Meptazinol HCl 59263-76-2

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Molecular Weight: 269.81 Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM.

Biological Activity

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


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 m orphine does not reverse the respiratory
depressant actions seen with m orphine alone, distinguishing meptazinol
from other mixed agonist/antagonists. 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. 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.


Meptazinol (25
mg/kg) evokes larger increases in nociceptive thresholds in the mouse
than in the rat, whereas mo rphine 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. 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.






Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	269.81
Formula	C15H23NO.HCl
CAS No.	59263-76-2

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	54 mg/mL (200.14 mM)
		Water	54 mg/mL (200.14 mM)
		Ethanol	54 mg/mL (200.14 mM)

Chemical Name	Phenol, 3-(3-ethylhexahydro-1-methyl-1H-azepin-3-yl)-, hydrochloride (1:1)

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Product Categories : Neuronal Signaling > Opioid Receptor Inhibitor