Meptazinol HCl

For research use only.

Catalog No.S3204

Meptazinol HCl Chemical Structure

CAS No. 59263-76-2

Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM.

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Biological Activity

Description Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM.
opioid receptor [1]
In vitro

Meptazinol inhibits a portion of 3H-labeled opiate and opioid peptide binding quite potently, with IC50 value under 1 nM. [1]

In vivo Naloxonazine treatment 24 hr earlier attenuates Meptazinol (10 mg/kg i.v.) analgesia in both the mouse writhing and rat tail-flick assays. Meptazinol administered with morphine does not reverse the respiratory depressant actions seen with morphine alone, distinguishing meptazinol from other mixed agonist/antagonists. [1] The absorption of Meptazinol (8 mg/kg i.v.) from nasal cavity to systemic circulation is rapid and complete in male Sprague-Dawley rats. The maximum observed concentration is achieved at 15 min after administration and the absolute bioavailability is 96.06%. The cerebrospinal fluid level of Meptazinol (8 mg/kg i.v.) attains a high concentration of 2.71 μg/mL and then is followed by an exponential decline. The concentration of intravenous Meptazinol (8 mg/kg i.v.) achieves a peak at 10 min followed by a steep decline in the cortex dialysate. [2] Inclusion of Meptazinol (2 mg/kg) reduces the total dose of anaesthetic required, allows a more rapid recovery and is associated with less movement in response to surgery in cystoscopy patients. The patients in the control group tends to hyperventilate, and has lower end-tidal CO2 tension, and also higher pulse rates during surgery than the Meptazinol group. [3] Meptazinol (25 mg/kg) evokes larger increases in nociceptive thresholds in the mouse than in the rat, whereas morphine induces large increases in both species. Antinociceptive responses to Meptazinol are consistently inhibited in animals pretreated with naloxone, whereas scopolamine attenuates the effects of meptazinol in some, particularly the mouse tail immersion test. [4] Meptazinol (2 mg/kg i.v.) greatly reduces the incidence of ventricular extrasystoles that resulted from acute coronary artery occlusion as well as ventricular fibrillation (VF) in rats. Meptazinol also reduces ventricular arrhythmias, including fibrillation, in conscious rats subjected to coronary artery occlusion. [5]


Solubility (25°C)

In vitro DMSO 53 mg/mL (196.43 mM)
Water 53 mg/mL (196.43 mM)
Ethanol 53 mg/mL (196.43 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 269.81


CAS No. 59263-76-2
Storage powder
in solvent
Synonyms N/A
Smiles CCC1(CCCCN(C1)C)C2=CC(=CC=C2)O.Cl

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Opioid Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID