Acute effects of nicotine on prolactin release in the rat: agonist and antagonist effects of a single injection of nicotine
Abstract
The effects of nicotine on prolactin release were studied in conscious, unrestrained rats in which an indwelling jugular cannula allowed multiple samplings of blood after i.v. administration of nicotine. Intravenous administration of nicotine bitartrate dihydrate increases plasma prolactin concentrations in a dose-dependent manner with an ED50 of approximately 100 micrograms/kg (200 nmol/kg) and this effect is blocked completely by pretreatment with mecamylamine, indicating that it is mediated by a nicotinic cholinergic receptor. Intracerebral ventricular injection of 1 microgram of nicotine also increases plasma prolactin levels, but i.v. injection of this same amount of nicotine has no effect, indicating that nicotine acts within the brain to release prolactin. A single i.v. injection of nicotine resulted in desensitization of the prolactin response to a subsequent injection of nicotine given 1 to 2 hr later, thus confirming a previous report by Sharp and Beyer (J. Pharmacol. Exp. Ther. 238: 486-491, 1986). The prolactin response to nicotine was restored within 24 hr after a single injection. The acute desensitization after a single injection of nicotine appears to be specific to release of prolactin by nicotine because the prolactin response to morphine was unaffected 1 hr after injection of nicotine. A single injection of nicotine appears to desensitize the prolactin response to a subsequent injection of nicotine with an ED50 of approximately 20 micrograms/kg (40 nmol/kg), indicating that nicotine is even more potent in stimulating desensitization of nicotinic cholinergic receptors than in stimulating prolactin release. These results support the concept that nicotine acts as a time-averaged antagonist.(ABSTRACT TRUNCATED AT 250 WORDS)
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Giving nicotine can cause receptors to remain desensitized for extended periods.
“As a time-averaged antagonist, nicotine administration can result in prolonged periods of receptor desensitization (Hulihan-Giblin et al., 1990).”
From Nicotinic Partial Agonists Varenicline and Sazetidine-A Have Differential Effects on Affective Behavior (2010) · cites this paper as Hulihan-Giblin et al., 1990
In living animals, nicotine desensitizes these receptors at roughly one-eighth the concentration needed to activate them.
“in fact, it is approximately eight times more potent to desensitize these receptors than to activate them in vivo (Hulihan-Giblin et al., 1990)”
From Chronic Sazetidine-A at Behaviorally Active Doses Does Not Increase Nicotinic Cholinergic Receptors in Rodent Brain (2012) · cites this paper as Hulihan-Giblin et al., 1990
Nicotine strongly desensitizes nicotinic receptors.
“Nicotine potently desensitizes nAChRs (Sharp and Beyer, 1986;Hulihan-Giblin et al., 1990;Grady et al., 1994;Marks et al., 1994;Lester and Dani, 1995;Pidoplichko et al., 1997; for reviews, see Meyer et al., 2001;Picciotto et al., 2008;Buccafusco et al., 2009);”
From Chronic Sazetidine-A at Behaviorally Active Doses Does Not Increase Nicotinic Cholinergic Receptors in Rodent Brain (2012) · cites this paper as Hulihan-Giblin et al., 1990
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- Authors
- Hulihan-Giblin, B. A., Lumpkin, M. D., & Kellar, K. J.
- Affiliations
- Georgetown University (US)
- ORCID
- Kellar, K J
- Venue
- The Journal of Pharmacology and Experimental Therapeutics
- Publisher
- Elsevier BV
- Published
- 1990-01
- Volume
- 252
- Issue
- 1
- Pages
- 15-20
- ISSN
- 0022-3565 (ISSN-L)
- OpenAlex
- W1856037288
- Cited by
- 77
- References
- 0
- Citations by year
- 2025: 1 · 2019: 3 · 2018: 1 · 2016: 1 · 2015: 5 · 2014: 3 · 2013: 5 · 2012: 2
- FWCI
- 0.56
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Pharmacology and Experimental Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- PubMed
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Health Sciences › Medicine › Physiology › Smoking Behavior and Cessation
- Keywords
- nicotine, prolactin secretion, nicotinic acetylcholine receptors, receptor desensitization, mecamylamine, morphine, plasma prolactin, dose-response relationship
- MeSH terms
- Animals, Brain, Dose-Response Relationship, Drug, Injections, Intraventricular, Male, Mecamylamine, Morphine, Nicotine, Prolactin, Rats, Inbred Strains, Receptors, Nicotinic, Rats
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