reflex, and does not drool… After disinfecting skin burns, cover with a dry, sterile dressing… /Toxins A and B/ Currance, PL Clements, B., Bronstein, AC (eds.).; First aid for exposure to hazardous substances. 3rd Edition, Elsevier Mosby, St. Louis, Missouri, 2005, p. 160
/SRP:/ Advanced Treatment: For patients with altered mental status, severe pulmonary edema, or severe respiratory distress, consider oropharyngeal or nasopharyngeal endotracheal intubation to control the airway. Positive pressure ventilation with a bag-valve-mask may be effective. Consider medical treatment for pulmonary edema… Consider the use of a beta-agonist (such as salbutamol) for severe bronchospasm… Monitor heart rhythm and treat arrhythmias as needed… Start intravenous infusion of 5% glucose solution /SRP: “Keep it patent”, minimum flow rate/. If signs of hypovolemia appear, use 0.9% normal saline (NS) or lactated Ringer's solution. Administer fluids with caution in cases of hypotension with signs of hypovolemia. Watch for signs of fluid overdose… Use diazepam or lorazepam for seizures… Use promecaine hydrochloride to assist eye irrigation… /Toxins A and B/ Currance, PL Clements, B., Bronstein, AC (eds.).; Emergency Care for Exposure to Hazardous Substances. 3rd ed., Elsevier Mosby, St. Louis, Missouri, 2005, pp. 160-161.
Non-human Toxicity Values

Mouse Intravenous LD50 35 mg/kg /Prilinol Hydrochloride/

Acta Crystallogr B Struct Sci Cryst Eng Mater. 2018 Jun 1;74(Pt 3):304-310.

Prilinol is a piperidine compound with a 3-hydroxy-3,3-diphenylpropyl group substituted at the 1-position. It has the effects of a muscle relaxant and an anti-Parkinson's disease drug. It is a tertiary alcohol belonging to the piperidine class of compounds.

---

Therapeutic Use
/EXPL THER/ A randomized, double-blind, placebo-controlled, phase III crossover study investigated the effects of two muscle relaxants (topaphene hydrochloride and prilinol mesylate) on experimental mandibular muscle pain and mandibular stretch reflex. Fifteen healthy men participated in three randomized trials, each at least one week apart. In each trial, subjects received a single oral dose of 300 mg topaphene, 8 mg prilinol mesylate, or placebo. One hour after administration, 0.3 mL of hypertonic saline (5.8%) was injected into the right masseter muscle to induce muscle pain. Subjects continuously assessed their perceived pain intensity using a 10 cm electronic visual analog scale (VAS). The pressure pain threshold (PPT) of the masseter and temporalis muscles at precontraction (15% of maximal voluntary contraction) was measured using a standardized traction device (1 mm displacement, 10 ms rise time) before administration (baseline), 1 hour after administration (post-administration), during sustained experimental muscle pain (post-administration pain), and 15 minutes after pain subsidence (post-pain). Analysis of variance showed that the peak VAS pain score was significantly lower after administration of tolperdone hydrochloride (5.9 ± 0.4 cm) compared to pyridinol mesylate (6.8 ± 0.4 cm) and placebo (6.6 ± 0.4 cm) (P = 0.020). The pain threshold (PPT) was significantly lower after administration of prilinol mesylate compared to tolperdone hydrochloride and placebo (P = 0.002), but this was not observed after experimental jaw muscle pain. The test drug had no significant effect on the peak-to-peak amplitude of the stretch reflex (P=0.762), but during sustained experimental jaw muscle pain, the peak-to-peak amplitude of the stretch reflex was significantly enhanced in all experimental phases (P=0.034). In summary, tolperdone hydrochloride slightly but significantly reduced the perceived intensity of experimental jaw muscle pain, while the dose in this study had no effect on the short-latency jaw stretch reflex. /Tolperdone hydrochloride and prilnor mesylate/

295.4186

295.194

C, 81.31; H, 8.53; N, 4.74; O, 5.42

511-45-5

968-58-1 (HCl); 511-45-5;

4904

Crystals

1.079 g/cm3

460.9ºC at 760 mmHg

120-121 °C

229.9ºC

3.736

1

2

5

22

294

0

C1=CC=C(C=C1)C(CCN2CCCCC2)(C3=CC=CC=C3)O

RQXCLMGKHJWMOA-UHFFFAOYSA-N

InChI=1S/C20H25NO/c22-20(18-10-4-1-5-11-18,19-12-6-2-7-13-19)14-17-21-15-8-3-9-16-21/h1-2,4-7,10-13,22H,3,8-9,14-17H2

1,1-diphenyl-3-piperidin-1-ylpropan-1-ol

pridinol; 511-45-5; 1,1-diphenyl-3-(piperidin-1-yl)propan-1-ol; Nonplesin; Lyseen; Parks; Parks 12; Parks 12 hommel;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

---

Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

View More

Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

---

Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

View More

Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

---

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

---

 (Please use freshly prepared in vivo formulations for optimal results.)